Search Result
Results for "
EGFR-IN-2
" in MedChemExpress (MCE) Product Catalog:
2
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-100520
-
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EGFR
|
Cancer
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EGFR-IN-2 is a a noncovalent, irreversible, mutant-selective second generation EGFR inhibitor.
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-
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- HY-128860
-
|
EGFR
|
Cancer
|
Mutated EGFR-IN-2 (compound 91) is a mutant-selective EGFR inhibitor extracted from patent WO2017036263A1, which potently inhibits single-mutant EGFR (T790M) and double-mutant EGFR (including L858R/T790M (IC50=<1nM) and ex19del/T790M), and can suppress activity of single gain-of-function mutant EGFR (including L858R and ex19del) as well. Mutated EGFR-IN-2 shows anti-tumor antivity .
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-
-
- HY-155227A
-
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Anaplastic lymphoma kinase (ALK)
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Cancer
|
ALK/EGFR-IN-2 is a potent dual inhibitor of ALK and EGFR. ALK/EGFR-IN-2 induces apoptosis and G0/G1 cell cycle arrest in cancer cells. ALK/EGFR-IN-2 significantly inhibits the cell proliferation of H1975, PC9, and Baf3-EML4-ALK cancer cell lines with IC50s of 0.0034, 0.0065, and 0.0018 μM, respectively .
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-
- HY-168514
-
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SOS1
EGFR
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Cancer
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SOS1/EGFR-IN-2 (Compound 4) is a SOS1 and EGFR dual inhibitor with IC50s of 8.3 and 14.6 nM, respectively. SOS1/EGFR-IN-2 exhibits significant antiproliferative effect on the cancer cells haboring various KRAS mutants .
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-
-
- HY-162623
-
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EGFR
|
Cancer
|
EGFR/HER2-IN-15, a dihydropyrimidine, is a potent EGFR/HER2 inhibitor. EGFR/HER2-IN-15 significantly inhibits EGFR wt activity with an IC50 of 37.21 nM. EGFR/HER2-IN-15 has anticaner effects .
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-
-
- HY-151573
-
|
EGFR
CDK
|
Cancer
|
EGFR/CDK2-IN-1 (Compound 3b) is an EGFR/CDK2 inhibitor. EGFR/CDK2-IN-1 shows good cytotoxicity against MCF7 and HepG2 cells. EGFR/CDK2-IN-1 can be used in cancer research .
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-
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- HY-174414
-
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EGFR
|
Cancer
|
EGFR/HER2-IN-18 is a stable EGFR/HER2 dual inhibitor with IC50 values of 0.09 (EGFR) and 0.08 μM (HER2) respectively. EGFR/HER2-IN-18 exhibits broad-spectrum anti-cancer activity. EGFR/HER2-IN-18 induces MCF-7 cells apoptosis and inhibits the cell cycle. EGFR/HER2-IN-18 can be used for the study of breast cancer .
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-
-
- HY-161602
-
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EGFR
|
Cancer
|
EGFR/HER2-IN-13 (Compd 38) is an inhibitor of mutant EGFR/HER2s which are resistant to other drugs. EGFR/HER2-IN-13 can be used for cancer research .
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-
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- HY-161603
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EGFR
|
Cancer
|
EGFR/HER2-IN-14 (Compd 46) is an inhibitor of mutant EGFR/HER2s which are resistant to other drugs. EGFR/HER2-IN-14 can be used for cancer research .
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-
-
- HY-146238
-
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EGFR
Thymidylate Synthase
Apoptosis
|
Cancer
|
EGFR/HER2/TS-IN-1 (Compound 4d) is an EGFR, HER2 and TS (Thymidylate synthase) inhibitor with IC50 values of 0.203, 0.088 and 0.168 μM against EGFR, HER2 and TS, respectively. EGFR/HER2/TS-IN-1 induces MCF7 cell apoptosis .
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-
-
- HY-151156
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EGFR
Apoptosis
|
Cancer
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EGFR/HER2-IN-6 (compound 43) is an EGFR/HER2 and DHFR inhibitor. EGFR/HER2-IN-6 inhibits EGFR kinase, HER2 kinase and DHFR with IC50s of 0.122, 0.078 and 0.585 μM, respectively. EGFR/HER2-IN-6 shows anticancer activity against several cancer cell lines with high safety profile and selectivity indices. EGFR/HER2-IN-8 can be used for the research of cancer .
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-
-
- HY-151161
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EGFR
|
Cancer
|
EGFR/HER2-IN-8 (compound 34) is a EGFR/HER2 and DHFR inhibitor. EGFR/HER2-IN-8 inhibits EGFR kinase, HER2 kinase and DHFR with IC50s of 0.45, 0.244 and 5.669 μM, respectively. EGFR/HER2-IN-8 shows anticancer activity against several cancer cell lines with high safety profile and selectivity indices. EGFR/HER2-IN-8 can be used for the research of cancer .
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- HY-168073
-
|
EGFR
VEGFR
Apoptosis
Microtubule/Tubulin
|
Cancer
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EGFR/VEGFR2-IN-1 (Compound 10e) is a VEGFR-2 and EGFR inhibitor (IC50: 0.26 and 0.14 μM respectively). EGFR/VEGFR2-IN-1 inhibits tubulin polymerization with an IC50 of 40.9 μM. EGFR/VEGFR2-IN-1 induces apoptosis. EGFR/VEGFR2-IN-1 can be used for research of antileukemia and antilymphoma .
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- HY-168655
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Apoptosis
EGFR
VEGFR
|
Cancer
|
EGFR/VEGFR2-IN-3 (compound 9) is a potent EGFR and VEGFR-2 inhibitor with IC50 values of 0.129, 0.142, 3.428 µM for EGFR, VEGFR-2, COX-2, respectively. EGFR/VEGFR2-IN-3 shows cytotoxicity. EGFR/VEGFR2-IN-3 induces apoptosis and cell cycle arrest at G2/M phase .
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-
-
- HY-144304
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PROTACs
EGFR
|
Cancer
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PROTAC EGFR degrader 2 is a potent PROTAC EGFR degrader. PROTAC EGFR degrader 2 exhibits excellent antiproliferative activity with IC50 of 4.0 nM and good EGFR degradation activity with DC50 of 36.51 nM. PROTAC EGFR degrader 2 can be used for the synthesis of nitroreductase (NTR)-responsive PROTAC .
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- HY-170932
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|
EGFR
COX
Apoptosis
|
Cancer
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EGFR/COX-2-IN-1 is an EGFR/COX-2 inhibitor. EGFR/COX-2-IN-1 inhibits EGFR WT, EGFR T790M, COX-1 and COX-2 with IC50s of 0.12, 0.076, 20.1 and 1.52 μM respectively. EGFR/COX-2-IN-1 inhibits and with IC50s of , respectively. EGFR/COX-2-IN-1 inhibits MCF-7, HT-29 and A-549 with IC50s of 1.20, 5.14 and 14.81 μM, respectively. EGFR/COX-2-IN-1 displays Apoptosis induction by up-regulating Bax and down-regulating Bcl-2 protein levels. EGFR/COX-2-IN-1 results in a significant increase in the percentage of cells at the G2/M in MFC-7 cells. EGFR/COX-2-IN-1 exhibits broad-spectrum antitumor effects .
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-
- HY-157399
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EGFR
|
Cancer
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EGFR/HER2-IN-10 (compound 9F) is a potent and selective dual EGFR/HER2 inhibitor with IC50s of 2.3 nM and 234 nM for EGFR and HER2, respectively. EGFR/HER2-IN-10 shows an effective antiproliferative action against prostate carcinoma .
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- HY-174841
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EGFR
|
Cancer
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EGFR/HER2-IN-19 (Compound L1) is a dual inhibitor against epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2). EGFR/HER2-IN-19 is promising for research of cancers driven by EGFR/HER2 .
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- HY-151158
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EGFR
|
Cancer
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EGFR/HER2-IN-7 is a potent anticancer agent with high selectivity against MCF-7 breast cancer cells. EGFR/HER2-IN-7 is a EGFR/HER2 kinase and DHFR inhibitor, with IC50s of 0.18 μM (EGFR), 0.146 μM (HER2), respectively. EGFR/HER2-IN-7 shows moderate inhibition on DHFR (IC50=0.907 μM) .
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- HY-149633
-
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EGFR
Dihydrofolate reductase (DHFR)
Apoptosis
|
Cancer
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EGFR/HER2/DHFR-IN-3 (compound 4c) is a potent dual inhibitor of EGFR/HER2, with IC50s of 0.138 and 0.092 μM, respectively. EGFR/HER2/DHFR-IN-3 also inhibits DHFR, with an IC50 of 0.193 M. EGFR/HER2/DHFR-IN-3 causes arrest at the S phase of the cell cycle and induces apoptosis in MCF7 breast cancer cells .
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- HY-147798
-
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EGFR
CDK
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Cancer
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EGFR/HER2/CDK9-IN-3 (Compound 10) is a potent inhibitor of EGFR/HER2/CDK9 with IC50s of 191.08, 132.65, and 113.98 nM, respectively. EGFR/HER2/CDK9-IN-3 exhibits remarkable antitumor activity .
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- HY-147796
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EGFR
CDK
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Cancer
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EGFR/HER2/CDK9-IN-1 (Compound 4) is a potent inhibitor of EGFR/HER2/CDK9 with IC50s of 90.17, 131.39, and 67.04 nM, respectively. EGFR/HER2/CDK9-IN-1 exhibits remarkable antitumor activity .
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-
- HY-147797
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EGFR
CDK
|
Cancer
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EGFR/HER2/CDK9-IN-2 (Compound 9) is a potent inhibitor of EGFR/HER2/CDK9 with IC50s of 145.35, 129.07, and 117.13 nM, respectively. EGFR/HER2/CDK9-IN-2 exhibits remarkable antitumor activity .
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-
- HY-172623
-
|
EGFR
Caspase
Apoptosis
Bcl-2 Family
|
Cancer
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EGFR/HER2-IN-17 (Compound 7h) is a dual inhibitor of epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2). EGFR/HER2-IN-17 inhibits cancer cell proliferation. EGFR/HER2-IN-17 interacts with the binding pockets of EGFR and HER2, activating caspase-3 and caspase-8, and decreases the expression of Bcl-2, thereby inducing apoptosis. EGFR/HER2-IN-17 is promising for research of cancers .
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-
- HY-151154
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|
EGFR
|
Cancer
|
EGFR/HER2/DHFR-IN-1 is a potent anticancer agent with high selectivity against MCF-7 breast cancer cells. EGFR/HER2/DHFR-IN-1 is a multiple inhibitor of EGFR/HER2 kinase and DHFR, with IC50s of 0.153 μM, 0.108 μM, 0.291 μM, respectively. EGFR/HER2/DHFR-IN-1 arrests cell cycle at G1/S and induces cells apoptosis .
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-
-
- HY-155005
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EGFR
|
Cancer
|
EGFR mutant-IN-2 (Compound D51) is an EGFR mutant inhibitor. EGFR mutant-IN-2 inhibits the EGFR L858R/T790M/C797S mutant with an IC50 value of 14 nM. EGFR mutant-IN-2 inhibits the EGFR del19/T790M/C797S mutant with an IC50 value of 62 nM. EGFR mutant-IN-2 has favorable PK parameters, safety properties, in vivo stability, and antitumor activity .
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-
-
- HY-146239
-
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EGFR
Thymidylate Synthase
|
Cancer
|
EGFR/HER2/TS-IN-2 (compound 17) is a potent EGFR/HER2 and TS (Thymidylate synthase) inhibitor, with IC50 values of 0.173, 0.125, and 1.12 μM, respectively. EGFR/HER2/TS-IN-2 shows cytotoxic activity against MDA-MB-231 cancer cell lines, with an IC50 of 1.69 µM .
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-
- HY-147994
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EGFR
|
Cancer
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EGFR/HER2-IN-5 (compound 6h) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-5 inhibits EGFR with an IC50 value of 1.01 nM and demonstrates potent EGFR kinase inhibitory activities on L858R and T790M mutations. EGFR/HER2-IN-5 has potent antitumor efficacy in vivo and can be used for lung cancer research .
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-
- HY-147992
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EGFR
|
Cancer
|
EGFR/HER2-IN-4(compound 6d) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-4 inhibits EGFR with an IC50 value of 0.6 nM and demonstrates potent EGFR kinase inhibitory activities on L858R and T790M mutations. EGFR/HER2-IN-4 has potent antitumor efficacy in vivo and can be used for lung cancer research .
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- HY-149632
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EGFR
Dihydrofolate reductase (DHFR)
|
Cancer
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EGFR/HER2/DHFR-IN-2 (Compound 4b) is an inhibitor of EGFR, HER2, and DHFR (IC50: 0.248, 0.156, 0.138 μM respectively). EGFR/HER2/DHFR-IN-2 has anticancer activities against a panel of cancer cells (IC50: 9.14, 7.33, 14.18, 24.87, 20.07, 6.16 μM for Hep G2, HeLa, HEp-2, HCT 116, PC-3, MCF7 cells). EGFR/HER2/DHFR-IN-2 reduce breast cancer tumor growth .
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-
- HY-156115
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EGFR
CDK
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Cancer
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EGFR/CDK2-IN-3 (compound 4b) is a dual inhibitor of EGFR and CDK-2 with IC50s of 71.7 and 113.7 nM, respectively. EGFR/CDK2-IN-3 induces apoptosis in MCF-7 cells and arrests the cell cycle in the S phase. EGFR/CDK2-IN-3 has significant anti-cancer cell toxicity and inhibits MCF-7 with an IC50 of 3.16 μM .
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- HY-156114
-
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EGFR
CDK
|
Cancer
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EGFR/CDK2-IN-2 (compound 6a) is a dual inhibitor of EGFR and CDK-2 with IC50s of 19.6 and 87.9 nM, respectively. EGFR/CDK2-IN-2 induces apoptosis in MCF-7 cells and arrests the cell cycle in the S phase. EGFR/CDK2-IN-2 has significant anti-cancer cell toxicity and inhibits MCF-7 with an IC50 of 0.39 μM .
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- HY-156116
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EGFR
CDK
|
Cancer
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EGFR/CDK2-IN-4 (compound 4c) is a dual inhibitor of EGFR and CDK-2 with IC50s of 89.6 and 165.4 nM, respectively. EGFR/CDK2-IN-4 induces apoptosis in MCF-7 cells and arrests the cell cycle in the S phase. EGFR/CDK2-IN-4 has significant anti-cancer cell toxicity and inhibits MCF-7 with an IC50 of 2.74 μM .
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-
- HY-17632
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TH-4000
|
EGFR
|
Cancer
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Tarloxotinib bromide (TH-4000) is an irreversible EGFR/HER2 inhibitor.
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-
-
- HY-160682
-
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EGFR
|
Others
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EGFR/HER2-IN-12 (compound 14b) is a dual inhibitor of EGFR and HER2 with 81% and 51% inhibition at 10 μM. The toxicity of EGFR/HER2-IN-12 to cancer cells A431 and MDA-MB-361 was not significant .
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- HY-159519
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Apoptosis
EGFR
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Cancer
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EGFR/HER2-IN-16 (compound 12K) is an effective dual-target inhibitor of EGFR (IC50=6.15 nM) and HER-2 (IC50=9.78 nM) with anti-tumor activity. EGFR/HER2-IN-16 can inhibit the migration of SK-BR-3 cells, arrest the cell cycle in the G0/G1 phase, and induce apoptosis. EGFR/HER2-IN-16 exhibits good anti-proliferative activity against tumor cell models and has little damage to healthy cells. EGFR/HER2-IN-16 can be used in breast cancer research .
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- HY-150905
-
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EGFR
|
Cancer
|
EGFR ligand-2 (compound C4), a covalent EGFR ligand, is a EGFR mutant inhibitor with IC50s of 21 nM and 48 nM for EGFR L858R and EGFR L858R/T790M, respectively. EGFR ligand-2 can be used to synthesize PROTAC .
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-
- HY-172179
-
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EGFR
VEGFR
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Cancer
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EGFR/VEGFR2-IN-5 (Compound 14) is an orally active dual inhibitor of EGFR and VEGFR2 with an IC50 value of 1.15 µM for VEGFR2 and an IC50 value of 0.28 μM for EGFR T790M. EGFR/VEGFR2-IN-5 has significant anticancer activity .
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-
- HY-115952
-
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EGFR
|
Cancer
|
EGFR/HER2-IN-3 (Compound ZINC21942954) is a dual inhibitor of EGFR and HER2 .
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- HY-136789
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BDTX-189
|
EGFR
|
Cancer
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Tuxobertinib (BDTX-189) is a potent, orally active and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations, including EGFR/HER2 exon 20 insertion mutants. Tuxobertinib shows KDs of 0.2, 0.76, 13 and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively. Anticancer activity .
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- HY-156639
-
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EGFR
|
Cancer
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EGFR/ErbB-2 inhibitor-1 is a ErbB2/HER2 inhibitor .
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-
-
- HY-168170
-
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VEGFR
EGFR
|
Cancer
|
EGFR/VEGFR2-IN-2 (compound 4b) is an dual inhibitor VEGFR-2 and EGFR. .
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-
- HY-104065
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SHR-1258
|
EGFR
|
Cancer
|
Pyrotinib (SHR-1258) is a potent and selective EGFR/HER2 dual inhibitor with IC50s of 13 and 38 nM, respectively .
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-
-
- HY-13050A
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AZD-8931 fumarate
|
EGFR
|
Cancer
|
Sapitinib fumarate is a reversible, ATP competitive EGFR inhibitor of with IC50s of 4, 3 and 4 nM for EGFR, ErbB2 and ErbB3 in cells, respectively.
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-
-
- HY-160613
-
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EGFR
|
Cancer
|
EGFR/HER2-IN-11 (compound 20) is an orally active dual inhibitor for human epidermal growth factor receptor 2 (HER2) and epidermal growth factor receptor (EGFR), with IC50s of 7.7 and 22 nM, respectively. EGFR/HER2-IN-11 exhibits antitumor efficacy and inhibits proliferation against cancer cells BT-474 with GI50 of 601 nM .
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-
- HY-104065B
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SHR-1258 dimaleate
|
EGFR
|
Cancer
|
Pyrotinib dimaleate (SHR-1258 dimaleate) is a potent and selective EGFR/HER2 dual inhibitor with IC50s of 13 and 38 nM, respectively .
|
-
-
- HY-18609
-
|
EGFR
|
Cancer
|
PD158780 is a potent EGFR family inhibitor with IC50s of 8 pM, 49, 52, 52 nM for EGFR, ErbB2, ErbB3, and ErbB4, respectively.
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-
-
- HY-104065A
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(Rac)-SHR-1258
|
Drug Isomer
|
Cancer
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(Rac)-Pyrotinib ((Rac)-SHR-1258) is the racemic form of Pyrotinib (HY-104065). Pyrotinib is a potent and selective dual EGFR/HER2 receptor inhibitor.
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-
-
- HY-13050
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AZD-8931
|
EGFR
|
Cancer
|
Sapitinib (AZD-8931) is a reversible, ATP competitive EGFR inhibitor of with IC50s of 4, 3 and 4 nM for EGFR, ErbB2 and ErbB3 in cells, respectively.
|
-
-
- HY-15732
-
JNJ-26483327
|
EGFR
|
Cancer
|
BGB-102 is a potent multi-kinase inhibitor against EGFR, HER2, and HER4 with IC50s of 9.6 nM, 18 nM and 40.3 nM, respectively.
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- HY-10333
-
-
- HY-13272
-
Dacomitinib
Maximum Cited Publications
22 Publications Verification
PF-00299804; PF-299804
|
EGFR
Apoptosis
|
Cancer
|
Dacomitinib (PF-00299804) is a specific and irreversible inhibitor of the ERBB family of kinases with IC50s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively .
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-
- HY-10368
-
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EGFR
VEGFR
|
Cancer
|
EGFR/VEGFR2-IN-4 (Compound 19) is the irreversible inhibitor for EGFR and VEGFR-2 with IC50 of 18.7 nM and 102.3 nM, under the presence of 1 μM ATP .
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- HY-103440
-
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EGFR
|
Cancer
|
EGFR/ErbB-2/ErbB-4 inhibitor-3 (compound 29) is a potent tyrosine kinase inhibitor with IC50s of 0.3, 1.1, 0.5, 2.5, 24 nM for erbB1, erbB2, erbB4, EGF, HER, respectively . EGFR/ErbB-2/ErbB-4 inhibitor-3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-115951
-
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EGFR
|
Cancer
|
EGFR/HER2-IN-2 (Compound ZINC35560729) is a dual inhibitor of EGFR and HER2 with IC50 values of 5.02 µM and 0.83 µM against EGFR and HER2, respectively .
|
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- HY-112420
-
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EGFR
|
Cancer
|
EGFR/ErbB-2/ErbB-4 inhibitor-2 (Compound 5) is a EGFR and ErbB inhibitor with IC50s of 0.017 μM, 0.08 μM, 1.91 μM .
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- HY-15661A
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CP 373413
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Drug Metabolite
|
Cancer
|
OSI-413 (free base) (CP 373413) is a major metabolite of Erlotinib (HY-50896). Erlotinib (CP-358774) is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR .
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- HY-153111
-
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EGFR
|
Cancer
|
EGFR/HER2-IN-9 (Compound 1) is an EGFR and HER2 inhibitor with IC50s of 3.2, 8.3 and 14 nM against EGFR, EGFR T790M and HER2, respectively .
|
-
- HY-13272S3
-
PF-00299804-d10; PF-299804-d10
|
Isotope-Labeled Compounds
EGFR
Apoptosis
|
Cancer
|
Dacomitinib-d10 is deuterium labeled Dacomitinib. Dacomitinib (PF-00299804) is a specific and irreversible inhibitor of the ERBB family of kinases with IC50s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively .
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-
- HY-13272S2
-
PF-00299804-d10 dihydrochloride; PF-299804-d10 dihydrochloride
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Isotope-Labeled Compounds
EGFR
Apoptosis
|
Cancer
|
Dacomitinib-d10 dihydrochloride is the deuterium labeled Dacomitinib dihydrochloride. Dacomitinib (PF-00299804) dihydrochloride is a specific and irreversible inhibitor of the ERBB family of kinases with IC50s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively .
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- HY-164548
-
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HSP
Apoptosis
|
Cancer
|
WK88-1, a Hsp90 inhibitor, induces overall degradation of multiple oncogenic signaling molecules including EGFR, ErbB2 and ErbB3, leading to subsequent growth arrest and apoptosis in the Gefitinib-resistant H1975 cell line .
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- HY-163723
-
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EGFR
VEGFR
Topoisomerase
|
Cancer
|
EGFR-IN-116 (compound 14D) is an anticancer agent. EGFR-IN-116 against EGFR has the IC50 valuesof EGFR, VEGFR-2 and Topo II are 0.103 μM, 0.069 μM and 19.74 μM, respectively .
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-
- HY-104065BR
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SHR-1258 dimaleate (Standard)
|
Reference Standards
EGFR
|
Cancer
|
Pyrotinib dimaleate (Standard) is the analytical standard of Pyrotinib dimaleate. This product is intended for research and analytical applications. Pyrotinib dimaleate (SHR-1258 dimaleate) is a potent and selective EGFR/HER2 dual inhibitor with IC50s of 13 and 38 nM, respectively .
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-
- HY-174671
-
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mRNA
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Cardiovascular Disease
|
Human HBEGF mRNA encodes the human heparin binding EGF like growth factor (HBEGF) protein, a growth factor that mediates its effects via EGFR, ERBB2 and ERBB4. HBEGF may be involved in normal cardiac valve formation and normal heart function.
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- HY-135815
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TAK-788; AP32788
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EGFR
|
Cancer
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Mobocertinib (TAK-788) is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib can be used in NSCLC research [2].
|
-
- HY-135815B
-
TAK-788 mesylate; AP32788 mesylate
|
EGFR
|
Cancer
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Mobocertinib (TAK-788) mesylate is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib mesylate potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib mesylate can be used in NSCLC research [2].
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-
- HY-13272R
-
PF-00299804 (Standard); PF-299804 (Standard)
|
Reference Standards
EGFR
Apoptosis
|
Cancer
|
Dacomitinib (Standard) is the analytical standard of Dacomitinib. This product is intended for research and analytical applications. Dacomitinib (PF-00299804) is a specific and irreversible inhibitor of the ERBB family of kinases with IC50s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively .
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-
- HY-161141
-
|
c-Met/HGFR
|
Cancer
|
EGFR/ C-Met-in-2 (Compound H-22) is a dual inhibitor of EGFR/c-Met. EGFR/c-Met-IN-2 inhibits cell proliferation by arresting G2/M phase. EGFR/c-Met-IN-2 has antitumor activity .
|
-
- HY-135815A
-
TAK-788 succINate; AP32788 succINate
|
EGFR
|
Cancer
|
Mobocertinib (TAK-788) succinate is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib succinate potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib succinate can be used in NSCLC research [2].
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-
- HY-103439
-
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EGFR
|
Cancer
|
GW 583340 dihydrochloride is a potent dual EGFR/ErbB2 tyrosine kinase inhibitor (IC50: 0.01 and 0.014 μM respectively). GW 583340 dihydrochloride reverses ABCG2- and ABCB1-mediated drug resistance. GW 583340 dihydrochloride has anti-cancer activity [2] .
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-
- HY-135815R
-
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EGFR
|
Cancer
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Mobocertinib (Standard) is the analytical standard of Mobocertinib. This product is intended for research and analytical applications. Mobocertinib (TAK-788) is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib can be used in NSCLC research [2].
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- HY-147794
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CDK
COX
EGFR
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Cancer
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CDK9-IN-41 is a potent CDK9, EGFR, HER2, and COX-2 kinases inhibitor with IC50s of 192.81 nM, 254.03 nM, 238.81 nM, and 775 nM. COX-2-IN-18 exhibits remarkable antitumor activity against leukemia cancer cells, colon cancer cells, melanoma cells, ovarian cells and breast cells .
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- HY-P99275
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Human Anti-ERBB3 RecombINant Antibody
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EGFR
Akt
ERK
PARP
Survivin
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Cancer
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Patritumab (Human Anti-ERBB3 Recombinant Antibody) is a neutralizing monoclonal antibody to ERBB3. Patritumab shows a synergy with Cetuximab (HY-P9905), potently inhibits the phosphorylation of EGFR, HER2, HER3, ERK, and AKT. Patritumab also induces cell apoptosis and suppresses the growth of pancreatic, non-small cell lung cancer, and colorectal cancer xenograft tumors .
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- HY-10261B
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(E/Z)-BIBW 2992
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EGFR
Apoptosis
c-Met/HGFR
Akt
p38 MAPK
Autophagy
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Others
Cancer
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(E/Z)-Afatinib ((E/Z)-BIBW 2992) is the mixture of (E)-Afatinib and (Z)-Afatinib. Afatinib (HY-10261) is an irreversible inhibitor of EGFR, by irreversibly binding to their ATP binding site to block activation of EGFR, HER2, HER4, and EGFRvIII. Afatinib used in co-administration with Temozolomide (HY-17364), potently targeting to EGFRvIII-cMet signaling in glioblastoma cells .
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- HY-100499
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TyrphostIN B66; AG 528
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EGFR
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Cancer
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Tyrphostin AG 528 is an inhibitor of EGFR and ErbB2 with IC50s of 4.9 and 2.1 μM, respectively.
Tyrphostin AG 528 (Tyrphostin B66) is a protein tyrosine kinase inhibitor, with IC50s of 4.9 μM for epidermal growth factor receptors (EGFR) and 2.1 μM for ErbB2 . Tyrphostin AG 528 is also an anticancer agent [2].
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- HY-135815AR
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EGFR
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Cancer
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Mobocertinib (succinate) (Standard) is the analytical standard of Mobocertinib (succinate). This product is intended for research and analytical applications. Mobocertinib (TAK-788) succinate is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib succinate potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib succinate can be used in NSCLC research [2].
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- HY-164489
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EGFR
Akt
ERK
Apoptosis
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Cancer
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KU004 is a potent dual EGFR/HER2 inhibitor with anticancer effects. KU004 inhibits the proliferation of human breast cancer SKBR3 cells by inducing G1 phase arrest. KU004 blocks the activation of HER2, EGFR and downstream Akt and Erk pathways and induces cell Apoptosis mainly via the extrinsic pathway. KU004 is a quinazoline derivative [2].
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- HY-135366
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IKK
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Inflammation/Immunology
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HPN-01 is a potent and selective IKK inhibitor, with pIC50 values of 6.4, 7.0 and <4.8 for IKK-α, IKK-β and IKK-ε, respectively. HPN-01 displays greater 50-fold selectivity over a panel of more than 50 other kinases, including ALK5, CDK-2, EGFR, ErbB2, GSK3β, PLK1, Src, and VEGFR-2 .
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- HY-101042
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TyrphostIN AG 494
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EGFR
CDK
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Cancer
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AG-494 (Tyrphostin AG 494) is a potent and selective EGFR tyrosine kinase inhibitor (IC50=0.7 μM). AG-494 inhibits the autophosphorylation of EGFR, ErbB2, HER1-2 and PDGF-R with IC50s 1.1, 39, 45 and 6 μM, respectively. AG-494 blocks Cdk2 activation and inhibits EGF-dependent DNA synthesis [2] .
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- HY-119016
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SK1-I
1 Publications Verification
BML-258
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SphK
CaMK
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Cancer
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SK1-I (BML-258), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a Ki value of 10 μM . SK1-I shows no activity at SPHK1 PKCα, PKCδ, PKA, AKT1, ERK1, EGFR, CDK2, IKKβ or CamK2β. SK1-I enhances autophagy and has antitumor activity [2].
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- HY-21291
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PDGFR
EGFR
IGF-1R
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Cancer
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SU-4313 is a potent protein tyrosine kinases (PTKs) modulator with IC50s of 14.5 μM, 18.8 μM, 11 μM, 16.9 μM, 8.0 μM for PDGFR, FLK-1, EGFR, HER2 Kinase and IGF-1R, respectively. SU-4313 has the potential for modulating tyrosine kinase signal transduction in order to regulate abnormal cell proliferation .
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- HY-146228
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HSP
Apoptosis
Topoisomerase
EGFR
VEGFR
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Cancer
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HSP90-IN-13 (compound 5k) is a highly potent HSP90 pan inhibitor with an IC50 value of 25.07 nM. HSP90-IN-13 has multi-target activity against EGFR, VEGFR-2 and Topoisomerase-2. HSP90-IN-13 causes cell cycle arrest at G2/M phase and induces apoptosis of MCF-7 cells through mitochondrial-mediated pathway .
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- HY-10261BR
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(E/Z)-BIBW 2992 (Standard)
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EGFR
Apoptosis
c-Met/HGFR
Akt
p38 MAPK
Autophagy
Reference Standards
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Others
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(E/Z)-Afatinib (Standard) is the analytical standard of (E/Z)-Afatinib. This product is intended for research and analytical applications. (E/Z)-Afatinib ((E/Z)-BIBW 2992) is the mixture of (E)-Afatinib and (Z)-Afatinib. Afatinib (HY-10261) is an irreversible inhibitor of EGFR, by irreversibly binding to their ATP binding site to block activation of EGFR, HER2, HER4, and EGFRvIII. Afatinib used in co-administration with Temozolomide (HY-17364), potently targeting to EGFRvIII-cMet signaling in glioblastoma cells .
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- HY-132842
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DZD9008
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EGFR
Btk
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Cancer
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Sunvozertinib (DZD9008) is a potent ErbBs (EGFR, Her2, especially mutant forms) and BTK inhibitor. Sunvozertinib shows IC50s of 20.4, 20.4, 1.1, 7.5, and 80.4 nM for EGFR exon 20 NPH insertion, EGFR exon 20 ASV insertion, EGFR L858R and T790M mutations, and Her2 Exon20 YVMA, and EGFR WT A431, respectively (patent WO2019149164A1, example 52) .
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- HY-100349
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PDGFR
VEGFR
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Cancer
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SU4312 is the racemate of (Z)-SU4312 and (E)-SU4312. (Z)-SU4312 inhibits PDGFR and FLK-1 with IC50s of 19.4 and 0.8 μM, respectively. (E)-SU4312 inhibits PDGFR, FLK-1, EGFR, HER-2, and IGF-1R with IC50s of 24.2, 5.2, 18.5, 16.9 and 10.0 μM, respectively .
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- HY-100349A
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(Z)-SU4312
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PDGFR
VEGFR
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Cancer
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cis-SU4312 ((Z)-SU4312) inhibits PDGFR and FLK-1 with IC50s of 19.4 and 0.8 μM, respectively. cis-SU4312 inhibits PDGFR, FLK-1, EGFR, HER-2, and IGF-1R with IC50s of 24.2, 5.2, 18.5, 16.9 and 10.0 μM, respectively. cis-SU4312 can cross blood brain barrier .
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- HY-169216
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EGFR
VEGFR
CDK
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Cancer
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Multi-target kinase inhibitor 3 (compund 6i) is a multi-kinase target inhibitor with anticancer activity. Multi-target kinase inhibitor 3 inhibits EGFR, HER2, VEGFR-2, and CDK2 with IC50s of 0.063 μM, 0.054 μM, 0.119 μM, and 0.448 μM, respectively. Multi-target kinase inhibitor 3 has a good inhibitory effect on breast cancer cells MCF-7, with an IC50 of 6.10 μM .
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- HY-149636
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EGFR
CDK
VEGFR
Apoptosis
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Cancer
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Multi-target kinase inhibitor 2 is a multi-targeted kinase inhibitor, and exhibits activity against EGFR, Her2, VEGFR2, and CDK2 enzymes, with IC50 values of 79 nM, 40 nM,136 nM, and 204 nM, respectively. Multi-target kinase inhibitor 2 shows cytotoxic effects were observed against HepG2, HeLa , MDA-MB-231 and MCF-7, with IC50 of 41, 57, 51 and 59 μM. Multi-target kinase inhibitor 2 induces cell cycle arrest and apoptosis in HepG2 cells .
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- HY-148118A
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LYTACs
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Cancer
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Tri-GalNAc(OAc)3 TFA is a trivalent N-acetylgalactosamine (GalNAc) derivative that can be used to synthesize GalNAc-LYTAC. Tri-GalNAc is a specific ligand targeting the asialoglycoprotein receptor (ASGPR), mediating the endocytosis and transport of cell surface proteins (such as EGFR, HER2) to lysosomes for degradation by lysosomal targeting chimeras (LYTACs). Tri-GalNAc significantly reduces the level of target proteins and inhibits downstream signaling pathways (such as EGFR-mediated Akt and MAPK signals). Tri-GalNAc(OAc)3 TFA can be used for hepatocyte targeting studies, and can degrade carcinogenic membrane proteins and inhibit tumor cell proliferation in liver cancer cell models .
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- HY-148118
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LYTACs
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Cancer
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Tri-GalNAc(OAc)3is a trivalent N-acetylgalactosamine (GalNAc) derivative that can be used to synthesize GalNAc-LYTAC. Tri-GalNAc is a specific ligand targeting the asialoglycoprotein receptor (ASGPR), mediating the endocytosis and transport of cell surface proteins (such as EGFR, HER2) to lysosomes for degradation by lysosomal targeting chimeras (LYTACs). Tri-GalNAc significantly reduces the level of target proteins and inhibits downstream signaling pathways (such as EGFR-mediated Akt and MAPK signals). Tri-GalNAc(OAc)3can be used for hepatocyte targeting studies, and can degrade carcinogenic membrane proteins and inhibit tumor cell proliferation in liver cancer cell models .
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- HY-175011
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EGFR
Apoptosis
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Cancer
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EGFR-IN-165 is a potent EGFR inhibitor. EGFR-IN-165 demonstrates superior potency with IC50s of 17.18 and 64.74 nM against EGFR L858R/T790M and EGFR WT; 2.17 and 6.2 μM against NCI-H1975 cells and A431 cells. EGFR-IN-165 significantly inhibits the migration and induces G1 phase cell cycle arrest and cell apoptosis. EGFR-IN-165 can be used for the study of cancers such as non-small cell lung cancer, colorectal cancer, and head and neck squamous cell carcinoma .
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- HY-149407
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VEGFR
CDK
EGFR
Necroptosis
Apoptosis
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Cancer
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Multi-kinase-IN-4 (compound 5d) is multi-targeted kinase inhibitor, including VEGFR2, EGFR, HER2, and CDK2, with IC50 values of 0.33, 0.22, 0.18 and 2.09 μM, respectively. Multi-kinase-IN-4 shows broad-spectrum anti-cancer activities against HepG2, MCF-7, MDA-231, and HeLa cell lines (IC50 = 1.94–7.1 µM), but exhibits lower toxicity in the WI-38 cells (IC50 = 40.85 µM). Multi-kinase-IN-4 induces apoptosis and arrests cell cycle at S phase in HepG2 cells. Multi-kinase-IN-4 has the potential for the research of cancer .
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P99275
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Human Anti-ERBB3 RecombINant Antibody
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EGFR
Akt
ERK
PARP
Survivin
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Cancer
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Patritumab (Human Anti-ERBB3 Recombinant Antibody) is a neutralizing monoclonal antibody to ERBB3. Patritumab shows a synergy with Cetuximab (HY-P9905), potently inhibits the phosphorylation of EGFR, HER2, HER3, ERK, and AKT. Patritumab also induces cell apoptosis and suppresses the growth of pancreatic, non-small cell lung cancer, and colorectal cancer xenograft tumors .
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Cat. No. |
Product Name |
Chemical Structure |
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- HY-13272S3
-
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Dacomitinib-d10 is deuterium labeled Dacomitinib. Dacomitinib (PF-00299804) is a specific and irreversible inhibitor of the ERBB family of kinases with IC50s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively .
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-
-
- HY-13272S2
-
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Dacomitinib-d10 dihydrochloride is the deuterium labeled Dacomitinib dihydrochloride. Dacomitinib (PF-00299804) dihydrochloride is a specific and irreversible inhibitor of the ERBB family of kinases with IC50s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively .
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Cat. No. |
Product Name |
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Classification |
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- HY-159519
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Azide
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EGFR/HER2-IN-16 (compound 12K) is an effective dual-target inhibitor of EGFR (IC50=6.15 nM) and HER-2 (IC50=9.78 nM) with anti-tumor activity. EGFR/HER2-IN-16 can inhibit the migration of SK-BR-3 cells, arrest the cell cycle in the G0/G1 phase, and induce apoptosis. EGFR/HER2-IN-16 exhibits good anti-proliferative activity against tumor cell models and has little damage to healthy cells. EGFR/HER2-IN-16 can be used in breast cancer research .
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- HY-15661A
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CP 373413
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|
Alkynes
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OSI-413 (free base) (CP 373413) is a major metabolite of Erlotinib (HY-50896). Erlotinib (CP-358774) is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR .
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Cat. No. |
Product Name |
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Classification |
-
- HY-174671
-
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mRNA
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Human HBEGF mRNA encodes the human heparin binding EGF like growth factor (HBEGF) protein, a growth factor that mediates its effects via EGFR, ERBB2 and ERBB4. HBEGF may be involved in normal cardiac valve formation and normal heart function.
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