Search Result
Results for "
ERBB inhibitor
" in MedChemExpress (MCE) Product Catalog:
9
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-103440
-
|
|
EGFR
|
Cancer
|
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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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-
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- HY-112420
-
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EGFR
|
Cancer
|
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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-50898
-
Lapatinib
Maximum Cited Publications
77 Publications Verification
GW572016; GW2016
|
EGFR
Autophagy
Ferroptosis
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Cancer
|
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Lapatinib (GW572016) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
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-
-
- HY-50898B
-
|
GW572016 ditosylate monohydrate; GW2016 ditosylate monohydrate
|
EGFR
Autophagy
Ferroptosis
|
Cancer
|
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Lapatinib ditosylate monohydrate (GW572016 ditosylate monohydrate) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
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-
-
- HY-156639
-
|
|
EGFR
|
Cancer
|
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EGFR/ErbB-2 inhibitor-1 is a ErbB2/HER2 inhibitor .
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-
-
- HY-110039
-
|
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EGFR
|
Infection
|
|
BIBX 1382 dihydrochloride is an ErbB kinase inhibitor with significant antiviral activity. BIBX 1382 affects the ability of viruses to enter host cells by inhibiting members of the ErbB kinase family. It can be used to study the interaction mechanism between virus and host and the broad spectrum intervention of highly pathogenic viruses .
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-
-
- HY-153856
-
|
|
EGFR
|
Cancer
|
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TAS2940 is a brain-penetrable, orally active, irreversible and selective pan-ERBB inhibitor. TAS2940 against wild-type HER2, HER2 V777L, and A775_G776insYVMA with IC50 values of 5.6 nM, 2.1 nM, and 1.0 nM, respectively. TAS2940 can be used for the study of tumors with HER2 and EGFR aberrations .
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-
-
- HY-153856A
-
|
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EGFR
|
Cancer
|
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TAS2940 fumarate is a brain-penetrable, orally active, irreversible and selective pan-ERBB inhibitor. TAS2940 fumarate against wild-type HER2, HER2 V777L, and A775_G776insYVMA with IC50 values of 5.6 nM, 2.1 nM, and 1.0 nM, respectively. TAS2940 fumarate can be used for the study of tumors with HER2 and EGFR aberrations .
|
-
-
- HY-137028
-
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PD157432
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EGFR
|
Cancer
|
|
2'-Thioadenosine (PD157432) is a selective and irreversible inhibitor of ErbB-1 and ErbB-2, with an IC50 of 45 µM for ErbB-2. 2'-Thioadenosine covalently inactivates ErbB-1 via modification of a cysteine residue at the active site .
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-
-
- HY-P991240
-
|
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EGFR
|
Cancer
|
|
CDX-3379 is a humanized monoclonal antibody inhibitor targeting ErbB3. CDX-3379 binds to ErbB3, blocking the dimerization of ErbB3 with other receptors, thereby inhibiting the phosphorylation of ErbB3. CDX-3379 can inhibit the growth and proliferation of tumor cells. CDX-3379 is promising for research of tumors expressing ErbB3 and NRG1, such as HNSCC .
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-
-
- HY-50898C
-
|
GW572016 tosylate; GW2016 tosylate
|
EGFR
Ferroptosis
Autophagy
|
Cancer
|
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Lapatinib (GW572016) tosylate is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
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-
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- HY-50898A
-
|
GW572016 ditosylate; GW2016 ditosylate
|
EGFR
Autophagy
Ferroptosis
|
Cancer
|
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Lapatinib ditosylate (GW572016 ditosylate) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
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- HY-103441
-
|
|
EGFR
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Cancer
|
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JNJ28871063 hydrochloride is an orally active, highly selective and ATP competitive pan-ErbB kinase inhibitor with IC50 values of 22 nM, 38 nM, and 21 nM for ErbB1, ErbB2, and ErbB4, respectively. JNJ28871063 hydrochloride inhibits phosphorylation of functionally important tyrosine residues in both EGFR and ErbB2. JNJ28871063 hydrochloride crosses the blood-brain barrier and has antitumor activity in human tumor xenograft models that overexpress EGFR and ErbB2 .
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-
-
- HY-P991243
-
|
|
EGFR
PI3K
Akt
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Cancer
|
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MP-RM-1 is a selective murine monoclonal antibody inhibitor targeting human epidermal growth factor receptor 3 (ErbB-3). MP-RM-1 blocks the activation of ErbB-3 induced by neuregulin 1 (NRG-1β) and promotes the internalization and degradation of ErbB-3, inhibiting downstream signaling pathways such as PI3K-Akt. MP-RM-1 is promising for research of ErbB-3 highly expressed solid tumors such as breast cancer, melanoma, and prostate cancer .
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-
-
- HY-18609
-
|
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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-P991241
-
|
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EGFR
|
Cancer
|
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Anti-ERBB3/HER3 (29Z6) is an antibody inhibitor, targeting to human ERBB3/HER3.
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-
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- HY-50898S2
-
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GW572016-d5; GW2016-d5
|
Isotope-Labeled Compounds
EGFR
Autophagy
Ferroptosis
|
Cancer
|
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Lapatinib-d5 is deuterium labeled Lapatinib. Lapatinib (GW572016) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
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-
-
- HY-50898S1
-
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GW572016-dd7 dihydrochloride; GW2016-dd7 dihydrochloride
|
Isotope-Labeled Compounds
EGFR
Autophagy
Ferroptosis
|
Cancer
|
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Lapatinib-d7 dihydrochloride is the deuterium labeled Lapatinib dihydrochloride. Lapatinib (GW572016) dihydrochloride is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
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-
-
- HY-50898S3
-
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GW572016-d4-1; GW2016-d4-1
|
Isotope-Labeled Compounds
EGFR
Autophagy
Ferroptosis
|
Cancer
|
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Lapatinib-d4-1 is deuterium labeled Lapatinib. Lapatinib (GW572016) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
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-
-
- HY-13272
-
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PF-00299804; PF-299804
|
EGFR
Apoptosis
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Cancer
|
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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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-
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- HY-50898S
-
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GW572016-d4; GW2016-d4
|
EGFR
Autophagy
Ferroptosis
|
Cancer
|
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Lapatinib-d4 is the deuterium labeled Lapatinib (HY-50898). Lapatinib is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
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-
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- HY-50898R
-
|
|
EGFR
Autophagy
Ferroptosis
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Cancer
|
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Lapatinib (Standard) is the analytical standard of Lapatinib. This product is intended for research and analytical applications. Lapatinib (GW572016) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
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-
-
- HY-W006886
-
|
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Amino Acid Derivatives
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Others
|
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Fmoc-(R)-2-(7-octenyl)Ala-OH is an amino acid derivative with an Fmoc protecting group that can be used to synthesize inhibitor peptides that combinatorially inactivate ErbB1, ErbB2, and ErbB3 .
|
-
-
- HY-50898S4
-
|
GW572016-d7; GW2016-d7
|
Isotope-Labeled Compounds
Autophagy
EGFR
Ferroptosis
|
Cancer
|
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Lapatinib-d7 (GW572016-d7) is deuterium labeled Lapatinib. Lapatinib (GW572016) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
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-
-
- HY-50898CS
-
|
GW572016-d4 tosylate; GW2016-d4 tosylate
|
Isotope-Labeled Compounds
EGFR
Autophagy
Ferroptosis
|
Cancer
|
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Lapatinib-d4 (GW572016-d4) tosylate is deuterium labeled Lapatinib (tosylate). Lapatinib (GW572016) tosylate is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
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-
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- HY-13050A
-
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AZD-8931 fumarate
|
EGFR
|
Cancer
|
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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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-
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- 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
-
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PF-00299804-d10 dihydrochloride; PF-299804-d10 dihydrochloride
|
Isotope-Labeled Compounds
EGFR
Apoptosis
|
Cancer
|
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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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-
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- HY-P991245
-
|
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EGFR
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Cancer
|
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Anti-ERBB3/HER3 (SGP1) is a human monoclonal antibody (mAb) targeting ERBB3/HER3. Anti-ERBB3/HER3 (SGP1) inhibits Neuregulin stimulated growth of cultured breast cancer cells. Anti-ERBB3/HER3 (SGP1) can be used in breast cancer research .
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- HY-14347
-
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EGFR
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Cancer
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EBE-A22 is a derivative of PD153035, which can inhibit the phosphorylation of ErbB-1, but EBE-A22 does not have this activity.
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-
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- HY-168438
-
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EGFR
Akt
ERK
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Cardiovascular Disease
|
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ERBB agonist-1 (Compound EF-1) is an agonist for ERBB4, that activates the ERBB4 signaling pathway by inducing dimerization of the ERBB4 receptor with an EC50 of 10.5 μM. ERBB agonist-1 induces phosphorylation of Akt and ERK1/2, reduces the collagen expression in cardiac fibroblasts, inhibits H2O2-induced cardiomyocyte death and Ang II (HY-13948)-induced cardiomyocyte hypertrophy. ERBB agonist-1 prevents fibrosis and exhibits cardioprotective efficacy in mouse models .
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- HY-13272R
-
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EGFR
Apoptosis
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Cancer
|
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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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-
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- HY-13050
-
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AZD-8931
|
EGFR
|
Cancer
|
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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.
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-
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- HY-129288
-
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NEU-391
|
EGFR
Paraptosis
Mitosis
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Infection
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GW837016X (NEU-391) is an orally active ErbB-2 kinase covalent inhibitor. GW837016X also is a potent antitrypanosome agent. GW837016X inhibits mitosis and cytokinesis .
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-
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- HY-118532
-
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AG30
|
EGFR
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Cancer
|
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Tyrphostin AG30 (AG30) is a potent and selective EGFR tyrosine kinase inhibitor. Tyrphostin AG30 (AG30) selectively inhibits self renewal induction by c-ErbB, and is able to inhibit activation of STAT5 by c-ErbB in primary erythroblasts .
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-
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- HY-160068
-
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EGFR
|
Cancer
|
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2-2(t) aptamer sodium is a 42-nucleotide trimeric complex of aptamer (2-2) targeting ErbB-2. 2-2(t) aptamer sodium inhibits the growth of gastric cancer cells in vitro and in vivo .
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-
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- HY-15375
-
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AST-1306; ALS 1306
|
EGFR
|
Cancer
|
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Allitinib (AST-1306) is an orally active and irreversible EGFR and ErbB2 inhibitor with IC50s of 0.5 and 3 nM, respectively. Allitinib also inhibits ErbB4 with an IC50 of 0.8 nM. Allitinib is an anilino-quinazoline compound and has anti-cancer activity .
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-
-
- HY-10045
-
AEE788
3 Publications Verification
NVP-AEE 788
|
EGFR
Apoptosis
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Cancer
|
|
AEE788 is an inhibitor of the EGFR and ErbB2 with IC50 values of 2 and 6 nM, respectively.
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-
-
- HY-13427
-
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AST-1306 (TsOH)
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EGFR
|
Cancer
|
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Allitinib tosylate (AST-1306 (TsOH)) is an orally active and irreversible EGFR and ErbB2 inhibitor with IC50s of 0.5 and 3 nM, respectively. Allitinib tosylate also inhibits ErbB4 with an IC50 of 0.8 nM. Allitinib tosylate is an anilino-quinazoline compound and has anti-cancer activity
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-
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- HY-164548
-
|
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HSP
Apoptosis
|
Cancer
|
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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-14674
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
CP-724714 is a potent, selective and orally active ErbB2 (HER2) tyrosine kinase inhibitor, with an IC50 of 10 nM. CP-724714 displays a marked selectivity against EGFR kinase (IC50=6400 nM). CP-724714 potently inhibits ErbB2 receptor autophosphorylation in intact cells. Antitumor activities .
|
-
-
- HY-20878
-
|
AG 879
|
Trk Receptor
EGFR
Apoptosis
|
Cancer
|
|
Tyrphostin AG 879 (AG 879) is a tyrosine kinase inhibitor that inhibits TrKA phosphorylation (IC50 of 10 μM), but not TrKB and TrKC. Tyrphostin AG 879 is also a selective ErbB2 tyrosine kinase inhibitor with an IC50 of 1 μM, and has at least 500-fold higher selectivity to ErbB2 than EGFR. Tyrphostin AG 879 has anticancer activity .
|
-
-
- HY-P991244
-
|
|
EGFR
|
Cancer
|
|
REGN-1400 is a humanized monoclonal antibody inhibitor targeting ErbB3. REGN-1400 reduces tumor cell proliferation by inhibiting ErbB3 and blocking related signaling pathways. REGN-1400 is promising for research of solid tumors such as non-small cell lung cancer (NSCLC), colorectal cancer (CRC), and squamous cell carcinoma of the head and neck (SCCHN) .
|
-
-
- HY-100499
-
|
Tyrphostin B66; AG 528
|
EGFR
|
Cancer
|
|
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 .
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-
-
- HY-143874
-
|
|
EGFR
|
Cancer
|
|
HER2-IN-7 is a potent inhibitor of HER2. Deregulation of ErbB family signalling modulates proliferation, invasion, metastasis, angiogenesis, and tumour cell survival. HER2-IN-7 has the potential for the research of diseases associated ErbBs (especially HER2), including cancer (extracted from patent WO2019214634A1, compound 23) .
|
-
-
- HY-P99275
-
|
Human Anti-ERBB3 Recombinant Antibody
|
EGFR
Akt
ERK
PARP
Survivin
|
Cancer
|
|
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-116437
-
|
|
EGFR
|
Cancer
|
|
Selatinib is a reversible and orally active dual EGFR and ErbB2 inhibitor with IC50s of 13 nM and 22.5 nM, respectively. Selatinib has anticancer effects .
|
-
-
- HY-118263
-
|
PF-00299804 hydrate; PF-299804 hydrate
|
EGFR
|
Cancer
|
|
Dacomitinib (PF-00299804) hydrate is an orally active, irreversible pan-ErbB inhibitor. Dacomitinib hydrate can be used in the research of cancers such as metastatic non-small cell lung cancer (NSCLC) .
|
-
-
- HY-32718
-
|
EKB-569; WAY-EKB 569
|
EGFR
Src
|
Cancer
|
|
Pelitinib (EKB-569;WAY-EKB 569) is an irreversible inhibitor of EGFR with an IC50 of 38.5 nM; also slightly inhibits Src, MEK/ERK and ErbB2 with IC50s of 282, 800, and 1255 nM, respectively.
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-
-
- HY-10531
-
|
|
EGFR
|
Cancer
|
|
ARRY-380 analog, an inhibitor of EGFR (ErbB1), is extracted from patent WO2015153959A2, compound 249 . ARRY-380 is a potent, selective, ATP-competitive, orally active inhibitor of HER2 .
|
-
- HY-103443
-
|
|
EGFR
|
Cancer
|
|
HKI-357 is an irreversible dual inhibitor of EGFR and ERBB2 with IC50s of 34 nM and 33 nM, respectively. HKI-357 suppresses EGFR autophosphorylation (at Y1068), and AKT and MAPK phosphorylation .
|
-
- HY-10367A
-
|
CI-1033 dihydrochloride; PD-183805 dihydrochloride
|
EGFR
Orthopoxvirus
|
Infection
Cancer
|
|
Canertinib dihydrochloride (CI-1033 dihydrochloride) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC50s of 7.4 and 9 nM. Canertinib dihydrochloride is active against vaccinia virus respiratory infection in mice .
|
-
- HY-W008914
-
|
|
EGFR
|
Cancer
|
|
(E/Z)-CP-724714 is a racemic compound of (E)-CP-724714 and (Z)-CP-724714 isomers. CP-724714 is a potent and selective orally active ErbB2 (HER2) inhibitor .
|
-
- HY-103443A
-
|
|
EGFR
|
Cancer
|
|
HKI-357 dimaleate is an irreversible dual inhibitor of EGFR and ERBB2 with IC50s of 34 nM and 33 nM, respectively. HKI-357 dimaleate suppresses EGFR autophosphorylation (at Y1068), and AKT and MAPK phosphorylation .
|
-
- HY-13896
-
|
|
EGFR
Autophagy
Apoptosis
|
Cancer
|
|
PD168393 is a potent, selective and cell-permeable inhibitor of EGFR tyrosine kinase and ErbB2. PD168393 irreversiblely inactivates EGF receptor ( IC50=0.7 nM) and is inactive against insulin receptor, PDGFR, FGFR and PKC .
|
-
- HY-10367
-
|
CI-1033; PD-183805
|
EGFR
Orthopoxvirus
|
Infection
Cancer
|
|
Canertinib (CI-1033;PD-183805) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC50s of 7.4 and 9 nM. Canertinib is active against vaccinia virus respiratory infection in mice .
|
-
- HY-10367AR
-
|
CI-1033 dihydrochloride (Standard); PD-183805 dihydrochloride (Standard)
|
Reference Standards
EGFR
Orthopoxvirus
|
Infection
Cancer
|
|
Canertinib (dihydrochloride) (Standard) is the analytical standard of Canertinib (dihydrochloride). This product is intended for research and analytical applications. Canertinib dihydrochloride (CI-1033 dihydrochloride) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC50s of 7.4 and 9 nM. Canertinib dihydrochloride is active against vaccinia virus respiratory infection in mice .
|
-
- HY-103439
-
|
|
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 .
|
-
- HY-10367R
-
|
CI-1033 (Standard); PD-183805 (Standard)
|
Reference Standards
EGFR
Orthopoxvirus
|
Infection
Cancer
|
|
Canertinib (Standard) is the analytical standard of Canertinib. This product is intended for research and analytical applications. Canertinib (CI-1033;PD-183805) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC50s of 7.4 and 9 nM. Canertinib is active against vaccinia virus respiratory infection in mice .
|
-
- HY-P99268
-
|
SAR 256212; MM 121; Anti-Human ERBB3/ERBB 3 Recombinant Antibody
|
EGFR
Apoptosis
|
Cancer
|
|
Seribantumab (MM 121) is a fully human IgG2 monoclonal antibody that targets HER3. Seribantumab blocks the activation of epidermal growth factor receptor (ErbB) family members and its downstream signal. Seribantumab inhibits neuregulin 1 (NRG1) fusion-dependent tumorigenesis in vitro and in vivo in breast, lung and ovarian patient-derived cancer models .
|
-
- HY-10346
-
AV-412
4 Publications Verification
MP412
|
EGFR
|
Cancer
|
|
AV-412 (MP412) is an EGFR inhibitor with IC50s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFR L858R, EGFR T790M, EGFR L858R/T790M and ErbB2, respectively.
|
-
- HY-B0793
-
AZ-5104
3 Publications Verification
|
EGFR
|
Cancer
|
|
AZ-5104 is an active, demethylated metabolite of AZD 9291. AZ-5104 is an EGFR inhibitor with IC50s of 1, 6, 1, 25 and 7 nM for EGFR L858R/T790M, EGFR L858R, EGFR L861Q, EGFR and ErbB4, respectively.
|
-
- HY-101042
-
|
Tyrphostin AG 494
|
EGFR
CDK
|
Cancer
|
|
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 .
|
-
- HY-B0793S1
-
|
|
EGFR
|
Cancer
|
|
AZ-5104-d2 is the deuterium labeled AZ-5104. AZ-5104 is an EGFR inhibitor with IC50s of 1 nM, 6 nM, 1 nM, 25 nM and 7 nM for EGFRL858R/T790M, EGFRL858R, EGFRL861Q, EGFR and ErbB4, respectively .
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-
- HY-10346A
-
|
MP-412 free base
|
EGFR
|
Cancer
|
|
AV-412 free base (MP-412 free base) is an EGFR inhibitor with IC50s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFR L858R, EGFR T790M, EGFR L858R/T790M and ErbB2, respectively.
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-
- HY-10322
-
|
BIBX 1382
|
EGFR
|
Cancer
|
|
Falnidamol (BIBX 1382) is an orally active, selective EGFR tyrosine kinase inhibitor with an IC50 of 3 nM. Falnidamol displays > 1000-fold lower potency against ErbB2 (IC50=3.4 μM) and a range of other related tyrosine kinases (IC50>10 μM). Falnidamol is a pyrimido-pyrimidine compound and has anti-cancer activity .
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-
- HY-168577
-
|
|
Ras
EGFR
|
Cancer
|
|
KRAS G12D inhibitor 25 (Compound 148) is an inhibitor for KRAS G12C and HSP90α with IC50 of < 0.1 μM and 0.1-1 μM, respectively. KRAS G12D inhibitor 25 inhibits the proliferation of MIA PaCa-2 and NCI-H358 with EC50 of < 0.1 μM and 0.1-1 μM, respectively. KRAS G12D inhibitor 25 degrades ERBB2 with a DC50 of 0.1-1 μM .
|
-
- HY-150023
-
|
|
EGFR
Itk
PI4K
Btk
CDK
Raf
JAK
|
Cancer
|
|
BI-1622 is an orally active, potent and highly selective HER2 (ERBB2) inhibitor, with an IC50 of 7 nM. BI-1622 shows greater than 25-fold selectivity over EGFR. BI-1622 shows high antitumor efficacy in vivo in xenograft mouse tumor models with engineered H2170 and PC9 cells and had a favorable agent metabolism and pharmacokinetics profile .
|
-
- HY-100848
-
|
|
EGFR
|
Cancer
|
|
TX1-85-1 is an irreversible Her3 (ErbB3) inhibitor with an IC50 of 23 nM. TX1-85-1 is also the first selective Her3 ligand, which forms a covalent bond with Cys721 located in the ATP-binding site of Her3. TX1-85-1 induces partial degradation of Her3 protein and attenuates Her3-dependent signaling .
|
-
- HY-15844
-
-
- HY-135366
-
|
|
IKK
|
Inflammation/Immunology
|
|
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-10322R
-
|
BIBX 1382 (Standard)
|
Reference Standards
EGFR
|
Cancer
|
|
Falnidamol (Standard) is the analytical standard of Falnidamol. This product is intended for research and analytical applications. Falnidamol (BIBX 1382) is an orally active, selective EGFR tyrosine kinase inhibitor with an IC50 of 3 nM. Falnidamol displays > 1000-fold lower potency against ErbB2 (IC50=3.4 μM) and a range of other related tyrosine kinases (IC50>10 μM). Falnidamol is a pyrimido-pyrimidine compound and has anti-cancer activity .
|
-
- HY-132842
-
|
DZD9008
|
EGFR
Btk
|
Cancer
|
|
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) .
|
-
- HY-118998
-
|
|
PROTACs
EGFR
ERK
Akt
|
Cancer
|
|
TX2-121-1 is a potent and selective Her3 (ErbB3) degrader that contains a hydrophobic adamantane moiety. TX2-121-1 has an IC50 of 49 nM for Her3. TX2-121-1 inhibits Her3-dependent signaling and heterodimerization of Her3. TX2-121-1 has the ability to inhibit cell proliferation. TX2-121-1 can be used in the study of tumors. (Pink: Her3 inhibitor (HY-164988); Black: Linker; Blue: Adamantane (HY-N2427)) .
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-
- HY-10261A
-
|
BIBW 2992MA2
|
EGFR
Autophagy
Apoptosis
c-Met/HGFR
Akt
p38 MAPK
|
Cancer
|
|
Afatinib (BIBW 2992) dimaleate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively. Afatinib dimaleate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
|
-
- HY-10261
-
|
BIBW 2992
|
EGFR
Autophagy
Apoptosis
c-Met/HGFR
Akt
p38 MAPK
|
Cancer
|
|
Afatinib (BIBW 2992) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
|
-
- HY-10261D
-
|
BIBW 2992 oxalate
|
EGFR
Autophagy
Apoptosis
c-Met/HGFR
Akt
|
Cancer
|
|
Afatinib (BIBW 2992) oxalate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively. Afatinib oxalate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
|
-
- HY-123035
-
|
|
HSP
Akt
EGFR
|
Endocrinology
|
|
Gamendazole, an indazole carboxylic acid (ICA), is an orally active, selective HSP90AB1 (HSP90BETA) and EEF1A1 (eEF1A) inhibitor. Gamendazole binds to the C-terminal nucleotide binding pocket of HSP90 and cause downregulation of clients AKT1 and ERBB2, but stabilizes the HSP90 heterocomplex. Gamendazole specifically inhibits the actin bundling function of EEF1A1, but does not bind to the nucleotide docking pocket nor inhibits the ribosome charging or protein translation functions of EEF1A1. Gamendazole, an antispermatogenic compound with antifertility effects, has the potential for reversible non-hormonal male contraceptive agent research .
|
-
- HY-10261R
-
|
BIBW 2992 (Standard)
|
Reference Standards
EGFR
Autophagy
Apoptosis
c-Met/HGFR
Akt
p38 MAPK
|
Cancer
|
|
Afatinib (Standard) is the analytical standard of Afatinib. This product is intended for research and analytical applications. Afatinib (BIBW 2992) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
|
-
- HY-W403933R
-
|
|
Autophagy
|
Metabolic Disease
|
|
Afatinib (Standard) is the analytical standard of Afatinib. This product is intended for research and analytical applications. Afatinib (BIBW 2992) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
|
-
- HY-10261AR
-
|
BIBW 2992MA2 (Standard)
|
Reference Standards
EGFR
Autophagy
Apoptosis
c-Met/HGFR
Akt
p38 MAPK
|
Cancer
|
|
Afatinib (dimaleate) (Standard) is the analytical standard of Afatinib (dimaleate). This product is intended for research and analytical applications. Afatinib (BIBW 2992) dimaleate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. Afatinib dimaleate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
|
-
- HY-10261E
-
|
(R)-BIBW 2992
|
EGFR
c-Met/HGFR
p38 MAPK
|
Cancer
|
|
(R)-Afatinib ((R)-BIBW 2992) is the Afatinib isomer. Afatinib (HY-10261) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
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-
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-W006886
-
|
|
Amino Acid Derivatives
|
Others
|
|
Fmoc-(R)-2-(7-octenyl)Ala-OH is an amino acid derivative with an Fmoc protecting group that can be used to synthesize inhibitor peptides that combinatorially inactivate ErbB1, ErbB2, and ErbB3 .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99275
-
|
Human Anti-ERBB3 Recombinant Antibody
|
EGFR
Akt
ERK
PARP
Survivin
|
Cancer
|
|
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 .
|
-
- HY-P99268
-
|
SAR 256212; MM 121; Anti-Human ERBB3/ERBB 3 Recombinant Antibody
|
EGFR
Apoptosis
|
Cancer
|
|
Seribantumab (MM 121) is a fully human IgG2 monoclonal antibody that targets HER3. Seribantumab blocks the activation of epidermal growth factor receptor (ErbB) family members and its downstream signal. Seribantumab inhibits neuregulin 1 (NRG1) fusion-dependent tumorigenesis in vitro and in vivo in breast, lung and ovarian patient-derived cancer models .
|
-
- HY-P991240
-
|
|
EGFR
|
Cancer
|
|
CDX-3379 is a humanized monoclonal antibody inhibitor targeting ErbB3. CDX-3379 binds to ErbB3, blocking the dimerization of ErbB3 with other receptors, thereby inhibiting the phosphorylation of ErbB3. CDX-3379 can inhibit the growth and proliferation of tumor cells. CDX-3379 is promising for research of tumors expressing ErbB3 and NRG1, such as HNSCC .
|
-
- HY-P991243
-
|
|
EGFR
PI3K
Akt
|
Cancer
|
|
MP-RM-1 is a selective murine monoclonal antibody inhibitor targeting human epidermal growth factor receptor 3 (ErbB-3). MP-RM-1 blocks the activation of ErbB-3 induced by neuregulin 1 (NRG-1β) and promotes the internalization and degradation of ErbB-3, inhibiting downstream signaling pathways such as PI3K-Akt. MP-RM-1 is promising for research of ErbB-3 highly expressed solid tumors such as breast cancer, melanoma, and prostate cancer .
|
-
- HY-P991241
-
|
|
EGFR
|
Cancer
|
|
Anti-ERBB3/HER3 (29Z6) is an antibody inhibitor, targeting to human ERBB3/HER3.
|
-
- HY-P991245
-
|
|
EGFR
|
Cancer
|
|
Anti-ERBB3/HER3 (SGP1) is a human monoclonal antibody (mAb) targeting ERBB3/HER3. Anti-ERBB3/HER3 (SGP1) inhibits Neuregulin stimulated growth of cultured breast cancer cells. Anti-ERBB3/HER3 (SGP1) can be used in breast cancer research .
|
-
- HY-P991244
-
|
|
EGFR
|
Cancer
|
|
REGN-1400 is a humanized monoclonal antibody inhibitor targeting ErbB3. REGN-1400 reduces tumor cell proliferation by inhibiting ErbB3 and blocking related signaling pathways. REGN-1400 is promising for research of solid tumors such as non-small cell lung cancer (NSCLC), colorectal cancer (CRC), and squamous cell carcinoma of the head and neck (SCCHN) .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-W403933R
-
|
|
Structural Classification
Human Gut Microbiota Metabolites
Microorganisms
Ketones, Aldehydes, Acids
Source classification
Endogenous metabolite
|
Autophagy
|
|
Afatinib (Standard) is the analytical standard of Afatinib. This product is intended for research and analytical applications. Afatinib (BIBW 2992) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
|
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-50898S
-
|
|
|
Lapatinib-d4 is the deuterium labeled Lapatinib (HY-50898). Lapatinib is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
|
-
-
- HY-50898S2
-
|
|
|
Lapatinib-d5 is deuterium labeled Lapatinib. Lapatinib (GW572016) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
|
-
-
- HY-50898S1
-
|
|
|
Lapatinib-d7 dihydrochloride is the deuterium labeled Lapatinib dihydrochloride. Lapatinib (GW572016) dihydrochloride is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
|
-
-
- HY-50898S3
-
|
|
|
Lapatinib-d4-1 is deuterium labeled Lapatinib. Lapatinib (GW572016) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
|
-
-
- HY-50898S4
-
|
|
|
Lapatinib-d7 (GW572016-d7) is deuterium labeled Lapatinib. Lapatinib (GW572016) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
|
-
-
- HY-50898CS
-
|
|
|
Lapatinib-d4 (GW572016-d4) tosylate is deuterium labeled Lapatinib (tosylate). Lapatinib (GW572016) tosylate is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
|
-
-
- HY-13272S3
-
|
|
|
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 .
|
-
-
- HY-13272S2
-
|
|
|
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 .
|
-
-
- HY-B0793S1
-
|
|
|
AZ-5104-d2 is the deuterium labeled AZ-5104. AZ-5104 is an EGFR inhibitor with IC50s of 1 nM, 6 nM, 1 nM, 25 nM and 7 nM for EGFRL858R/T790M, EGFRL858R, EGFRL861Q, EGFR and ErbB4, respectively .
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-160068
-
|
|
|
Aptamers
|
|
2-2(t) aptamer sodium is a 42-nucleotide trimeric complex of aptamer (2-2) targeting ErbB-2. 2-2(t) aptamer sodium inhibits the growth of gastric cancer cells in vitro and in vivo .
|
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