Search Result
Results for "
KRAS G12D inhibitor
" in MedChemExpress (MCE) Product Catalog:
2
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-115880A
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Ras
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Cancer
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KRAS G12D inhibitor 3 TFA is a KRAS G12D inhibitor with an IC50 of <500 nM. KRAS G12D inhibitor 3 TFA has antitumor effects (WO2022002102A1; compound 146) . KRAS G12D inhibitor 3 (TFA) 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-144661
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Ras
Apoptosis
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Cancer
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KRAS G12D inhibitor 14 is a potent KRAS G12D inhibitor with a KD of 33 nM for binding to KRAS G12D protein. KRAS G12D inhibitor 14 decreases the active form of KRAS G12D (KRAS G12D-GTP) but not KRAS G13D .
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- HY-115880
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Ras
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Cancer
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KRAS G12D inhibitor 3 is a KRAS G12D inhibitor with an IC50 of <500 nM. KRAS G12D inhibitor 3 has antitumor effects (WO2022002102A1; compound 146) . KRAS G12D 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-160445
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Ras
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Cancer
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KRAS G12D inhibitor 19 (Compound 7) is a KRAS G12D inhibitor. KRAS G12D inhibitor 19 can be used for the research of cancer .
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- HY-162366
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Ras
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Cancer
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KRAS G12D inhibitor 20 (Compound 14) is a selective G12D KRAS inhibitor. KRAS G12D inhibitor 20 has antitumor activity .
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- HY-172626
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Ras
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Cancer
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KRAS G12D inhibitor 28 (Compound 1) is a KRAS G12D inhibitor. KRAS G12D inhibitor 28 (Compound 1) can be used in the cancer research .
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- HY-148260
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Ras
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Cancer
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KRAS G12D inhibitor 16 is a KRAS G12D inhibitor. KRAS G12D inhibitor 16 has inhibitory activity against KRAS G12D and KRAS G12D mutation with IC50 value of 0.7 nM and 0.35 μM, respectively. KRAS G12D inhibitor 16 can be used for the research of many malignant tumor, such as pancreatic ductal adenocarcinomas (PDAC), colon and rectal carcinomas (CRC), non-small cell lung carcinomas (NSCLC) .
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- HY-158703
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Ras
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Cancer
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KRAS G12D inhibitor 24 (compound 103) is a potent inhibitor of KRAS G12D, with the IC50 of 0.004 μM. KRAS G12D inhibitor 24 has oral bioactivity .
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- HY-139894
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Ras
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Cancer
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KRAS G12D inhibitor 5 is a KRAS G12D inhibitor for the potential research of pancreatic cancer.
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- HY-158701
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Ras
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Cancer
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KRAS G12D inhibitor 23 (compound 46-3) is a potent inhibitor of KRAS G12D, with the IC50 of 0.007 μM. KRAS G12D inhibitor 23 plays an important role in cancer research .
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- HY-171255
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Ras
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Cancer
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KRAS G12D inhibitor 26 is a modulator of Kras, targeting Kras(G12D) with an IC50 ≤ 100 nM .
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- HY-143606
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Ras
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Cancer
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KRAS G12D inhibitor 12 is a potent inhibitor of KRAS G12D. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12D inhibitor 12 has the potential for the research of KRAS G12D-mediated cancer (extracted from patent WO2021108683A1, compound 134) .
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- HY-134811
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Ras
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Cancer
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KRAS G12D inhibitor 1 (example 243) is a KRAS G12D inhibitor, with an IC50 of 0.8 nM for KRAS G12D-mediated ERK phosphorylation . KRAS G12D inhibitor 1 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-143604
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Ras
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Cancer
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KRAS G12D inhibitor 11 is a potent inhibitor of KRAS G12D. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12D inhibitor 11 has the potential for the research of KRAS G12D-mediated cancer (extracted from patent WO2021108683A1, compound 52) .
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- HY-143599
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Ras
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Cancer
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KRAS G12D inhibitor 8 is a potent inhibitor of KRAS G12D. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12D inhibitor 8 has the potential for the research of KRAS G12D-mediated cancer (extracted from patent WO2021107160A1, compound 2) .
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- HY-143607
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Ras
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Cancer
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KRAS G12D inhibitor 13 is a potent inhibitor of KRAS G12D. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12D inhibitor 13 has the potential for the research of KRAS G12D-mediated cancer (extracted from patent WO2021108683A1, compound 142) .
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- HY-143602
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Ras
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Cancer
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KRAS G12D inhibitor 9 is a potent inhibitor of KRAS G12D. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12D inhibitor 9 has the potential for the research of KRAS G12D-mediated cancer (extracted from patent WO2021108683A1, compound 20) .
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- HY-143603
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Ras
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Cancer
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KRAS G12D inhibitor 10 is a potent inhibitor of KRAS G12D. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12D inhibitor 10 has the potential for the research of KRAS G12D-mediated cancer (extracted from patent WO2021108683A1, compound 34) .
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- HY-162444
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Ras
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Cancer
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KRAS G12D inhibitor 22 (compound 6) is a inhibitor of KRAS mutation. KRAS G12D inhibitor 22 has high activity (IC50＜100 nM), good selectivity and low toxicity.KRAS G12D inhibitor 22 can be used in breast cancer research .
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- HY-139911
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Ras
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Cancer
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KRAS G12D inhibitor 7 is a potent inhibitor of KRAS G12D (extracted from patent WO2021108683, compound 114) .
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- HY-139910
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Ras
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Cancer
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KRAS G12D inhibitor 6 is a potent inhibitor of KRAS G12D (extracted from patent WO2021108683A1, compound 112) .
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- HY-147595
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Ras
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Cancer
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KRAS G12D inhibitor 15 is a potent inhibitor of KRAS G12D. KRAS G12D inhibitor 15 has the potential for the research of various diseases or disorders, such as cancer or cancer metastasis (extracted from patent WO2022042630A1, compound 243) . KRAS G12D inhibitor 15 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-168577
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Ras
EGFR
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Cancer
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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 .
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- HY-156819
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RMC-9805; KRAS G12D inhibitor 18
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Ras
Apoptosis
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Cancer
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Zoldonrasib (RMC-9805) is a potent and orally active KRAS G12D inhibitor.Zoldonrasib induces apoptosis in KRAS G12D mutant cancer cells. Zoldonrasib has the potential for the research of KRAS G12D mutant cancer .
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- HY-148273
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KRAS G12D inhibitor 17
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PROTACs
Ras
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Cancer
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Setidegrasib (KRAS G12D inhibitor 17, Example 8) is a PROTAC KRAS degrader (DC50: 37 nM). Setidegrasib induces the degradation of G12D-mutation KRAS protein. Setidegrasib has antitumor effect. (Blue: E3 ligase ligand (HY-168699); Black: linker (HY-168698); Pink: G12D ligand (HY-168700)) .
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- HY-168847
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Ras
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Cancer
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INCB159020 is an orally active KRAS G12D inhibitor with a KRAS G12D SPR value of 2.2 nM. INCB159020 has antitumor activity .
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- HY-162445
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Ras
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Cancer
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KRASG12D-IN-3 (compound Z1084) is an orally active KRAS G12D inhibitor that inhibits the cell growth of AGS and AsPC-1 cells with IC50 values of 0.38 nM and 1.23 nM, respectively .
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- HY-163488
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Ras
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Cancer
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KRASG12D-IN-4 (example 38) is a KRas G12D inhibitor with an IC50 of 3.3 nM. KRASG12D-IN-4 inhibits proliferation of pancreatic cancer ASPC-1 cells with an IC50 of 12 nM .
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- HY-153413
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Ras
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Cancer
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Kras4B G12D-IN-1 is a Kras4B G12D inhibitor with anticancer effects. Kras4B G12D-IN-1 decreases Kras protein expression in mouse embryonic fibroblasts (MEF) expressing Kras4B G12D (WO2016179558A1, Comp 994566) .
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- HY-176134
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PROTACs
Ras
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Cancer
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RP03707 is a PROTAC based KRAS G12D degrader (Red: KRAS G12D inhibitor (HY-134813), black: linker, Blue: E3 ligase ligand) .
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- HY-134813
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MRTX1133
Maximum Cited Publications
22 Publications Verification
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Ras
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Cancer
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MRTX1133 is a noncovalent, potent, and selective alkyne-based KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .
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- HY-173329
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Ras
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Cancer
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KRAS inhibitor-41 is an inhibitor of KRAS with IC50 values of <0.01 μM for KRAS G12D and KRAS G12V. KRAS inhibitor-41 inhibits RAS mutant cell lines, GP2D (KRAS-G12D) and SW620 (KRAS-G12V). KRAS inhibitor-41 can be used in cancer research .
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- HY-173632
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Ras
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Cancer
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AMG410 is a non-covalent and selective pan-KRAS inhibitor with IC50 values of 1-4 nM for KRAS G12D, KRAS G12V, and KRAS G13D. AMG410 shows greater than 100-fold selectivity against both HRAS and NRAS. AMG410 is a dual GTP(on)- and GDP(off)-state inhibitor (Kd(GDP-state) of 1 nM; Kd(GTP-state) of 22 nM). AMG410 blocks KRAS signaling in a cycling state-independent manner and also blocks proliferation in wildtype KRAS-amplified tumor cells. AMG410 can be used for the study of colorectal, pancreatic, and lung cancers .
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- HY-153663
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Ras
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Cancer
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TH-Z827 is a mutant selective KRAS(G12D) inhibitor with an IC50 of 2.4 μM. TH-Z827 does not bind KRAS(WT) or KRAS(G12C). TH-Z827 blocked the KRAS(G12D)-CRAF interaction with an IC50 value of 42 μM .
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- HY-169312
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Ras
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Cancer
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KRAS inhibitor-38 (Example 18) is a KRAS inhibitor that effectively suppresses the activity of KRAS G12C, KRAS G12D, and KRAS G12V in vivo .
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- HY-134813A
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Ras
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Cancer
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MRTX1133 formic is a noncovalent, potent, and selective KRAS G12D inhibitor. MRTX1133 formic optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 formic prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRASG12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 formic shows efficacy in tumor models harboring KRAS G12D mutations .
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- HY-173637
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Ras
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Cancer
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AZD0022 is a selective and orally active KRAS G12D inhibitor. AZD0022 inhibits KRAS pathway suppression in the GP2D xenograft model .
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- HY-162439
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Ras
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Cancer
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pan-KRAS-IN-6 (compound 12) is a potent pan KRAS inhibitor with IC50 values of 9.79 nM (Kras G12D) and 6.03 nM (Kras G12V) .
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- HY-159652
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Ras
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Cancer
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KRAS inhibitor-31 (compound 33) is a KRAS inhibitor, with KD (SPR) values of 0.019 nM, 0.019 nM and 0.096 nM for KRas G12D, KRas G12C and KRas G12V, respectively .
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- HY-145962
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Ras
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Cancer
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MRTX-EX185 is a potent inhibitor of GDP-loaded KRAS and KRAS(G12D), with an IC50 of 90 nM for KRAS(G12D). MRTX-EX185 also binds GDP-loaded HRAS . MRTX-EX185 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-162446
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Ras
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Cancer
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pan-KRAS-IN-13 (compound 2) is a potent inhibitor of KRAS, with IC50s of 2.75 nM and 2.89 nM for G12D and G12V, respectively
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- HY-145962A
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Ras
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Cancer
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MRTX-EX185 formic is a potent inhibitor of GDP-loaded KRAS and KRAS(G12D), with an IC50 of 90 nM for KRAS(G12D). MRTX-EX185 formic also binds GDP-loaded HRAS . MRTX-EX185 (formic) is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-153724
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BI-2865
5 Publications Verification
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Ras
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Cancer
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BI-2865 is a none-covalent pan-KRAS Inhibitor. BI-2865 binds to WT, G12C, G12D, G12V and G13D mutant KRAS with KDs of 6.9, 4.5, 32, 26, 4.3 nM respectively. BI-2865 inhibits the proliferation of G12C, G12D or G12V mutant KRAS expressing BaF3 cells (mean IC50: roughly 140 nM) .
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- HY-163595
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Ras
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Cancer
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Pan-RAS-IN-4 (compound 2) is a potent inhibitor of RAS, with the IC50 of ＜ 100 nM for KRAS G12D. Pan-RAS-IN-4 plays an important rile in cancer research .
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- HY-153412
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Ras
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Cancer
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KRAS inhibitor-22 (compound FB9/6B9) is a potent inhibitor of K-Ras. KRAS inhibitor-22 targets to Kras 4B(G12D) and (G12C), which can be used for cancer research .
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- HY-146243
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Ras
Apoptosis
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Cancer
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TH-Z835 is a mutant selective KRAS (G12D) inhibitor with an IC50 of 1.6 μM. TH-Z835 inhibits both mantGMPPNP/GPPNP exchange and GPPNP/mantGMPPNP exchange .
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- HY-162441
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Ras
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Cancer
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pan-KRAS-IN-8 (Compound 38) is an inhibitor for in human tumor mutated genes KRAS, which inhibits proliferation of KRAS mutated cells AsPC-1 (G12D mutant) and SW480 (G12V mutant) with IC50 of 0.07 and 0.18 nM, respectively .
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- HY-162440
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Ras
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Cancer
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pan-KRAS-IN-7 (Compound 25) is an inhibitor for in human tumor mutated genes KRAS, which inhibits proliferation of KRAS mutated cells AsPC-1 (G12D mutant) and SW480 (G12V mutant) with IC50 of 0.35 and 0.51 nM, respectively .
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- HY-162442
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Ras
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Cancer
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pan-KRAS-IN-9 (Compound 52) is an inhibitor for in human tumor mutated genes KRAS, which inhibits proliferation of KRAS mutated cells AsPC-1 (G12D mutant) and SW480 (G12V mutant) with IC50 of 0.24 and 0.30 nM, respectively .
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- HY-162443
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Ras
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Cancer
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pan-KRAS-IN-10 (Compound 58) is an inhibitor for in human tumor mutated genes KRAS, which inhibits proliferation of KRAS mutated cells AsPC-1 (G12D mutant) and SW480 (G12V mutant) with IC50 of 0.7 and 0.24 nM, respectively .
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- HY-122914
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Ras
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Cancer
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KRAS inhibitor-3 is an inhibitor of KRAS inhibitor. KRAS inhibitor-3 binds to WT and oncogenic KRAS mutants with high affinity (KD: 0.28 μM for KRAS WT, 0.63 μM for KRAS G12C, 0.37 μM for KRAS G12D, 0.74 μM for KRAS Q61H). KRAS inhibitor-3 also disrupts interaction of KRAS with Raf .
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- HY-156529
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Ras
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Cancer
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pan-KRAS-IN-2 (compound 6) is a pan inhibitor of with IC50s ≤10 nM for KRAS WT and mutants (G12D, G12C, G12V, G12S, G12A, Q61H), and ＞10 μM for KRAS G13D, respectively .
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- HY-159127
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Ras
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Cancer
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HRS-4642 is a selective KRAS(G12D) inhibitor (Kd=0.083 nM) with anti-cancer activity. HRS-4642 synergizes with Carfilzomib (HY-10455) and exhibits significant in vivo potency to reshape the tumor microenvironment into an immune-activating microenvironment.
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- HY-157029S
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Ras
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Cancer
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KRASG12D-IN-1 (compound 22) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
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- HY-157031S
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Ras
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Cancer
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KRASG12D-IN-2 (compound 28) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
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- HY-137497
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Ras
Apoptosis
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Cancer
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KRAS inhibitor-9, a potent KRAS inhibitor (Kd=92 μM), blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 binds to KRAS G12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSCLC cells with KRAS mutation but not normal lung cells .
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- HY-164365
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PROTACs
Ras
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Cancer
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PROTAC K-Ras degrader-2 (compound 48) is a pan-KRAS-mutant PROTAC degrader with an IC50 of ≤200 nM for KRAS G12V/RAF1. PROTAC K-Ras degrader-2 degrades SW620 KRAS G12D with a DC50 of ≤200 nM. PROTAC K-Ras degrader-2 inhibits cell growth of SW620 3D cell with an IC50 of ≤20 nM. (Pink: KRAS inhibitor-30 (HY-164366)) .
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- HY-169311
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Ras
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Cancer
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KRAS inhibitor-37 (compound 2) is a potent KRAS inhibitor with KDs of 0.004 nM, 0.041 nM, 0.019 nM and 0.144 nM for KRAS wild type, KRAS G12D, KRAS G12C and KRAS G12V by SPR binding assay, respectively. KRAS inhibitor-37 inhibits cell proliferation with IC50s of <2 nM-14 nM for H358, SW620, PANC08.13 cells, respectively. KRAS inhibitor-37 has the potential for cancer research .
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- HY-164350
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Ras
ERK
p38 MAPK
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Cancer
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KRAS inhibitor-27 (Compound 15h) is the inhibitor for KRAS. KRAS inhibitor-27 inhibits KRAS G12D/G12V mutated cells AsPC-1, SW620 and KRAS wildtype cell HT-29 with IC50 of 378, 0.6 and 3230 nM, respectively. KRAS inhibitor-27 inhibits ERK phosphorylation (IC50 in cell AsPC-1 and SW620 is 0.6 nM and 1 nM), reduces the expression of DUSP4, thereby inhibiting MAPK signaling pathway .
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- HY-P10847
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Ras
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Cancer
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KS-58 is a KRpep-2d (HY-P3277) derivative. KS-58 is a K-Ras (G12D) inhibitory peptide that selectively binds K-Ras. KS-58 can enter cells and block intracellular Ras interaction with effector proteins. KS-58 inhibits the proliferation of tumor cells and has antitumor activity .
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- HY-159788
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PROTACs
Ras
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Cancer
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PROTAC K-Ras Degrader-4 (Compound 4) is a PROTAC degrader for KRAS that degrades KRAS G12D in GP5d and degrades KRAS G12V in cell SW620 with DC50s of 1 nM and 13 nM. PROTAC K-Ras Degrader-4 inhibits MAPK signaling pathway . (Pink: ligand for target protein pan-KRAS degrader 1 (HY-162960); Black: linker (HY-159790); Blue: ligand for E3 ligase VHL (HY-W998248))
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- HY-P2265
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SOS1
Ras
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Cancer
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SAH-SOS1A is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM), directly and independently blocks nucleotide association, impairs KRAS-driven cancer cell viability, and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .
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- HY-162873
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MEK
Raf
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Cancer
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MEK/RAF-IN-1 (Compound 16b) is an inhibitor of both MEK and RAF. It shows potent inhibition with IC50 values of 28 nM for MEK1, and 3 nM each for BRAF and BRAFV600E. MEK/RAF-IN-1 demonstrates significant antitumor activity, effectively inhibiting cell proliferation in vitro against MIA PaCa-2 (G12C KRAS), HCT116 (G13D KRAS), and C26 (G12D KRAS) cells. Additionally, it inhibits tumor growth in xenograft mouse models of colorectal cancer .
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- HY-P2265A
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SOS1
Ras
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Cancer
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SAH-SOS1A TFA is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A TFA binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM). SAH-SOS1A TFA directly and independently blocks nucleotide association. SAH-SOS1A TFA impairs KRAS-driven cancer cell viability and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .
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- HY-168012
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Ras
Phosphatase
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Cancer
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Pan-RAS-IN-6 (compound 24) is an inhibitor targeting DUSP6, which reduces MAPK activation in the brain of the NCI-H1373-Luc model (DUSP6), at the same time, it shows significant tumor growth inhibition and tumor regression effects in the NSCLC brain metastasis mouse model. Pan-RAS-IN-6 shows high selectivity and strong inhibitory effects, especially in KRAS mutation-related signaling pathways, demonstrating varying inhibitory activity against different KRAS mutants and interacting proteins. The IC50 values for KRAS G12C, G12D, and G12V are 1.3 nM, 4.7 nM, and 0.3 nM, respectively .
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- HY-147245
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STP1002
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PARP
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Cancer
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Basroparib (STP1002) is a selective, orally active inhibitor of tankyrase (TNKS1/TNKS2) with IC50 of 29.94 nM and 3.68 nM for TNKS1 and TNKS2, respectively. Basroparib has an IC50 of >10 μM for PARP1. Basroparib binds to TNKS, stabilizes AXIN1/2 proteins, blocks Wnt/β-catenin signaling pathway, inhibits tumor cell proliferation and induces apoptosis, while reducing cancer stem cell properties. Basroparib can be used in colorectal cancer (CRC) studies with KRAS mutations (such as G12V/G12D) to overcome acquired resistance to MEK inhibitors. STP1002 has synergistic antitumor activity with MEK inhibitors .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P2265A
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SOS1
Ras
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Cancer
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SAH-SOS1A TFA is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A TFA binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM). SAH-SOS1A TFA directly and independently blocks nucleotide association. SAH-SOS1A TFA impairs KRAS-driven cancer cell viability and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .
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- HY-P10847
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Ras
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Cancer
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KS-58 is a KRpep-2d (HY-P3277) derivative. KS-58 is a K-Ras (G12D) inhibitory peptide that selectively binds K-Ras. KS-58 can enter cells and block intracellular Ras interaction with effector proteins. KS-58 inhibits the proliferation of tumor cells and has antitumor activity .
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- HY-P2265
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SOS1
Ras
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Cancer
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SAH-SOS1A is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM), directly and independently blocks nucleotide association, impairs KRAS-driven cancer cell viability, and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .
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| Cat. No. |
Product Name |
Chemical Structure |
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- HY-157029S
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KRASG12D-IN-1 (compound 22) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
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- HY-157031S
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KRASG12D-IN-2 (compound 28) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
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| Cat. No. |
Product Name |
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Classification |
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- HY-115880A
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Alkynes
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KRAS G12D inhibitor 3 TFA is a KRAS G12D inhibitor with an IC50 of <500 nM. KRAS G12D inhibitor 3 TFA has antitumor effects (WO2022002102A1; compound 146) . KRAS G12D inhibitor 3 (TFA) 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-134811
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Alkynes
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KRAS G12D inhibitor 1 (example 243) is a KRAS G12D inhibitor, with an IC50 of 0.8 nM for KRAS G12D-mediated ERK phosphorylation . KRAS G12D inhibitor 1 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-134813
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Alkynes
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MRTX1133 is a noncovalent, potent, and selective alkyne-based KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .
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- HY-115880
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Alkynes
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KRAS G12D inhibitor 3 is a KRAS G12D inhibitor with an IC50 of <500 nM. KRAS G12D inhibitor 3 has antitumor effects (WO2022002102A1; compound 146) . KRAS G12D 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-158701
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Alkynes
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KRAS G12D inhibitor 23 (compound 46-3) is a potent inhibitor of KRAS G12D, with the IC50 of 0.007 μM. KRAS G12D inhibitor 23 plays an important role in cancer research .
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- HY-147595
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Alkynes
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KRAS G12D inhibitor 15 is a potent inhibitor of KRAS G12D. KRAS G12D inhibitor 15 has the potential for the research of various diseases or disorders, such as cancer or cancer metastasis (extracted from patent WO2022042630A1, compound 243) . KRAS G12D inhibitor 15 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-163488
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Alkynes
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KRASG12D-IN-4 (example 38) is a KRas G12D inhibitor with an IC50 of 3.3 nM. KRASG12D-IN-4 inhibits proliferation of pancreatic cancer ASPC-1 cells with an IC50 of 12 nM .
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- HY-173637
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Alkynes
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AZD0022 is a selective and orally active KRAS G12D inhibitor. AZD0022 inhibits KRAS pathway suppression in the GP2D xenograft model .
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- HY-159652
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Alkynes
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KRAS inhibitor-31 (compound 33) is a KRAS inhibitor, with KD (SPR) values of 0.019 nM, 0.019 nM and 0.096 nM for KRas G12D, KRas G12C and KRas G12V, respectively .
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- HY-145962
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Alkynes
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MRTX-EX185 is a potent inhibitor of GDP-loaded KRAS and KRAS(G12D), with an IC50 of 90 nM for KRAS(G12D). MRTX-EX185 also binds GDP-loaded HRAS . MRTX-EX185 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-162446
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Alkynes
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pan-KRAS-IN-13 (compound 2) is a potent inhibitor of KRAS, with IC50s of 2.75 nM and 2.89 nM for G12D and G12V, respectively
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- HY-145962A
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Alkynes
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MRTX-EX185 formic is a potent inhibitor of GDP-loaded KRAS and KRAS(G12D), with an IC50 of 90 nM for KRAS(G12D). MRTX-EX185 formic also binds GDP-loaded HRAS . MRTX-EX185 (formic) is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-157029S
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Alkynes
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KRASG12D-IN-1 (compound 22) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
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- HY-157031S
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Alkynes
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KRASG12D-IN-2 (compound 28) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
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