Search Result
Results for "
KRAS G12C inhibitor
" in MedChemExpress (MCE) Product Catalog:
2
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-142460
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Ras
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Cancer
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KRAS G12C inhibitor 28 is a KRAS G12C inhibitor with an IC50 of 57 nM. KRAS G12C inhibitor 28 has antitumor effects (WO2021113595A1; Example 1) .
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- HY-142458
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Ras
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Cancer
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KRAS G12C inhibitor 27 is a KRAS G12C inhibitor with antitumor effects (WO2021109737) .
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- HY-142457
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Ras
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Cancer
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KRAS G12C inhibitor 26 is a KRAS G12C inhibitor with antitumor effects (WO2021109737) .
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- HY-157067
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Ras
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Cancer
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KRAS G12C inhibitor 62 is a KRAS G12C inhibitor. KRAS G12C inhibitor 62 has the potential for the research of KRAS G12C-mediated cancer (extracted from patent WO2021121367A1) .
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- HY-147636
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Ras
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Cancer
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KRAS G12C inhibitor 55 (Compound 1) is a KRAS G12C inhibitor .
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- HY-147634
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Ras
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Cancer
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KRAS G12C inhibitor 53 (Compound 1) is a KRAS G12C inhibitor .
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-
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- HY-147632
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Ras
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Cancer
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KRAS G12C inhibitor 51 (example 1) is a KRAS G12C inhibitor .
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- HY-147635
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Ras
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Cancer
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KRAS G12C inhibitor 54 (Compound 1) is a KRAS G12C inhibitor .
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-
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- HY-147633
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Ras
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Cancer
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KRAS G12C inhibitor 52 (Compound 7) is a KRAS G12C inhibitor .
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- HY-145022
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Ras
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Cancer
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KRAS G12C inhibitor 25 is a KRAS G12C inhibitor. KRAS G12C inhibitor 25 inhibits SOSl-assisted GDP/GTP exchanging activity of KRAS-G12C mutant (IC50=0.48 nM). From WO2021216770A1 compound 3 .
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- HY-132980
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Ras
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Cancer
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KRAS G12C inhibitor 19 is a potent inhibitor of KRAS G12C. KRAS G12C inhibitor 19 significantly inhibits tumor growth (extracted from patent WO2021118877A1) .
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- HY-145020
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Ras
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Cancer
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KRAS G12C inhibitor 23 is a KRAS G12C inhibitor. KRAS G12C inhibitor 23 inhibits H358 cells with an IC50 of 491 nM (WO2021218939A1, compound 1) .
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- HY-142947
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Ras
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Cancer
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KRAS G12C inhibitor 45 (compound 78) is a potent KRAS G12C inhibitor .
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- HY-153461
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Ras
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Cancer
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KRAS G12C inhibitor 58 is a KRAS G12C inhibitor, used in cancer research .
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- HY-143592
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Ras
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Cancer
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KRAS G12C inhibitor 39 is a potent inhibitor of KRAS G12C. KRas is a highly attractable target of the pharmaceutical industry for cancer research. KRAS G12C inhibitor 39 has the potential for the research of KRAS G12C-mediated cancer (extracted from patent WO2019099524A1, compound 494) .
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- HY-142478
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Ras
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Cancer
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KRAS G12C inhibitor 29 is a KRAS G12C inhibitor extracted from patent WO2021252339A1, compound 3. KRAS G12C inhibitor 29 can be used for the research of cancer .
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- HY-142481
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Ras
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Cancer
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KRAS G12C inhibitor 30 is a KRAS G12C inhibitor extracted from patent WO2021252339A1, compound 2. KRAS G12C inhibitor 30 can be used for the research of cancer .
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- HY-142485
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Ras
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Cancer
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KRAS G12C inhibitor 31 is a KRAS G12C inhibitor extracted from patent WO2021252339A1, compound 1. KRAS G12C inhibitor 31 can be used for the research of cancer .
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- HY-142490
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Ras
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Cancer
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KRAS G12C inhibitor 33 is a KRAS G12C inhibitor extracted from patent WO2021244603A1, compound 1. KRAS G12C inhibitor 33 can be used for the research of cancer .
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- HY-151968
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Ras
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Cancer
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KRAS G12C inhibitor 57 (Compound 50) is a potent, selective, covalent and orally active KRAS G12C inhibitor with an IC50 of 0.21 μM in KRAS G12C/SOS1 binding assay. KRAS G12C inhibitor 57 induces cancer cell apoptosis .
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- HY-142948
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Ras
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Cancer
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KRAS G12C inhibitor 46 (compound WX003) is a potent KRAS G12C inhibitor .
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- HY-142511
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Ras
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Cancer
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KRAS G12C inhibitor 34 is a KRAS G12C inhibitor extracted from patent WO2021239058A1, compound Z1. KRAS G12C inhibitor 34 can be used for the research of cancer .
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- HY-153944
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Ras
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Cancer
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KRAS G12C inhibitor 60 (compound 23) is a Kras-G12C inhibitor. KRAS G12C inhibitor 60 can be used for the research of lung cancer, colorectal cancer, pancreatic cancer .
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- HY-147631
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Ras
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Cancer
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KRAS G12C inhibitor 50 (Example 4) is a KRAS G12C inhibitor with an IC50 of 46.7 nM .
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- HY-143588
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Ras
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Cancer
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KRAS G12C inhibitor 35 is a potent inhibitor of KRAS G12C. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12C inhibitor 35 has the potential for the research of KRAS G12C-mediated cancer (extracted from patent CN112920183A, compound 3) .
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- HY-132979
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Ras
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Cancer
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KRAS G12C inhibitor 18 is a potent and orally active KRAS G12C inhibitor. Anti-tumor activities .
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- HY-143596
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Ras
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Cancer
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KRAS G12C inhibitor 41 is a potent inhibitor of KRAS G12C. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12C inhibitor 41 has the potential for the research of KRAS G12C-mediated cancer (extracted from patent WO2021129824A1, compound 121) .
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- HY-143594
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Ras
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Cancer
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KRAS G12C inhibitor 40 is a potent inhibitor of KRAS G12C. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12C inhibitor 40 has the potential for the research of KRAS G12C-mediated cancer (extracted from patent WO2021129824A1, compound 70) .
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- HY-143590
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Ras
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Cancer
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KRAS G12C inhibitor 37 is a potent inhibitor of KRAS G12C. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12C inhibitor 37 has the potential for the research of KRAS G12C-mediated cancer (extracted from patent WO2018143315A1, compound 65) .
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- HY-143591
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Ras
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Cancer
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KRAS G12C inhibitor 38 is a potent inhibitor of KRAS G12C. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12C inhibitor 38 has the potential for the research of KRAS G12C-mediated cancer (extracted from patent WO2021129820A1, compound 171) .
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- HY-143598
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Ras
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Cancer
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KRAS G12C inhibitor 42 is a potent inhibitor of KRAS G12C. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12C inhibitor 42 has the potential for the research of KRAS G12C-mediated cancer (extracted from patent WO2020146613A1, compound 10) .
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- HY-112494
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Ras
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Cancer
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KRas G12C inhibitor 1 is a compound that inhibits KRas G12C, extracted from patent US 20180072723 A1.
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- HY-112491
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Ras
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Cancer
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KRas G12C inhibitor 1 is a compound that inhibits KRas G12C, extracted from patent US 20180072723 A1.
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- HY-112493
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Ras
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Cancer
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KRas G12C inhibitor 3 is a compound that inhibits KRas G12C, extracted from patent US 20180072723 A1.
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- HY-112492
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Ras
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Cancer
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KRas G12C inhibitor 2 is a compound that inhibits KRas G12C, extracted from patent US 20180072723 A1.
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- HY-145017
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Ras
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Cancer
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KRAS G12C inhibitor 20 is a KRAS G12C inhibitor extracted from patent CN112694475A, example 1 .
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- HY-142487
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Ras
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Cancer
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KRAS G12C inhibitor 32, an eight membered heterocyclic compound containing N, is a potent KRAS G12C inhibitor .
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- HY-153899
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Ras
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Cancer
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KRAS G12C inhibitor 59 is a KRAS G12C inhibitor with anticancer effects (WO2023036282A1, compound II) .
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- HY-142946
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Ras
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Cancer
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KRAS G12C inhibitor 44 (compound 54) is a potent and orally active KRAS G12C inhibitor. KRAS G12C inhibitor 44 shows anti-proliferation activities with IC50s of 0.016, 0.028 µM in MIA PaCA-2, H358 cells, respectively. KRAS G12C inhibitor 44 shows antitumor effects in vivo .
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- HY-126292
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Ras
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Cancer
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KRAS G12C inhibitor 13 is a KRAS G12C inhibitor extracted from patent WO2018143315A1, compound 30 .
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- HY-145018
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Ras
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Cancer
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KRAS G12C inhibitor 21 is a KRAS G12C inhibitor extracted from patent WO2021219090A1, example 7 .
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- HY-145019
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Ras
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Cancer
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KRAS G12C inhibitor 22 is a KRAS G12C inhibitor extracted from patent WO2021219072A1, example 120 .
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- HY-114168
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Ras
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Cancer
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KRAS G12C inhibitor 5 is a KRas G12C inhibitor extracted from patent WO2017201161A1, Compound example 147 .
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- HY-146537
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Ras
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Cancer
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KRAS G12C inhibitor 47 (compound 8-1-1) is a potent KRAS G12C inhibitor with an IC50 of 0.172 µM. KRAS G12C inhibitor 47 shows p-ERK inhibition activities with IC50s of 0.046, 69.8 µM in MIA PaCA-2, A549 cells, respectively. KRAS G12C inhibitor 47 has the potential for the research of pancreatic, colorectal, and lung cancers .
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- HY-125873
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Ras
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Cancer
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KRAS G12C inhibitor 15 is a potent KRAS G12C inhibitor extracted from patent WO2019110751A1, compound 22, has an IC50 of 5 nM .
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- HY-125875
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Ras
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Cancer
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KRAS G12C inhibitor 17 is a potent KRAS G12C inhibitor extracted from patent WO2019110751A1, compound 82, has an IC50 of 5 nM .
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- HY-125874
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Ras
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Cancer
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KRAS G12C inhibitor 16 is a potent KRAS G12C inhibitor extracted from patent WO2019110751A1, compound 39, has an IC50 of 97 nM .
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- HY-125872
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Ras
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Cancer
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KRAS G12C inhibitor 14 is a potent KRAS G12C inhibitor extracted from patent WO2019110751A1, compound 17, has an IC50 of 18 nM .
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- HY-142945
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Ras
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Cancer
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KRAS G12C inhibitor 43 (compound 59) is a potent KRAS G12C inhibitor. KRAS G12C inhibitor 43 shows antimigration and anti-proliferative activity with IC50s of 0.001-1 µM, >1 µM, >1 µM for H358, A549, HCC cells ,respectively .
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- HY-148261
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Ras
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Cancer
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KRAS G12C inhibitor 56 (compound IC-6) is a potent SOS1 inhibitor with an IC50 of 1.6 nM. KRAS G12C inhibitor 56 can be used in cancer research .
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- HY-146061
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Ras
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Cancer
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KRAS G12C inhibitor 48 (compound 6e) is a potent KRAS G12C inhibitor with an IC50 of 639.91 nM. KRAS G12C inhibitor 48 (0-50 µM) shows anti-proliferative activity with IC50s of 0.796, 6.33, 16.14 µM for H358, H23, A549 cells, respectively .
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- HY-156549
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ERK
Ras
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Cancer
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KRAS G12C inhibitor 61 (Example 3) inhibits phospho-ERK 1/2 in MIA PaCa-2 cells with an IC50 value of 9 nM. KRAS G12C inhibitor 61 can be used for research of pancreatic, colorectal, and lung cancers .
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- HY-143589
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JAB-21822; KRAS G12C inhibitor 36
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Ras
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Cancer
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Glecirasib (KRAS G12C inhibitor 36) is a potent inhibitor of KRAS G12C. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. Glecirasib has the potential for the research of KRAS G12C-mediated cancer (extracted from patent WO2021121367A1, compound 1-2) .
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- HY-12446
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Ras
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Cancer
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K-Ras (G12C) inhibitor 9 is an allosteric inhibitor of the K-Ras (G12C) .
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- HY-114277A
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AMG-510 racemate
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Ras
p38 MAPK
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Cancer
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Sotorasib racemate (Compound A) is an orally active racemate of Sotorasib (HY-114277), a covalent inhibitor of KRAS G12C mutant which induces adaptive feedback activation of MAPK pathway. Sotorasib racemate also exerts inhibitor activity against KRAS G12C induced cancer and can be applied to cancer research .
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- HY-114277
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Sotorasib
Maximum Cited Publications
44 Publications Verification
AMG-510
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Ras
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Cancer
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Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib is the first KRAS G12C inhibitor in clinical development and leads to the regression of KRAS G12C tumors .
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- HY-158107
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Ras
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Cancer
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BBO-8520 is a direct small molecule covalent inhibitor targeting KRAS G12C with high oral availability. BBO-8520 has the characteristics of KRAS G12C (OFF) inhibitor and the function of blocking KRAS G12C (ON) signal. BBO-8520 inhibits cell proliferation by inhibiting KRAS G12C (ON) by binding GTP protein. BBO-8520 can block RAS-RAF1 interaction and return KRAS G12C to the inactive (OFF) state .
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- HY-18605
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Ras
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Cancer
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K-Ras G12C-IN-2 is an irreversible covalent K-Ras G12C inhibitor.
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- HY-18606
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Ras
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Cancer
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K-Ras G12C-IN-3 is a novel and irreversible inhibitor of mutant K-ras G12C.
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- HY-151287
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Ras
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Cancer
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KRAS inhibitor-20 is a small molecular inhibitor of KRas G12C, the oncogenic mutant. KRAS inhibitor-20 inhibits KRas G12C with the IC50 value <10 nM .
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- HY-128771
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Ras
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Cancer
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K-Ras G12C-IN-4, compound 1, is a potent Covalent Inhibitor of KRAS G12C .
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- HY-18604
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Ras
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Cancer
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K-Ras G12C-IN-1 is a novel and irreversible inhibitor of mutant K-ras G12C extracted from patent WO 2014152588 A1.
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- HY-132966
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Ras
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Cancer
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ASP2453 is a potent, selective and covalent KRAS G12C inhibitor. ASP2453 inhibits the Son of Sevenless (SOS)-mediated interaction between KRAS G12C and Raf with an IC50 value of 40 nM.
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- HY-141477
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Ras
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Cancer
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RM-018 is a potent, functionally distinct tricomplex KRAS G12C active-state inhibitor. RM-018 retains the ability to bind and inhibit KRAS G12C/Y96D and could overcome resistance. RM-018 binds specifically to the GTP-bound, active [“RAS(ON)”] state of KRAS G12C .
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- HY-153821
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Ras
PROTACs
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Cancer
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PROTAC KRAS G12C degrader-2 (compound 432) is a modulator of K-Ras protein hydrolysis. PROTAC KRAS G12C degrader-2 is a bifunctional compound, which contain on one end a cereblon inhibitor of apoptosis proteins (IAP) and on the other end a moiety which binds KRAS .
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- HY-144323
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PROTACs
PERK
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Cancer
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YF135 is an efficient and reversible-covalent KRAS G12C PROTAC. YF135 is designed and synthesized by tethering KRAS G12C inhibitor 48 (compound 6d) as the ligand, and basing on the scaffold of MRTX849 linkage VHL ligand. YF135 significantly induces the degradation of KRAS G12C in a reversible manner and decreases phospho-ERK level through the E3 ligase VHL mediated proteasome pathway .
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- HY-130149
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MRTX849
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Ras
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Cancer
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Adagrasib (MRTX849) is a potent, orally-available, and mutation-selective covalent inhibitor of KRAS G12C with potential antineoplastic activity. Adagrasib covalently binds to KRAS G12C at the cysteine at residue 12, locks the protein in its inactive GDP-bound conformation, and inhibits KRAS-dependent signal transduction .
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- HY-153346
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Ras
ERK
Apoptosis
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Cancer
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RMC-6291 is an orally active and covalent inhibitor of KRAS G12C(ON). RMC-6291 forms a tri-complex within tumor cells between KRAS G12C(ON) and cyclophilin A (CypA). Thus, RMC-6291 prevents KRAS G12C(ON) from signaling via steric blockade of RAS effector binding. RMC-6291 inhibits ERK signaling and induced apoptosis in KRASG12C-mutant H358 cells. RMC-6291 also inhibits the proliferation of KRAS G12C mutant cells with a median IC50 of 0.11 nM .
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- HY-151999
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Ras
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Cancer
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KRASG12C IN-1 is a potent and covalent KRAS G12C inhibitor that traps KRAS G12C in the GDP-bound state. KRASG12C IN-1 exhibits potent antitumor activity against KRAS-mutant non-small cell lung cancer .
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- HY-U00418
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Ras
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Cancer
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ARS-1620 is an atropisomeric selective KRAS G12C inhibitor with desirable pharmacokinetics.
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- HY-145928
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GDC-6036
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Ras
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Cancer
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Divarasib (GDC-6036) is an orally bioavailable, highly potent, and selective KRAS G12C inhibitor with an IC50 of <0.01 μM. Divarasib covalently binds to the switch II (SW-II) pocket of KRAS G12C and irreversibly locks it in the inactive GDP-bound state.
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- HY-114277S
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AMG-510-d7
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Ras
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Cancer
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Sotorasib-d7 (AMG-510-d7) is a deuterium-labeled Sotorasib (HY-114277). Sotorasib is an orally active covalent inhibitor of KRAS G12C. Sotorasib can lead to the regression of KRAS G12C tumors .
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- HY-148098
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Ras
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Cancer
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Pan KRas-IN-1 is a pan KRas inhibitor, can be used for agent resistance in cancer developed with KRas G12C inhibitors .
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- HY-135864
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Ras
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Cancer
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KRAS inhibitor-6 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound A .
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- HY-145928B
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GDC-6036 adipate
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Ras
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Cancer
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Divarasib (GDC-6036) adipate is an orally bioavailable, highly potent, and selective KRAS G12C inhibitor with an IC50 of <0.01 μM. Divarasib covalently binds to the switch II (SW-II) pocket of KRAS G12C and irreversibly locks it in the inactive GDP-bound state .
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- HY-135866
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Ras
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Cancer
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KRAS inhibitor-8 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound C .
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- HY-135865
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Ras
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Cancer
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KRAS inhibitor-7 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound B .
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- HY-152248
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Ras
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Cancer
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ARS-2102 is a potent covalent KRAS G12C inhibitor for use in cancer research .
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- HY-156671
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Ras
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Cancer
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RMC-4998 is a molecular glue compound with good antitumor activity. RMC-4998 is able to form a ternary complex with CYPA and an activated KRAS G12C mutant. Furthermore, CYPA binding to KRAS G12C blocks the interaction between activated KRAS mutants and downstream effector proteins, thereby inhibiting signaling that promotes cell proliferation .
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- HY-151288
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Ras
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Cancer
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KRAS inhibitor-21 (22b) is a KRAS G12C inhibitor with an IC50 value of <0.01 μM. KRAS inhibitor-21 can be used in cancer research .
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- HY-156528
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Ras
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Cancer
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pan-KRAS-IN-4 (compound 5) is a potent inhibitor of KRAS with IC50s of 0.37 nM (Kras G12C), 0.19 nM (Kras G12V), respectively .
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- HY-114436
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Ras
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Cancer
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MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells .
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- HY-151571
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Ras
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Cancer
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ZG1077 is a covalent KRAS G12C inhibitor. ZG1077 can be used in the research of non-small cell lung cancer (NSCLC) .
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- HY-153724
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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-144207
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Ras
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Cancer
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SOS1-IN-9 is a potent SOS1 inhibitor with an IC50 of 116.5 nM for SOS1-KRAS G12C (WO2022028506A1, compound 302) .
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- HY-U00416
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Ras
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Cancer
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ARS-1323, the racemate of ARS-1620, is a novel inhibitor of mutant K-ras G12C extracted from patent WO 2015054572 A1.
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- HY-154959
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Ras
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Cancer
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AZD4747 is a selective, blood-brain barrier-permeable mutant GTPase KRAS G12C inhibitor. AZD4747 has the potential to study cancer .
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- HY-162281
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Others
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Cancer
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PROTAC SOS1 degrader-6 (compound 23) is a potent SOS1 PROTACs degrader with synergistic efficacy with KRAS G12C inhibitors .
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- HY-114277B
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AMG-510 isomer
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Others
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Others
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Sotorasib (AMG-510) isomer is the less active isomer of Sotorasib (AMG-510). AMG-510 is a potent KRAS G12C covalent inhibitor.
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- HY-148278
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Ras
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Cancer
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BI-0474 is a potent KRAS G12C inhibitor with an IC50 value of 7.0 nM for the GDP-KRAS::SOS1 protein-protein interaction. BI-0474 exhibits good anti-proliferative activity against NCI-H358 cells carrying the G12C mutation. BI-0474 also shows good anti-tumour activity in non-small cell lung cancer xenograft models .
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- HY-U00417
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Ras
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Cancer
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ARS-1630, a less active enantiomer of ARS-1620, is a novel inhibitor of mutant K-ras G12C extracted from patent WO 2015054572 A1.
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- HY-146223
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Ras
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Cancer
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AZD4625 (Compound 21) is a highly potent, selective, covalent and allosteric inhibitor of the mutant GTPase KRAS G12C. AZD4625 has high oral bioavailability .
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- HY-153262
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Ras
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Cancer
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KRASG12C IN-2 (compound 17) is an orally active KRAS G12C inhibitor. KRASG12C IN-2 inhibits tumor growth in mice .
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- HY-162249
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Ras
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Cancer
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ASP6918 is a potent and orally active KRAS G12C inhibitor with an IC50 value of 0.028 µM. ASP6918 inhibits cell growth. ASP6918 shows antitumor activity .
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- HY-19706
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ARS-853
2 Publications Verification
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Ras
Apoptosis
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Cancer
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ARS-853 is a cell-active, selective, covalent KRAS G12C inhibitor with an IC50 of 2.5 μM. ARS-853 inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation .
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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-144213
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Ras
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Cancer
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SOS1-IN-10 is a potent SOS1 inhibitor with an IC50 of 13 nM for KRAS G12C-SOS1 (WO2022017519A1, compound 8) .
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- HY-154313
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Clospirazine
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Ras
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Cancer
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Spiclomazine (Clospirazine) is a potent mutant KRAS(G12C) inhibitor that selectively inhibits mutant KRAS-driven pancreatic cancer. Spiclomazine can eliminate KRas-GTP levels in KRAS-driven pancreatic cancer and effectively inhibit RAS-mediated signaling. Spiclomazine significantly inhibits tumor progression in mouse renal capsule xenotransplantation models .
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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-139612
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JDQ-443; NVP-JDQ443
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Ras
PERK
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Cancer
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Opnurasib (JDQ-443) (NVP-JDQ443) is an orally active, potent, selective, and covalent KRAS G12C inhibitor (extracted from patent WO2021120890A1). Opnurasib shows antitumor activity .
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- HY-W016889
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Ras
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Cancer
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CFL-137 is a potent KRas G12C inhibitor. CFL-137 shows an antiproliferative effect. CFL-137 shows anticancer activity. CFL-137 has the potential for the research of lung cancer .
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- HY-W041315
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Ras
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Cancer
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CFL-120 is a potent KRas G12C inhibitor. CFL-120 shows an antiproliferative effect. CFL-120 shows anticancer activity. CFL-120 has the potential for the research of lung cancer .
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- HY-114436S
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Isotope-Labeled Compounds
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Cancer
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MRTX-1257-d6 is the deuterium labeled MRTX-1257 (HY-114436). MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells .
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- HY-146543
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Ras
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Cancer
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KRAS inhibitor-13 (compound 5-6) is a potent KRAS G12C inhibitor with an IC50 of 0.883 µM. KRAS inhibitor-13 shows p-ERK inhibition activities with IC50s of 5.9, >100 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-13 has the potential for the research of pancreatic, colorectal, 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-160699
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ULK
Ras
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Cancer
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DCC-3116 is an orally active ULK1/2 inhibitor. DCC-3116 can promote autophagy in lung cancer cells by inhibiting KRAS G12C signaling, thereby inhibiting the proliferation of lung cancer cells and exerting anti-cancer effects .
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- HY-162431
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Ras
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Cancer
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MK-1084 is a selective KRAS G12C inhibitor that is currently in Phase I clinical trial (NCT05067283). MK-1084 exhibits anticancer activity and can be used either alone or in combination with pembrolizumab (HY-P9902) for cancer research .
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- HY-146533
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Ras
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Cancer
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KRAS inhibitor-12 (compound 6-1) is a potent KRAS G12C inhibitor with an IC50 of 0.537 µM. KRAS inhibitor-12 shows p-ERK inhibition activities with IC50s of 1.3, 3.7 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-12 has the potential for the research of pancreatic, colorectal, and lung cancers .
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-
- HY-146544
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|
Ras
|
Cancer
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KRAS inhibitor-14 (compound 3-22) is a potent KRAS G12C inhibitor with an IC50 of 0.249 µM. KRAS inhibitor-14 shows p-ERK inhibition activities with IC50s of 1.12, >33.3 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-14 has the potential for the research of pancreatic, colorectal, and lung cancers .
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- HY-146545
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Ras
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Cancer
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KRAS inhibitor-15 (compound 3-19) is a potent KRAS G12C inhibitor with an IC50 of 0.954 µM. KRAS inhibitor-15 shows p-ERK inhibition activities with IC50s of 2.03, >33.3 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-15 has the potential for the research of pancreatic, colorectal, and lung cancers .
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-
- HY-146546
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|
Ras
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Cancer
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KRAS inhibitor-16 (compound 3-11) is a potent KRAS G12C inhibitor with an IC50 of 0.457 µM. KRAS inhibitor-16 shows p-ERK inhibition activities with IC50s of 3.06, 11.1 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-16 has the potential for the research of pancreatic, colorectal, and lung cancers .
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- HY-146475
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Ras
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Cancer
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KRAS inhibitor-17 (compound 3-9) is a potent KRAS G12C inhibitor with an IC50 of 3.37 µM. KRAS inhibitor-17 shows p-ERK inhibition activities with IC50s of 9.25, >33.3 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-17 has the potential for the research of pancreatic, colorectal, and lung cancers .
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- HY-146476
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Ras
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Cancer
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KRAS inhibitor-18 (compound 3-10) is a potent KRAS G12C inhibitor with an IC50 of 4.74 µM. KRAS inhibitor-18 shows p-ERK inhibition activities with IC50s of 66.4, 11.1 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-18 has the potential for the research of pancreatic, colorectal, and lung cancers .
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- HY-147214
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YAP
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Cancer
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GNE-7883 is a pan-TEAD inhibitor with anti-cell proliferation activity. GNE-7883 overcomes resistance to KRAS G12C inhibitors in multiple preclinical models by inhibiting YAP/TAZ activation. GNE-7883 may be used in the study of YAP/TAZ-dependent cancers .
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- HY-137497
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Ras
Apoptosis
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Cancer
|
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-145571
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D-1553
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Ras
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Cancer
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Garsorasib is a potent inhibitor of KRAS G12C with an IC50 of 10 nM. Garsorasib has the potential for the research of various cancer such as pancreatic cancer, endometrial cancer, colorectal cancer, or lung cancer (non-small cell lung cancer) (extracted from patent WO2020233592A1, compound 2) .
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- HY-154959A
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Others
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Cancer
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(9R,12aR)-AZD4747 is a diastereomer of AZD4747 (HY-154959). AZD4747 is a selective mutant GTPase KRAS G12C inhibitor with blood-brain barrier permeability. AZD4747 has the potential to study cancer .
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- HY-139612A
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(S)-NVP-JDQ443
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Ras
PERK
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Cancer
|
(S)-JDQ-443 is an isomer of JDQ-443 (HY-139612). JDQ-443 is an orally active, potent, selective, and covalent KRAS G12C inhibitor (extracted from patent WO2021120890A1). JDQ-443 shows antitumor activity .
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- HY-156498
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|
Ras
|
Cancer
|
RMC-7977 is a reversible, tri-complex RAS inhibitor with broad spectrum activity for both mutant and wild-type (WT) KRAS, NRAS, and HRAS variants.RMC-7977 can lead to tumor regressions and was well tolerated in diverse RAS-addicted preclinical cancer models. RMC-7977 also can inhibit the growth of KRAS G12C cancer models .
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- HY-128522
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Ras
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Cancer
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ARS-1323-alkyne, a switch-II pocket (S-IIP) inhibitor, is a conformational specific chemical reporter of KRAS G12C nucleotide state in living cells . ARS-1323-alkyne 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-146223A
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Others
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Cancer
|
(3R,10R,14aS)-AZD4625 is the isomer of AZD4625 (HY-146223), and can be used as an experimental control. AZD4625 (Compound 21) is a highly potent, selective, covalent and allosteric inhibitor of the mutant GTPase KRAS G12C. AZD4625 has high oral bioavailability .
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- HY-P2265
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Ras
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Cancer
|
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-115907
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Ras
ERK
Apoptosis
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Cancer
|
K20 is a potent and selective KRas G12C inhibitor with an IC50 of 1.16 µM. K20 shows anticancer activity in H358 cells (IC50= 0.78 µM). K20 decreases the levels of phosphorylated Erk and leads to cancer cell apoptosis. K20 suppresses NCI-H358 tumor growth with a TGI of 41% without causing obvious toxicity .
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- HY-P2265A
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|
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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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P2265A
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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-P2265
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|
Ras
|
Cancer
|
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 |
-
- HY-114277S
-
|
Sotorasib-d7 (AMG-510-d7) is a deuterium-labeled Sotorasib (HY-114277). Sotorasib is an orally active covalent inhibitor of KRAS G12C. Sotorasib can lead to the regression of KRAS G12C tumors .
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-
-
- HY-114436S
-
|
MRTX-1257-d6 is the deuterium labeled MRTX-1257 (HY-114436). MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells .
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Cat. No. |
Product Name |
|
Classification |
-
- HY-134654
-
|
|
Alkynes
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MRTX849 analog 24 is an alkyne-containing click probe analogue of KRAS G12C inhibitor MRTX849, which is used to research MRTX849 function .
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- HY-128522
-
|
|
Alkynes
|
ARS-1323-alkyne, a switch-II pocket (S-IIP) inhibitor, is a conformational specific chemical reporter of KRAS G12C nucleotide state in living cells . ARS-1323-alkyne 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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