AMG-510

• CAT Number: I001014
• CAS Number: 2252403-56-6
• PubChem Substance ID: 137278711
• Molecular Formula: C30H30F2N6O3
• Molecular Weight: 560.6
• Purity: 98%
• Synonyms: AMG-510;AMG510
• Target: KRAS
• Solubility: DMSO
• Appearance: Solid powder
• Storage: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
• Related CAS: 2296729-00-3 (racemate)
• Analysis method: HPLC
• IUPAC Name: 6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-propan-2-ylpyridin-3-yl)-4-[(2S)-2-methyl-4-prop-2-enoylpiperazin-1-yl]pyrido[2,3-d]pyrimidin-2-one
• InChI: InChI=1S/C30H30F2N6O3/c1-6-23(40)36-12-13-37(18(5)15-36)28-19-14-21(32)26(24-20(31)8-7-9-22(24)39)34-29(19)38(30(41)35-28)27-17(4)10-11-33-25(27)16(2)3/h6-11,14,16,18,39H,1,12-13,15H2,2-5H3/t18-/m0/s1
• InChIKey: NXQKSXLFSAEQCZ-SFHVURJKSA-N
• SMILES: O=C1N(C=2C(C(=N1)N3[C@@H](C)CN(C(C=C)=O)CC3)=CC(F)=C(N2)C4=C(F)C=CC=C4O)C5=C(C(C)C)N=CC=C5C

AMG-510 (CAT: I001014) is a small molecule inhibitor that targets KRAS G12C, a mutated form of the KRAS protein found in various cancers. KRAS G12C is known to drive tumor growth and is frequently found in lung adenocarcinoma and other solid tumors. AMG-510 works by irreversibly binding to the mutant KRAS protein, inhibiting its activity and blocking downstream signaling pathways involved in cancer cell proliferation. It has shown promising results in preclinical and early clinical studies, demonstrating tumor regression and durable responses in patients with KRAS G12C-mutated cancers. AMG-510 represents a potential targeted therapy for patients with KRAS G12C-driven cancers.

Overview of Clinical Research

KRAS protein inhibitor. It has been granted for the orphan drug status in colorectal cancer and non-small cell lung cancer.National Cancer Institute planned a phase II trial for Non-small cell lung cancer (Late-stage disease, Second-line therapy or greater) in September 2021 (PO) (NCT04625647).

Reference

1.Canon, Jude, et al. "The clinical KRAS (G12C) inhibitor AMG 510 drives anti-tumour immunity." Nature 575.7781 (2019): 217-223. 
2.Saiki, Anne Y., et al. "Discovery and in vitro characterization of AMG 510–a potent and selective covalent small-molecule inhibitor of KRASG12C." (2019): 4484-4484.