AMG-510

• CAT Number: I014769
• CAS Number: 2296729-00-3
• Molecular Formula: C30H30F2N6O3
• Molecular Weight: 560.6
• Purity: ≥95%
• Synonyms: AMG-510 (S)-enantiomer
• 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: CC1CN(CCN1C2=NC(=O)N(C3=NC(=C(C=C32)F)C4=C(C=CC=C4F)O)C5=C(C=CN=C5C(C)C)C)C(=O)C=C

AMG-510(CAT: I014769) is a small-molecule inhibitor of KRAS^G12C, an oncogenic mutant form of the KRAS protein that is commonly found in many types of cancer. KRAS is a signaling protein that plays a crucial role in regulating cell growth and proliferation. However, when it is mutated, KRAS can become hyperactivated and drive the growth of cancer cells. AMG-510 works by irreversibly binding to the mutant KRAS^G12C protein, thereby blocking its activity and inhibiting the growth of cancer cells. AMG-510 has shown promising results in preclinical and clinical studies, particularly in the treatment of non-small cell lung cancer (NSCLC) and colorectal cancer. Common side effects of AMG-510 include diarrhea, nausea, and fatigue.

Overview of Clinical Research

AMG-510 is a KRAS protein inhibitor. It has been granted for the orphan drug status in Colorectal cancer and Non-small cell lung cancer.

Reference

1.Fakih, Marwan, et al. "Phase 1 study evaluating the safety, tolerability, pharmacokinetics (PK), and efficacy of AMG 510, a novel small molecule KRASG12C inhibitor, in advanced solid tumors." (2019): 3003-3003.
2.Rex, Karen, et al. "In vivo characterization of AMG 510-a potent and selective KRASG12Ccovalent small molecule inhibitor in preclinical KRASG12Ccancer models." (2019): 3090-3090.
3.Canon, Jude, et al. "The clinical KRAS (G12C) inhibitor AMG 510 drives anti-tumour immunity." Nature 575.7781 (2019): 217-223.
4.Lanman, Brian A., et al. "Discovery of AMG 510, a first-in-human covalent inhibitor of KRASG12C for the treatment of solid tumors." (2019): 4455-4455.