AMG-510 racemate
AMG-510 is a potent KRAS G12C covalent inhibitor. AMG-510 selectively targets the KRAS p.G12C mutant, at either the DNA, RNA or protein level, and prevents, through an as of yet not elucidated manner, expression of and/or tumor cell signaling through the KRAS p.G12C mutant. This may inhibit growth in KRAS p.G12C-expressing tumor cells.
For research use only. We do not sell to patients.
Chemical Information
| Name | AMG-510 racemate |
|---|---|
| Iupac Chemical Name | 4-((S)-4-acryloyl-2-methylpiperazin-1-yl)-6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(2-isopropyl-4-methylpyridin-3-yl)pyrido[2,3-d]pyrimidin-2(1H)-one |
| Synonyms | AMG-510 ; AMG 510 ; AMG510 ; AMG-510 racemate |
| Molecular Formula | C30H30F2N6O3 |
| Molecular Weight | 560.59 |
| Smile | C(C=C)(=O)N1C[C@@H](N(CC1)C=1C2=C(N(C(N1)=O)C=1C(=NC=CC1C)C(C)C)N=C(C(=C2)F)C2=C(C=CC=C2O)F)C |
| InChiKey | NXQKSXLFSAEQCZ-SFHVURJKSA-N |
| 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 |
| CAS Number | 2252403-56-6 |
| Related CAS | 2252403-56-6 ( AMG-510 racemate ) ; 2296729-00-3 ( AMG510 ) |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | crystalline solid |
|---|---|
| Purity | 98% Min. |
| Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Solubility | Soluble in DMSO, not in water |
| Handling | |
| Shipping Condition | Shipped under ambient temperature |
| HS Code |
| Targets | |
|---|---|
| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
[1]. Marwan Fakih, et al, Phase 1 study evaluating the safety, tolerability, pharmacokinetics (PK), and efficacy of AMG 510, a novel small molecule KRASG12Cinhibitor, in advanced solid tumors. Journal of Clinical Oncology.
[2]. Karen Rex, et al. Abstract 3090: In vivo characterization of AMG 510 - a potent and selective KRASG12Ccovalent small molecule inhibitor in preclinical KRASG12Ccancer models. Experimental and Molecular Therapeutics.
[3]. Brian A. Lanman, et al.Abstract 4455: Discovery of AMG 510, a first-in-human covalent inhibitor of KRASG12C for the treatment of solid tumors. Cancer Chemistry.
Chemical Structure
