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.
仅供研究使用。 我们不向患者出售。
化学信息
| 名称 | AMG-510 racemate |
|---|---|
| Iupac 化学名称 | 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 |
| 同义词 | AMG-510 ; AMG 510 ; AMG510 ; AMG-510 racemate |
| 英文同义词 | AMG-510 ; AMG 510 ; AMG510 ; AMG-510 racemate |
| 分子式 | C30H30F2N6O3 |
| 分子量 | 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号 | 2252403-56-6 |
| 相关CAS号 | 2252403-56-6 ( AMG-510 racemate ) ; 2296729-00-3 ( AMG510 ) |
订购信息
| 包装 | 价格 | 库存 | 纯度 | 备货期 |
|---|---|---|---|---|
| 大货 | 询价 | 询价 | 询价 |
| 外观性状 | crystalline solid |
|---|---|
| 纯度 | 98% Min. |
| 存储 | 短期可在0-4度保存，数天至数月；长期可在-20度保存三年。 |
| 可溶性 | 可溶于DMSO；不溶于水 |
| 处理方式 | |
| 运输条件 | 可在常温下运输 |
| 海关编码 |
| 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.
