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AMG-510

Catalog No.: 112193
Cas No.: 2252403-56-6
Purity : 98% Min.
112193 - AMG-510 | CAS 2252403-56-6

Catalog number : 112193

CAS number : 2252403-56-6

分子式 : C30H30F2N6O3

分子量 : 560.59

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

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

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同义词AMG-510; AMG 510; AMG510
英文同义词AMG-510; AMG 510; AMG510
分子式C30H30F2N6O3
分子量560.59
外观crystalline solid 
纯度98% Min.
可溶性可溶于DMSO;不溶于水
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。
运输条件可在常温下运输
SmileC(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
InChiKeyNXQKSXLFSAEQCZ-SFHVURJKSA-N
InChiInChI=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
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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.

[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.


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