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MRTX849
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MRTX849图片
CAS NO:2326521-71-3
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
500mg电议

产品介绍
MRTX849 (MRTX849) 是一种有效的、可口服的、突变选择性的 KRAS G12C 共价抑制剂,具有潜在的抗肿瘤活性。 MRTX849 在残基 12 的半胱氨酸处与 KRAS G12C 共价结合,将蛋白质锁定在其无活性的 GDP 结合构象中,并抑制 KRAS 依赖性信号转导。
Cas No.2326521-71-3
别名(2S)-4-[7-(8-氯-1-萘)-5,6,7,8-四氢-2-[[((2S)-1-甲基-2-吡咯烷基]甲氧基]吡啶基[3,4-d]嘧啶-4-基]-1-(2-氟-1-氧代-2-丙烯-1-基)-2-哌嗪乙腈,MRTX849
Canonical SMILESN#CC[C@@H]1N(C(C(F)=C)=O)CCN(C2=C3C(CN(C4=C5C(Cl)=CC=CC5=CC=C4)CC3)=NC(OC[C@H]6N(C)CCC6)=N2)C1
分子式C32H35ClFN7O2
分子量604.12
溶解度DMSO: 25 mg/mL (41.38 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

MRTX849 is a potent, orally-available, and mutation-selective covalent inhibitor of KRAS G12C with potential antineoplastic activity. MRTX849 covalently binds to KRAS G12C at the cysteine at residue 12, locks the protein in its inactive GDP-bound conformation, and inhibits KRAS-dependent signal transduction[1][2].

In cell lines, MRTX849 inhibits growth and viability of cells harboring KRASG12C mutations, but not in cells with other mutant forms or of wild-type KRAS[2].

MRTX849 inhibits KRASG12C signaling in cell lines harboring this mutation, and results in tumor regression in a broad spectrum of KRASG12C animal models[2].

[1]. Christensen JG, et al. The KRASG12C Inhibitor, MRTX849, Provides Insight Toward Therapeutic Susceptibility of KRAS Mutant Cancers in Mouse Models and Patients. Cancer Discov. 2019 Oct 28. pii: CD-19-1167. [2]. Kyriakos P. Papadopoulos, et al. A phase I/II multiple expansion cohort trial of MRTX849 in patients with advanced solid tumors with KRAS G12C mutation. Journal of Clinical Oncology 2019 37:15_suppl, TPS3161-TPS3161.