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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-Ras-RMC-7977
RMC-7977

Chemical Structure : RMC-7977

CAS No.: 2765082-12-8

RMC-7977 (RMC7977, RM-042)

货号: PC-22112Not For Human Use, Lab Use Only.

RMC-7977 is a potent, highly selective inhibitor of the active (GTP-bound) forms of KRAS, HRAS, and NRAS with Kd of 116 nM, 94.7 nM and 101 nM respectively, KRAS G12V Kd of 85 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

RMC-7977 is a potent, highly selective inhibitor of the active (GTP-bound) forms of KRAS, HRAS, and NRAS with Kd of 116 nM, 94.7 nM and 101 nM respectively, KRAS G12V Kd of 85 nM.
RMC-7977 is more than tenfold more potent for KRAS than MRAS and other RAS family small GTPase proteins with high sequence identity to KRAS.
RMC-7977 exhibits similar activity for wild-type and mutant RAS variants in biochemical assays
RMC-7977 inhibits the active state of multiple RAS variants.
RMC-7977 exhibits low nanomolar potency for growth inhibition of Matrigel-embedded human KRASG12X-mutant PDAC patient-derived organoids.
RMC-7977 (50 mg/kg, po, q.o.d) inhibits tumor growth and extends survival in autochthonous models of PDAC.

物理化学性质&存储条件

分子量 865.11
分子式 C47H60N8O6S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

参考文献

1. Urszula N Wasko, et al. bioRxiv. 2023 Dec 4:2023.12.03.569791.

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