RMC-6291 | KRAS G12C inhibitor | Probechem Biochemicals

Chemical Structure : RMC-6291

CAS No.: 2641998-63-0

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RMC-6291 (RMC6291)

货号: PC-20608Not For Human Use, Lab Use Only.

RMC-6291 (RMC6291) is a potent, covalent, next-generation, mutant-selective inhibitor of active state KRAS G12C(ON) with IC50 of 0.7 nM (pERK), RMC-6291 forms a tri-complex within tumor cells between KRASG12C(ON) and cyclophilin A (CypA).

规格	价格	库存
2 mg	￥3980	In stock
5 mg	￥5980	In stock
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25 mg		Get quote

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生物&药学活性

RMC-6291 (RMC6291) is a potent, covalent, next-generation, mutant-selective inhibitor of active state KRAS G12C(ON) with IC50 of 0.7 nM (pERK), RMC-6291 forms a tri-complex within tumor cells between KRASG12C(ON) and cyclophilin A (CypA).
RMC-6291 potently inhibits HCI-H358 cell growth (KRAS G12C) with IC50 of 0.09 nM, >10000-fold selectivity over WT cell.
RMC-6291 overcomes the limitations of first-generation KRASG12C(OFF) inhibitors in preclinical models by directly targeting the active form of KRAS G12C.
Oral administration of RMC-6291 produces deep and durable suppression of RAS pathway activity in KRASG12C tumor models and drives profound tumor regressions in vivo at well-tolerated doses.
RMC-6291 outperforms MRTX849 (Adagrasib, Cat. PC-72227), a KRASG12C(OFF) inhibitor, in mouse clinical trial consisting of multiple patient- and cell line-derived xenograft models of KRASG12C NSCLC.
Combination treatment with RMC-6291 and SHP2 or SOS1 inhibitors was well tolerated in preclinical models and further increased anti-tumor activity.
RMC-6291 also combined well with immune checkpoint inhibitors, sensitizing KRASG12C-bearing cancer models to anti-tumor immunity.

物理化学性质&存储条件

分子量	1012.28
分子式	C55H78FN9O8
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	1-(4-(dimethylamino)-4-methylpent-2-ynoyl)-N-((2S)-1-(((22S,63S,4S)-11-ethyl-12-(2-((S)-1-methoxyethyl)pyridin-3-yl)-10,10-dimethyl-5,7-dioxo-61,62,63,64,65,66-hexahydro-11H-8-oxa-2(4,2)-morpholina-1(5,3)-indola-6(1,3)-pyridazinacycloundecaphane-4-yl)amino)-3-methyl-1-oxobutan-2-yl)-4-fluoro-N-methylpiperidine-4-carboxamide

参考文献

1. Robert J. Nichols, et al. Cancer Res (2022) 82 (12_Supplement): 3595.

RMC-6291 (RMC6291)

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物理化学性质&存储条件

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RMC-6291 (RMC6291)

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物理化学性质&存储条件

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