RMC-5127 (RMC5127) | RAS(ON) G12V inhibitor | Probechem Biochemicals

Chemical Structure : RMC-5127

CAS No.: 3082166-76-2

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RMC-5127 (MC-5127)

货号: PC-26762Not For Human Use, Lab Use Only.

RMC-5127 (RMC5127) is a potent, selective and orally bioavailable RAS(ON) G12V inhibitor with EC50 of 2.1 nM, 26-fold selective over RAS WT.

规格	价格	库存
2 mg	￥2580	In stock
5 mg	￥4580	In stock
10 mg	￥7280	In stock
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

RMC-5127 (RMC5127) is a potent, selective and orally bioavailable RAS(ON) G12V inhibitor with EC50 of 2.1 nM, 26-fold selectivity over RAS WT.
RMC-5127 potently inhibits cellular pERK with IC50 of 0.6 nM in Capan-1 cell line.
RMC-5127 suppressed RAS pathway activity, inhibits cell proliferation, and induced apoptosis in a panel of KRASG12V mutant human cancer cells in vitro but only caused submaximal inhibition in the panel of K/N/HRAS wildtype cancer cells.
RMC-5127 (3-100 mg/kg po qd) induced profound and durable anti-tumor activity in subcutaneous CDX and PDX models of KRASG12V mutant NSCLC, PDAC, and CRC in vivo.

物理化学性质&存储条件

分子量	1062.33
分子式	C57H75N9O9S
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	O=C1OCC(C)(CC2=C(C3=CC(N4CCN(C5CC5)CC4)=CN=C3[C@@H](C)OC)N(CCOC6CCOCC6)C7=CC=C(C8=CSC([C@@H]([C@H](C(N9N[C@H]1C%10CC9C%10)=O)NC([C@H]%11OC[C@@H]%11C)=O)N%12CC%13(C%12)COC%13)=N8)C=C27)C

参考文献

1. Zhe Chen, et al. Cancer Res (2024) 84 (6_Supplement): 3340.

2. Patent WO2025080946 A2.

RMC-5127 (MC-5127)

生物&药学活性

物理化学性质&存储条件

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RMC-5127 (MC-5127)

生物&药学活性

物理化学性质&存储条件

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