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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-Ras-RMC-9805
RMC-9805

Chemical Structure : RMC-9805

CAS No.: 2922732-54-3

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RMC-9805 (RMC9805)

货号: PC-23832Not For Human Use, Lab Use Only.

RMC-9805 is a potent, selective and covalent inhibitor of KRAS G12D with EC50 of 23 nM (AsPC-1, pERK), highly selective for crosslinking RAS G12D(ON).

规格 价格 库存 数量
1 mg ￥1580 In stock
5 mg ￥2980 In stock
10 mg ￥4880 In stock
25 mg ￥7880 In stock
50 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

RMC-9805 is a potent, selective and covalent inhibitor of KRAS G12D with EC50 of 23 nM (AsPC-1, pERK), highly selective for crosslinking RAS G12D(ON).
RMC-9805 modulates RAS pathway signaling and induces apoptosis in KRASG12D xenograft tumors in vivo, causes regressions of KRASG12D xenograft models at well-tolerated doses in vivo.
RMC-9805 monotherapy elicited tumor regressions in most preclinical PDAC and NSCLC cancer models harboring KRASG12D.
RMC-9805 also synergized with anti-PD1 therapy in KRASG12D tumors in immune-competent animal models by shaping a favorable tumor immune microenvironment through cytokine modulation.

物理化学性质&存储条件

分子量 1168.44
分子式 C63H88F3N11O7
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

(2S)-2-Cyclopentyl-2-((S)-7-((2R,3R)-3-cyclopropyl-1-methylaziridine-2-carbonyl)-2,7-diazaspiro[4.4]nonan-2-yl)-N-((22S,63S,4S)-12-(5-(4-cyclopropylpiperazin-1-yl)-2-((S)-1-methoxyethyl)pyridin-3-yl)-10,10-dimethyl-5,7-dioxo-11-(2,2,2-trifluoroethyl)-61,62,63,64,65,66-hexahydro-11H-8-oxa-2(4,2)-morpholina-1(5,3)-indola-6(1,3)-pyridazinacycloundecaphane-4-yl)acetamide

参考文献

1. Lingyan Jiang, et al. Cancer Res (2023) 83 (7_Supplement): 526.

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