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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-Ras-AMG410
AMG410

Chemical Structure : AMG410

CAS No.: 3040175-17-2

AMG410 (AMG-410)

货号: PC-24662Not For Human Use, Lab Use Only.

AMG410 is a potent, non-covalent and selective pan-KRAS inhibitor with IC50 values of 1-4 nM for KRAS G12D, KRAS G12V, and KRAS G13D,> 100-fold selectivity against both HRAS and NRAS.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

AMG410 is a potent, non-covalent and selective pan-KRAS inhibitor with IC50 values of 1-4 nM for KRAS G12D, KRAS G12V, and KRAS G13D,> 100-fold selectivity against both HRAS and NRAS.
AMG 410 is a dual GTP(on)- and GDP(off)-state inhibitor (KD(GDP-state) = 1 nM; KD(GTP-state) = 22 nM), enabling blockade of KRAS signaling in a cycling state-independent manner.
AMG410 blocks KRAS signaling in a cycling state-independent manner and also blocks proliferation in wildtype KRAS-amplified tumor cells.
AMG 410 shows potent antiproliferative activity in KRAS-mutant cells (median IC50 = 12 nM), with no anti-proliferative effects in non-KRAS-transformed cells (median IC50 >5 µM).

物理化学性质&存储条件

分子量 656.09
分子式 C31H32ClF2N7O5
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

FC=1C=2C=3C4=C(C=C(Cl)C3CCCOC(=O)O[C@]5(CN(C=6C(C1N=C(OC[C@@]78N(C[C@H](F)C7)CCC8)N6)=CN2)CCOC5)[H])NN=C4

参考文献

1. Patent WO2024107686A1.

2. AACR Annual Meeting: April 25-30, 2025

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