AMG410 (AMG-410, AMG 410)

Chemical Structure : AMG410

CAS No.: 3040175-17-2

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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.

规格	价格	库存
1 mg	￥1980	In stock
5 mg	￥3980	In stock
10 mg	￥5980	In stock
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

AMG410 (AMG-410, AMG 410) 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	(16S)-36-Chloro-28-fluoro-22-(((2R,7aS)-2-fluorotetrahydro-1H-pyrrolizin-7a(5H)-yl)methoxy)-31H-7,9-dioxa-1(4,6)-oxazepana-2(4,7)-pyrido[4,3-d]pyrimidina-3(4,5)-indazolacyclononaphan-8-one

参考文献

1. Patent WO2024107686A1.

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