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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-Ras-JMKX1899
JMKX1899

Chemical Structure : JMKX1899

CAS No.: 2633665-97-9

JMKX1899 (JMKX-1899)

货号: PC-27036Not For Human Use, Lab Use Only.

JMKX1899 is a potent and selective, covalent, BBB-penetrating KRAS G12C inhibitor.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

JMKX1899 is a potent and selective, covalent, BBB-penetrating KRAS G12C inhibitor.
JMKX1899 effectively and selectively inhibits cell growth in nearly all KRAS G12C-mutated cell lines but has no effect on non-KRAS G12C-mutated cell lines.
JMKX1899 (1 nM) significantly reduced the p-ERK/ ERK and p-AKT/ AKT ratio in the H358 cell line.
JMKX1899 inhibits tumor growth in vivo in KRAS G12C-mutant subcutaneous xenograft tumor models.
JMKX1899 can penetrate the CNS and achieve tumor regression in BM models.
JMKX1899 demonstrates profound antitumor activity in BM models compared to AMG510.

物理化学性质&存储条件

分子量 688.20
分子式 C36H39ClFN7O4
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

(2R,4aR)-3-acryloyl-11-chloro-6-(2-(dimethylamino)ethyl)-10-(2-fluoro-6-hydroxyphenyl)-8-(2-isopropyl-4-methylpyridin-3-yl)-2-methyl-2,3,4,4a,6,8-hexahydro-1H-pyrazino[1',2':4,5]pyrazino[2,3-c][1,8]naphthyridine-5,7-dione

参考文献

1. Danming He, et al. J Natl Cancer Cent. 2025 Dec 5;6(3):286-296.

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