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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-Raf-GNE-9815
GNE-9815

Chemical Structure : GNE-9815

CAS No.: 2729996-45-4

GNE-9815 (GNE9815)

货号: PC-72469Not For Human Use, Lab Use Only.

GNE-9815 (GNE9815) is a potent, selective, oral Type II pan-RAF inhibitor with Ki of 0.062 and 0.19 nM for CRAF and BRAF, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GNE-9815 (GNE9815) is a potent, selective, oral Type II pan-RAF inhibitor with Ki of 0.062 and 0.19 nM for CRAF and BRAF, respectively.
GNE-9815 displays clean kinase selectivity against a panel of 223 kinases (no inhibition > 70% at a concentration of 0.1 μM) besides RAF kinases).
GNE-9815 demonstrates synergistic activity in KRAS mutant A549 and HCT116 cancer cells in combination with the MEK inhibitor cobimetinib.
GNE-9815 in combination with the MEK inhibitor cobimetinib demonstrated synergistic MAPK pathway modulation in an HCT116 xenograft mouse model.

 

物理化学性质&存储条件

分子量 455.493
分子式 C26H22FN5O2
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

3-(2-cyanopropan-2-yl)-N-(2-fluoro-4-methyl-5-(7-methyl-8-oxo-7,8-dihydropyrido[2,3-d]pyridazin-3-yl)phenyl)benzamide

参考文献

1. Malcolm P Huestis, et al. ACS Med Chem Lett. 2021 Apr 21;12(5):791-797.

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