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FRAX1036

品牌
Sigma-Aldrich
CAS
1432908-05-8
货号
SML2618
规格纯度
≥98% (HPLC)
价格
1168.11 *本价格含增值税费
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半岛bd体育手机客户端 名称:
1432908-05-8
FRAX1036
6-[2-Chloro-4-(6-methyl-2-pyrazinyl)phenyl]-8-ethyl-2-[[2-(1-methyl-4-piperidinyl)ethyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one
6-(2-Chloro-4-(6-methylpyrazin-2-yl)phenyl)-8-ethyl-2-((2-(1-methylpiperidin-4-yl)ethyl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one
FRAX-1036
FRAX 1036
半岛bd体育手机客户端 介绍:

半岛bd体育手机客户端 说明

生化/生理作用

FRAX1036 is a potent, group I-selective p21-activated kinase (PAK) inhibitor (PAK1/4 Ki = 23 nM/1.4 μM; PAK1/4 IC50 = 2 nM/>500 nM; >96% PAK1/2/3 inhibition vs. 5.1%/8.2%/22.2% PAK4/5/6 inhibition at 1 μM) with significant inhibitory activity toward only 11 other kinases at a high concentration of 1 μM (78.7-100% inhibition) among a panel of 240. FRAX1036 exhibits higher antiproliferation activity in PAK negative regulator NF2-deficient meningioma cultures (NF2-/- Ben-Men-1/KT21-MG1 IC50 = 1.888/1.991 μM vs.NF2+/+ MN328/MN525 IC50 = 4.239/3.296 μM) by inhibiting cellular PAK autophosphorylation and downstream signaling events. When administered orally in a murine orthotopic meningioma model, FRAX1036 effectively suppresses the growth of established KT21 and Ben-Men tumorsin vivo(30 mg/kg/d p.o.).

基本信息

经验(实验)分子式 C28H32ClN7O
分子量 518.05
MDL编号 MFCD30187513

半岛bd体育手机客户端 性质

测定 ≥98% (HPLC)
形式 powder
颜色 white to beige
溶解性 DMSO: 2 mg/mL, clear
储存温度 ?20℃

安全信息

储存分类代码 11 - Combustible Solids
WGK WGK 3
闪点(F) Not applicable
闪点(C) Not applicable

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