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FRAX1036
产品别名
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
结构式
基本信息
| Empirical Formula【经验(实验)分子式】 | C28H32ClN7O |
| Molecular weight | 518.05 |
| MDL number | MFCD30187513 |
| Biochem/physiol Actions【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 tumors in vivo (30 mg/kg/d p.o.). |
产品性质
| Assay【测定】 | ≥98% (HPLC) |
| form【形式】 | powder |
| color【颜色】 | white to beige |
| solubility【溶解性】 | DMSO: 2 mg/mL, clear |
| storage temp.【储存温度】 | −20℃ |
安全信息
| Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
| WGK | WGK 3 |
