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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-p21-activated Kinase (PAK)-FRAX486
FRAX486

Chemical Structure : FRAX486

CAS No.: 1232030-35-1

FRAX486 (FRAX-486)

货号: PC-73199Not For Human Use, Lab Use Only.

FRAX486 is potent, selective, brain-penetrant group I PAKs inhibitor with IC50 of 8.25, 39.5, and 55.3 nM for PAK1, PAK2 and PAK3, respectively.

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10 mg ¥880 In stock
25 mg ¥1480 In stock
50 mg ¥2480 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

FRAX486 is potent, selective, brain-penetrant group I PAKs inhibitor with IC50 of 8.25, 39.5, and 55.3 nM for PAK1, PAK2 and PAK3, respectively.
FRAX486 poorly inhibits group II PAK (PAK4) with IC50 of 779 nM.
FRAX486 rescued increased density of apical dendritic spines, reversed hyperactivity and repetitive behaviors in Fmr1 KO mice.
FRAX486 ameliorateed adolescent synapse loss in the prefrontal cortex and adult behavior change in a DISC1 knockdown mouse model.
FRAX486 combined with midostaurin significantly prolonged leukemia progression-free survival in FLT3 D835H PDX-ALL model.

物理化学性质&存储条件

分子量 513.4
分子式 C25H23Cl2FN6O
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

6-(2,4-Dichlorophenyl)-8-ethyl-2-[[3-fluoro-4-(1-piperazinyl)phenyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one

参考文献

1. Hayashi-Takagi A, et al. Proc Natl Acad Sci U S A. 2014 Apr 29;111(17):6461-6.

2. Dolan BM, et al. Proc Natl Acad Sci U S A. 2013 Apr 2;110(14):5671-6.

3. Wang Y, et al. PLoS One. 2016 Apr 12;11(4):e0153312.

4. Siekmann IK, et al. Blood Adv. 2018 Oct 9;2(19):2554-2567.

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