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CAS No.: 1286739-19-2

FRAX597 Catalog No. CSN15824

Synonyms: FRAX597

FRAX597, a small-molecule pyridopyrimidinone, is a potent and ATP competitive inhibitor of the group I PAKs (PAK1 IC50= 8 nM, PAK2 IC50= 13 nM, PAK3 IC50= 19 nM).

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 PAK1

IC50:8nM PAK2

IC50:13nM PAK3

IC50:19nM
描述The family of serine/threonine p21-activating kinases, known as PAK proteins, are critical effectors that link Rho GTPases to cytoskeleton reorganization and nuclear signaling, and they serve as targets for the small GTP binding proteins Cdc42 and Rac. PAK proteins involve in intracellular signaling pathways downstream of integrins and receptor-type kinases. This family of proteins play an important role in cytoskeleton dynamics, in cell adhesion, migration, proliferation, apoptosis, mitosis, and in vesicle-mediated transport processes. FRAX597 is a group Ⅰ PAK inhibitor. Based on enzymatic assays, the inhibitory IC50 values of FRAX597 against group Ⅰ PAK members PAK1, PAK2 and PAK3 are 7.7 nM, 12.8 nM and 19.3 nM, respectively^[3].When Nf2-null SC4 Schwann cells were treated with 1 μM FRAX597 for a period of 96h, it was shown that FRAX597 dramatically impaired cell proliferation from the 48h time point^[3]. In a cell cycle analysis, results show that FRAX597 blocked the cell cycle in G1 phase. However, the absence of a sub-G1 population suggested that FRAX597 did not impact cell viability.In an orthotopic model of schwannomas established by injection of luciferase-tagged schwannoma cells into a myelinated nerve, oral administration of FRAX597 at the dose of 100 mg/kg once daily, starting from 10 days post tumor cell implantation and lasting for a period of 14 days, significantly slowed down tumor growth rate. FRAX597-treated cohort showed significantly lower average tumor weight compared with control at the end point of the experiment^[3].
作用机制Structural assay revealed that FRAX597 inhibited PAK1 kinase by occupying the ATP binding site. In details, a phenyl ring that traverses the gatekeeper residue and positions the thiazole in the back cavity of the ATP binding site, a site rarely targeted by kinase inhibitors, was characterized in the FRAX597/PAK1 complex^[3].
动物研究
剂量
Mice: 3 mg/kg^[3] (i.p.), 20 mg/kg - 90 mg/kg^[4] (p.o.)

给药途径
i.p., p.o.

动物研究
剂量	Mice: 3 mg/kg^[3] (i.p.), 20 mg/kg - 90 mg/kg^[4] (p.o.)
给药途径	i.p., p.o.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.7918 mL
- 8.9590 mL
- 17.9180 mL
- 5 mM
- 0.3584 mL
- 1.7918 mL
- 3.5836 mL
- 10 mM
- 0.1792 mL
- 0.8959 mL
- 1.7918 mL

技术信息

CAS号

1286739-19-2

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C29H28ClN7OS

运输

蓝冰

分子量

558.10

别名

FRAX597

溶解度

DMSO	25.0 mg/mL (44.8 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+water	0.5 mg/mL	clear
PO	0.5% CMC-Na	30 mg/mL	suspension

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靶点	Description	IC50
PAK1		IC50:8nM
PAK2		IC50:13nM
PAK3		IC50:19nM

FRAX597 Catalog No. CSN15824

靶点选择性

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