|1-(2-(5-(2-甲氧基乙氧基)-1H-苯并[d]咪唑-1-基)喹啉-8-基)哌啶-4-胺|CsnPharm

CAS No.: 343787-29-1

CP-673451 Catalog No. CSN16419

Synonyms: CP 673,451

CP-673451 is a selective inhibitor of PDGFRα/β with IC50 of 10 nM/1 nM in cell-free assays, exhibits > 450-fold selectivity over other angiogenic receptors, has antiangiogenic and antitumor activity.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

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 PDGFRα

IC50:10nM PDGFRβ

IC50:1nM
描述The activating mutations of KIT or PDGFRα are important to the pathogenesis of tumors. CP-673451 is a potent and selective inhibitor of PDGFRα and PDGFRβ with IC50 values of 10nM and 1nM, respectively, with more than 250-fold selectivity for PDGFRβthan c-kit kinase, 450-5000 fold than other angiogenic tyrosine kinases, including VEGFR-1, VEGFR-2, TIE-2 and FGFR-2 (measured by kinase inhibition assay). Treatment with CP-673451 at concentration of 3-100nM caused dose-dependent inhibition of p-PDGFR induced by PDGF-BB with IC50 value of 6.4nM in PAE-PDGFR-βcells. Oral dose of 3, 10 and 30mg/kg CP-673451 daily for 5 days inhibited PDGF-BB-induced angiogenesis by 70%, 81% and 95% in the sponge model, with no obvious inhibition of bFGF-and VEGF165-induced antiangiogenesis at dose of 5mg/kg. Dose-dependent decrease of p-PDGFR by CP-673451 can be observed in C6 tumors treated with CP-673451 at 33mg/kg and 100mg/kg in ex vivo study. Oral treatment with CP-673451 q.d. or b.i.d. for 10-11 days caused tumor growth inhibition in U87MG xenografts by 80% at dose of 100mg/kg, LS174T xenografts by 64% at 50mg/kg, H460 xenografts by 80% at 33mg/kg and Colo205 xenografts by 75% at 33mg/kg. Reduction of microvascular density up to 47% can be observed in tumors of Colo205-bearing mice dosed with 5mg/kg CP-673451 twice daily for 5 days. Combination of 33mg/kg CP-673451 once daily for 10 days with 10mg/kg Paclitaxel dosed once daily on days 1 to 5 caused tumor growth inhibition by 88%, compared with the agent alone by 49% or 54%, in mice bearing LS174T human colon adenocarcinoma xenografts^[1].
作用机制CP-673451 is an ATP-competitive inhibitor of PDGFR.^[1]
动物研究
剂量
Mice: 3 mg/kg - 100 mg/kg^[1] (p.o.)

给药途径
p.o.

动物研究
剂量	Mice: 3 mg/kg - 100 mg/kg^[1] (p.o.)
给药途径	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
- 2.3952 mL
- 11.9759 mL
- 23.9519 mL
- 5 mM
- 0.4790 mL
- 2.3952 mL
- 4.7904 mL
- 10 mM
- 0.2395 mL
- 1.1976 mL
- 2.3952 mL

技术信息

CAS号

343787-29-1

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C24H27N5O2

运输

蓝冰

分子量

417.50

别名

CP 673,451

溶解度

DMSO	400.0 mg/mL (958.1 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+40% PEG300+water	8 mg/mL	clear
PO	0.5% CMC-Na	18 mg/mL	suspension

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

靶点	Description	IC50
PDGFRα		IC50:10nM
PDGFRβ		IC50:1nM

CP-673451 Catalog No. CSN16419

靶点选择性

请登录您的专属账户

确认信息