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Crenolanib (CP-868596)670220-88-9

更新时间:2024-05-25

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厂商性质:经销商

生产地址:上海一基

简要描述:
Crenolanib (CP-868596)670220-88-9
上海一基实业有限公司是主要从事配套试剂的生产和销售的企业,产品用途:科研实验,标准对照品研究中心代理的作为一种衡量标准

Crenolanib (CP-868596)670220-88-9

Crenolanib (CP-868596)
分子式:C26H29N5O2分子量:443.54
 
产品描述
Crenolanib (CP-868596)是有效的,选择性PDGFRα/β抑制剂,Kd为2.1 nM/3.2 nM, 也有效抑制FLT3, 对D842V突变型而不是V561D突变型敏感, 作用于PDGFR比作用于c-Kit, VEGFR-2, TIE-2, FGFR-2, EGFR, erbB2, 和Src选择性高100倍以上。
靶点
PDGFRα
PDGFRα (D842V)
PDGFRα (purified)
PDGFRβ (purified)
   
IC50
11nM
10 nM
0.9 nM
1.8 nM
   
体外研究
Crenolanib is significantly more potent than imatinib in inhibiting the kinase activity of imatinib-resistant PDGFRα kinases (D842I, D842V, D842Y, D1842-843IM, and deletion I843). Crenolanib is 135-fold more otent than imatinib against D842V in the isogenic model system, with an IC50 of approximay 10 nM. Crenolanib inhibits the kinase activity of the fusion oncogene in EOL-1 cell line, which is derived from a patient with chronic eosinophilic leukemia and expresses the constitutively activated FIP1L1- PDGFRα fusion kinase, with IC50 = 21 nM. Crenolanib also inhibits the proliferation of EOL-1 cells with IC50 = 0.2 pM. Crenolanib inhibits the activation of V561D or D842V-mutant kinases expressed in BaF3 cells with IC50 with 85 nM or 272 nM, respectively. Crenolanib inhibits PDGFRα activation in H1703 non-small cell lung cancer cell line which has 24-fold amplification of the 4q12 region that contains the PDGFRα locus, with IC50 with 26 nM.Crenolanib is an orally bioavailable, highly potent and selective PDGFR TKI. Crenolanib is a benzimidazole compound that has IC50s of 0.9 nM and 1.8 nM for PDGFRA and PDGFRB, respectively.
体内研究
 
溶解性
DMSO 89 mg/mL,水 <1 mg/mL,乙醇 7 mg/mL
稳定性
2年 -20°C粉状,6月-80°C溶于DMSO

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