[1-[2-[5-(3-甲基氧杂环丁烷-3-基甲氧基)苯并咪唑
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产品名称:[1-[2-[5-(3-甲基氧杂环丁烷-3-基甲氧基)苯并咪唑-1-基]喹啉-8-基]哌啶-4-基]胺CAS:670220-88-9别名：[1-[2-[5-(3-甲基氧杂环丁烷-3-基甲氧基)苯并咪唑-1-基]喹啉-8-基]哌啶-4-基]胺英文名：Crenolanib
- 生物活性Crenolanib (CP-868596)是一种有效的，选择性的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。
- 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 approximately 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.
