compound introduction
Crenolanib (CP-868596, ARO 002)是一种有效的，选择性PDGFRα/β抑制剂，在CHO细胞中Kd为2.1 nM/3.2 nM，也能有效抑制FLT3，对D842V突变型敏感对V561D突变型不敏感，作用于PDGFR比作用于c-Kit，VEGFR-2，TIE-2，FGFR-2，EGFR，erbB2，和Src的选择性高100倍以上。Crenolanib可辅助诱导线粒体自噬。 Crenolanib (CP-868596, ARO 002) is a potent and selective PDGFRα/β inhibitor with a Kd of 2.1 nM/3.2 nM in CHO cells. It can also effectively inhibit FLT3. It is sensitive to the D842V mutant and sensitive to the V561D mutant. It is not sensitive, and the selectivity for PDGFR is more than 100 times higher than that for c-Kit, VEGFR-2, TIE-2, FGFR-2, EGFR, erbB2, and Src. Crenolanib can help induce mitochondrial autophagy.
