Pexidartinib抑制剂、激动剂(CAS号1029044-16-3)Pexidartinib(PLX-3397)是受体酪氨酸激酶Fms,Kit和Flt3小分子抑制剂,临床2期。 Pexidartinib(PLX-3397) is a small-molecule receptor tyrosine kinase (RTK) inhibitor of KIT, CSF1R and FLT3 with potential antineoplastic activity.
IC50 value: 28/16 nM(Fms/Kit)
Target: multikinase inhibitor
Multitargeted tyrosine kinase inhibitor PLX3397 binds to and inhibits phosphorylation of stem cell factor receptor (KIT), colony-stimulating factor-1 receptor (CSF1R) and FMS-like tyrosine kinase 3 (FLT3), which may result in the inhibition of tumor cell proliferation and down-modulation of macrophages, osteoclasts and mast cells involved in the osteolytic metastatic disease. FLT3, CSF1R and FLT3 are overexpressed or mutated in many cancer cell types and play major roles in tumor cell proliferation and metastasis.