纯度:>98% by HPLC;NMR (Conforms)
分子式:C30H28FN7O3
分子量:553.6
溶剂:DMSO (>25 mg/ml)
性状:White to off-white solid
存储:-20°C
Activity (short version):Bcl-Abl1 inhibitor
Function / Pharmacology:Rebastinib is a potent ABL1 kinase inhibitor (IC50 = 0.8 nM) that binds to amino acid residues that are used to switch between active and inactive conformations.1 It inhibits both phosphorylated and unphosphorylated ABL1 as well as gatekeeper mutant T315I (IC50 = 4 nM). Rebastinib was active against chronic myeloid leukemia Ba/F3 cells expressing BCR-ABL (IC50 = 19 nM) and BCR-ABLT315I (IC50 = 63 nM) and most kinase mutants.2 Rebastinib has been reported to inhibit the growth and metastasis of xenografted MDA-MB-231 triple-negative breast cancer cells by targeting AXL/MET.3 It has also been shown to be a potent inhibitor of Tie2 kinase (IC50 = 0.63 nM).4 Rebastinib blocked necroptosis via inhibition of RIPK1 and RIPK3.5