纯度:98% by HPLC;NMR (Conforms)
分子式:C33H29F2N5O4S
分子量:629.68
溶剂:DMSO (>25 mg/ml) Ethanol (>25 mg/ml)
性状:Off-white solid
存储:-20°C
Activity (short version):Multikinase inhibitor / Immuno-oncology agent
Function / Pharmacology:Sitravatinib is a broad spectrum receptor tyrosine kinase inhibitor. Its targets include Axl, c-Met, PDGFR, VEGFR, Ephrin receptor family, and FLT3 among others at nanomolar levels.1 Sitravatinib has been tested in mouse models of sarcoma and showed better efficacy than both imatinib and crizotinib. Because of its unique kinase inhibition profile (especially that of TAM receptors), it has been used to restore response to anti-PD-1 therapy (nivolumab) in NSCLC patients.2 Sitravatinib was able to significantly alter the immunosuppressive tumor microenvironment in three preclinical tumor models to enhance the effects of PD-1 blockade therapy.3