WebCancer Res. Eritja N et al., 2014, Combinatorial therapy using dovitinib and ICI182.780 (fulvestrant) blocks tumoral activity of endometrial cancer cells., Mol Cancer Ther. Lim et al., 2016, Efficacy and safety of dovitinib in pretreated patients with advanced squamous non-small cell lung cancer with FGFR1 amplification: A single-arm, phase 2 ... WebJan 8, 2008 · To assess how many binding interactions may have been missed, we measured dissociation constants for sorafenib (Nexavar), VX-680/MK-0457, CHIR-258/TKI-258 and CHIR-265/RAF-265 against each...
CHIR258 MedChemExpress Life Science Reagents
WebApr 1, 2005 · CHIR-258 potently inhibits FGFR3 with an inhibitory concentration of 50% (IC50) of 5 nM in in vitro kinase assays and selectively inhibited the growth of B9 cells and human myeloma cell lines expressing wild-type (WT) or activated mutant FGFR3. In responsive cell lines, CHIR-258 induced cytostatic and cytotoxic effects. WebDovitinib (CHIR-258) is an orally active and potent receptor tyrosine kinase (RTK) inhibitor against class III (FLT3/KIT/PDGFR1/CSFR/PDGFR2 IC50 = 1/2/27/36/200 nM), class IV (FGFR1/3 IC50 = 8/9 nM), and class V (VEGFR1/2/3 IC50 = 10/13/8 nM) RTKs, but not INSR, EGFR1, ErbB2 or Raf (IC50 = 2.1, 2.2, >20, >25 μM, respectively). flora mcnichol
CHIR-258: A Potent Inhibitor of FLT3 Kinase in Experimental Tumor ...
WebDovitinib (TKI258; formerly CHIR-258) is an orally bioavailable inhibitor of multiple receptor tyrosine kinases. Interestingly, Dovitinib triggered a G2 /M arrest in cancer cell lines from diverse origins including HeLa, nasopharyngeal carcinoma, and hepatocellular carcinoma. WebCHIR-258 potently inhibits FGFR3 with an inhibitory concentration of 50% (IC50) of 5 nM in in vitro kinase assays and selectively inhibited the growth of B9 cells and human myeloma cell lines expressing wild-type (WT) or activated mutant FGFR3. In responsive cell lines, CHIR-258 induced cytostatic and cytotoxic effects. ... WebDovitinib, also known as TKI-258 or CHIR-258, is an orally bioavailable FGFR3 inhibitor. Dovitinib also induced caspase-dependent apoptosis in IM-9 cells without significant … great smoky mountains fs19 map