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. ... 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 ...
Maryon Hardie
WebJun 20, 2006 · 17502. Background: CHIR-258 is an orally active small molecule receptor tyrosine kinase (RTK) inhibitor which has potent activity against multiple RTKs involved in tumor growth and angiogenesis (IC50 ≤13 nM for FGFR, VEGFR, PDGFR, C-KIT, and FLT3). Approximately 15% of newly diagnosed MM patients harbor a t(4;14) … flanged hex screw
Phase I trial of chir-258 in multiple myeloma Request PDF
WebMay 15, 2005 · CHIR-258 exhibits properties that make it a promising candidate for clinical develop … These studies provide evidence that biological activity of CHIR-258 in tumors correlates with efficacy and aids in the identification of potential biomarkers of this multitargeted receptor tyrosine kinase inhibitor. WebIn addition, CHIR-258 potently inhibited class IV (FGFR1 and 3) and class V (VEGFR1-4) RTKs with IC50 values of 0.008 to 0.013 mM. For insulin receptor, EGFR, c-Met, EphrinA2, Tie2, IGFR1, and HER2 significant inhibition was observed only at more than 10-fold higher concentrations. These studies demonstrated that CHIR-258 is a selective but ... WebDovitinib (CHIR-258; 10-60 mg/kg/day; gavage; for 21 days) has a significant antitumor effect [1]. Dovitinib (50 and 75 mg/kg) results in 97% and 98% tumor growth inhibition, respectively, and the maximal efficacy … flanged housing