Chir-258
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 … 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 ...
Chir-258
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WebJan 28, 2024 · EGFR-TKIs (Epidermal growth factor receptor tyrosine kinase inhibitors) is widely used in advanced non-small cell lung cancer (non-small cell lung cancer, NSCLC), especially in patients with lung adenocarcinoma with … 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...
WebFind chir and related products for scientific research at MilliporeSigma. US EN. Applications Products Services Support. Advanced Search ... (4-methyl-1-piperazinyl)-1H … WebJan 14, 2024 · Dovitinib is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/3, VEGFR1/2/3 and PDGFRα/β, respectively. Dovitinib potently inhibits the FGF-stimulated growth of WT and F384L-FGFR3-expressing B9 cells with IC50 values of 25 nM.
WebJan 5, 2011 · Safety of CHIR-258 (TKI258) in Advanced Solid Tumors The safety and scientific validity of this study is the responsibility of the study sponsor and investigators. … WebTitle: MC 258, Report of Nonpayment of Restitution Author: Michigan State Court Administrative Office Created Date: 9/11/2024 9:05:46 AM
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. ...
WebThis paper is a case history of the early stage chemical development of CHIR-258 (4-amino-5-fluoro-3- [6 (4-methyl-1-piperazinyl)-1H-benzimidazol-2-yl]-2 (1H)-quinolinone, DL-lactate salt), a... include\u0027does not name a typeWebJun 1, 2005 · Background: CHIR-258 is an orally active small molecule that exhibits potent inhibitory activity against multiple RTKs involved in tumor growth and angiogenesis (IC … include_bibliographyWebJun 20, 2006 · Methods: CHIR-258 was administered once daily in a dose-escalating phase 1 study to patients with relapsed/refractory MM. Drug tolerability and safety, pharmacokinetics (PK) and pharmacodynamics ... include_dirs cmakeWebCancer 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 ... include_directories $ cmake_source_dirWebJun 23, 2011 · This is a prospective, multi-center, open-label, single-arm, non-randomized, Phase II study to evaluate the efficacy and safety of TKI258 as second-line therapy in patients with either FGFR2 mutated or wild-type advanced and/or metastatic endometrial cancer. Study Design Go to Arms and Interventions Go to Outcome Measures Primary … inc. stockinc. stock holdersWebJul 15, 2005 · CHIR-258: a potent inhibitor of FLT3 kinase in experimental tumor xenograft models of human acute myelogenous leukemia. Our data indicate that CHIR-258 may be … inc. stock split