Chir-258
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... WebAug 1, 2005 · Dovitinib, also known as TKI-258, is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that potently inhibits Class III (FLT3/c-Kit), Class IV (FGFR1/3), and Class V (VEGFR1-4) RTKs with...
Chir-258
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WebJun 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 … WebDovitinib lactate (TKI258 lactate) is a multi-targeted tyrosine kinase inhibitor with IC50 s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/3, VEGFR1/2/3 and PDGFRα/β, …
WebNov 16, 2005 · Background: CHIR-258 is an orally active small molecule receptor tyrosine kinase (RTK) inhibitor which exhibits potent single digit nanomolar inhibito Skip to Main … 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 ...
WebJul 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 …
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). hoffman sheffield sauseda \u0026 hoffmanWebCHIR258 related products. MedChemExpress provides thousands of inhibitors, modulators and agonists with high purity and quality, excellent customer reviews, precise and professional product citations, tech support and prompt delivery. hoffman sheila j phdWebJun 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 ... hoffmans homestyleWebNov 16, 2004 · Dovitinib (TKI258; formerly CHIR-258) is an orally bioavailable inhibitor of a number of RTKs [5]. It targets several members of the class III, IV and V RTK family, including vascular endothelial ... h\\u0026r block for s corporationWebApr 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 … hoffman shelfWebJan 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. … h\u0026r block fort atkinson wiWebJul 20, 2005 · CHIR-258 has ≤10 nmol/L activity against VEGF1/2/3 kinases, and our data clearly showed that CHIR-258 can inhibit autocrine VEGF levels in MV4;11 in vitro … hoffman shoes