Chir-258
WebJan 9, 2024 · Date Chamber Status AR JPN; Tue, Mar 22, 2016: House: Enrolled on Tuesday, March 22, 2016 2394 WebCHIR-258 (TKI-258,Dovitinib) Molecular Weight: 500.5. Parent Compound: CID 135743690 (5-fluoro-4-imino-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one) …
Chir-258
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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... 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...
WebNov 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 ... WebNov 16, 2005 · Download Citation CHIR-258 Efficacy in a Newly Developed Preclinical Bone Marrow Model of t(4;14) Multiple Myeloma. Multiple myeloma (MM) remains a fatal hematological malignancy due to the ...
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. WebJul 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 …
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). note for the employerWebJun 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 … note for the loss of a fatherWebApr 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. how to set favourite bar in edgeWebDovitinib (TKI-258/CHIR-258) is a pan receptor tyrosine kinase (RTK) inhibitor that targets VEGFR, FGFR, PDGFR, and KIT. It has shown efficacy in mouse-model of PCa bone metastasis, and is presently in clinical trials for several cancers. note for the loss of a motherWebNational Center for Biotechnology Information. 8600 Rockville Pike, Bethesda, MD, 20894 USA. Contact. Policies. FOIA. HHS Vulnerability Disclosure. National Library of Medicine. National Institutes of Health. Department of Health and Human Services. note for todayWebDovitinib (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 … how to set fax machineWebCHIR-258, a novel, multitargeted tyrosine kinase inhibitor for the potential treatment of t(4;14) multiple myeloma. Blood. 2005 Apr 1;105(7):2941-8. Epub 2004 Dec 14. PubMed ID note for the loss of a daughter