Chir-258
WebCHIR-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 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 …
Chir-258
Did you know?
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). http://kslegislature.org/li/b2015_16/measures/hcr5008/
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 (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.
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 ... 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...
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 …
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... how many blocks is a chunk in minecraftWebMay 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. high precision mandaluyong branchWebJan 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. … how many blocks is persona qWebAug 16, 2006 · CHIR-258 is a small-molecule inhibitor that targets multiple receptor tyrosine kinases, including VEGF receptor 2 and platelet-derived growth factor receptor (IC 50 … how many blocks is a mapWebApr 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. high precision maxicareWebFind chir and related products for scientific research at MilliporeSigma. US EN. Applications Products Services Support. Advanced Search ... (4-methyl-1-piperazinyl)-1H … high precision malolos bulacanWebNational 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. high precision mems 3-axis accelerometer