ACTB-1003 _FGFR 抑制剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEACTB-1003Cat. No.: HY-16025CAS No.: 939805-30-8分式: CHFNO分量: 591.53作靶点: FGFR; VEGFR作通路: Protein Tyrosine Kinase/RTK储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 35 mg/mL (59.17 mM)* means

2、soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.6905 mL 8.4527 mL 16.9053 mL5 mM 0.3381 mL 1.6905 mL 3.3811 mL10 mM 0.1691 mL 0.8453 mL 1.6905 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 ACTB-1003服可的激酶抑制剂，抑制 FGFR1，VEGFR2 和 Tie-2 的 IC50 值分

3、别为6，2 和 4 nM。IC50 & Target FGFR1 VEGFR2 Tie-26 nM (IC50) 2 nM (IC50) 4 nM (IC50)体外研究ACTB-1003 is an oral kinase inhibitor with multiple modes of action, targeting cancer mutations via FGFR1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEinhibition FGFR1 (IC50=6 nM), angiogenesis through inhibition o

4、f VEGFR2 (2 nM), Tie-2 (4 nM), and inducesapoptosis likely by targeting RSK (5 nM) and p70S6K (32 nM). ACTB-1003 is highly active with dose-dependent tumor growth inhibition in cell lines with FGFR genetic alterations - OPM2 human multiplemyeloma and the murine leukemia Ba/F3-TEL-FGFR1. OPM2 cells h

5、arbor the FGFR3 t(4:14) translocation,FGFR3 K650E mutation and PTEN deletion while the Ba/F3-TEL-FGFR1 cells are driven by FGFR1 over-expression 1.体内研究 ACTB-1003 is shown to inhibit tumor angiogenesis evident by the inhibition of CD31 staining in tumorsections. ACTB-1003 is combinable with 5-FU or p

6、aclitaxel without diminishing the activity or increasing thetoxicity of these chemotherapy agents in the HCT-116 colon tumor xenograft model 1.户使本产品发表的科研献 Science. 2017 Dec 1;358(6367).See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Patel K, et al. ACTB-1003: An oral kinase inhibitor targeting cancer mutations (FGFR), angiogenesis (VEGFR2, TEK), and induction ofapoptosis (RSK and p70S6K). Journal of Clinical Oncology 28, no. 15 DOI: 10.1200/jco.2010.28.15_suppl.e13665McePdfHeightCaution: Product has not been fully validated for medical applications.For research use on