Ningetinib-Tosylate _TAM Receptor 抑制劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemENingetinib TosylateCat. No.: HY-107145CAS No.: 1394820-77-9分式: CHFNOS分量: 728.79作靶點(diǎn): TAM Receptor; VEGFR; c-Met/HGFR作通路: Protein Tyrosine Kinase/RTK儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) D

2、MSO : 8.25 mg/mL (11.32 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 1.3721 mL 6.8607 mL 13.7214 mL5 mM 0.2744 mL 1.3721 mL 2.7443 mL10 mM 0.1372 mL 0.6861 mL 1.3721 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Ningetinib Tosylate種有效的服物可的

3、分酪氨酸激酶抑制劑 (TKI)，對(duì) c-Met，VEGFR-2 和 Axl的 IC50 值分別為 6.7, 1.9 和 1.0 nM。IC50 & Target VEGFR21.9 nM (IC50)體外研究Ningetinib Tosylate is a potent, orally bioavailable small molecule tyrosine kinase inhibitor (TKI) with IC50s of1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE6.7, 1.9 and 50 values of 8.6 and

4、6.3 nM, respectively 1.體內(nèi)研究 When single dosed orally (3 mg/kg) to U87MG tumor-bearing nude mice, Ningetinib Tosylate (CT053PTSA)potently inhibits the phosphorylation of c-Met and its downstream signaling kinases AKT and ERK1/2 for upto 6 hours in tumor tissues. In orthotopic U87MG human glioblastoma

5、 xenograft model, Ningetinib Tosylateprolongs the median survival time (MST) and yields significant increase in life-span value (ILS=32%,p=0.003) at an oral dose of 20 mg/kg/day (dosed 21 days) versus the vehicle-treated group 1.REFERENCES1. Ning Xi, et al. Abstract 1755: CT053PTSA, a novel c-MET and VEGFR2 inhibitor, potently suppresses angiogenesis and tumor growth.Cancer Res 2014;74(19 Suppl):Abstract nr 1755.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-820-379