产品
编 号:F611957
分子式:C19H17F2N5OS
分子量:401.43
产品类型
结构图
CAS No: 639858-32-5
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产品详情
生物活性:
BMS-605541 is a selective and orally active inhibitor of VEGFR-2 kinase with an IC50 value of 23 nM and Ki value of 49 nM. BMS-605541 inhibits the activity of Flk-1, VEGFR-1 and PDGFR-β with IC50 values of 40 nM, 400 nM and 200 nM, respectively. BMS-605541 can be used for cancer research.
体内研究:
BMS-605541 (12.5-180 mg/kg;一天 1 次或一天 2 次,持续 14 天) 对皮下植入 L2987 和 HCT-116 异种移植物的无胸腺小鼠具有抗肿瘤活性。BMS-605541 的药代动力学 (PK) 参数SpeciesAdministration mannerDose (mg/kg)Cmax (μM)Tmax (h)AUC (μM?h)T1/2 (h)MRT (h)Cl (mL/min?kg)Vss (L/kg) Fpo (%)
MouseOral gavage901480.5649 (0-24 h)1.73.4100
MouseIntravenous injection10 11.81.7100
RatOral gavage5044.02.02022.23.5100
RatIntravenous injection10 13.61.1100
CynoOral gavage58.00.7528.57.17.952
CynoIntravenous injection1 3.91.652
体外研究:
BMS-605541 (Compound 14) 通过 VEGF 抑制 HUVECs 的生长,IC50 值为 25 nM。