货号: | ONI-171793 |
CAS号: | 635702-64-6 |
供应商: | 美国 |
数量: | 1292.0 |
英文名: | GW-786034,GW786034,GW 786034 |
保质期: | 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO |
保存条件: | 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO |
规格: | (5mg/100mg/842mg) |
Pazopanib Hcl (GW-786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM, respectively. IC50 value: 10/30/47/84/74/140/146 nM (pan VEGFR1/2/3/PDGFR/FGFR/c-Kit/c-Fms) [1] Target: VEGFR/PDGFR/VEGFR/CSF1R in vitro: Pazopanib potently inhibits VEGF-induced phosphorylation of VEGFR2 in HUVEC cells with IC50 of 8 nM [1]. PPazopanib shows dose-dependent growth inhibition in all synovial sarcoma cell lines including SYO-1 and HS-SY-II cells. Proliferation of SYO-1 and HS-SY-II cells is inhibited even at 1 μg/mL of Pazopanib and is completely abolished at 5 μg/mL. Pazopanib induces G1 arrest, and thereby suppresses the growth of synovial sarcoma cells. Phosphorylation of Akts, GSK-3β, JNKs, p70 S6 Kinase, and mTOR is suppressed in Pazopanib-treated SYO-1 cells compared with that in the vehicle-treated cells [2]. Pazopanib between 20 m g/mL and 22.5 m g/mL shows an increasing reduction of RPE cell viability [3]. in vivo: The mice treated with 30 mg/kg or 100 mg/kg Pazopanib reveals a significant decrease in tumor burden compared with the mice treated with vehicle or 10 mg/kg Pazopanib. Treatment with Pazopanib is well-tolerated and there is no significant difference in the body weight among the mice in each group [2].
温馨提示:不可用于临床治疗。