中文名：Pazopanib HCl (GW786034 HCl)
英文名：Pazopanib HCl (GW786034 HCl)
英文別名：5-(4-((2,3-dimethyl-2H-indazol-6-yl)(methyl)amino)pyrimidin-2-ylamino)-2-methylbenzenesulfonamide hydrochloride
純度：10mM in DMSO
貨號：P409237
包裝：1ml
Cas號：635702-64-6
存儲溫度：-80℃儲存
產(chǎn)品介紹：
Information
Pazopanib HCl (GW786034 HCl) is a novel multi-target inhibitor ofVEGFR1,VEGFR2,VEGFR3, PDGFR, FGFR, c-Kit and c-Fms withIC50of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces autophagic Type II cel
In?vitro
Pazopanib potently inhibits VEGF-induced phosphorylation of VEGFR2 in HUVEC cells with IC50 of 8 nM. Pazopanib 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\u2009μg/mL of Pazopanib and is completely abolished at 5\u2009μg/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. Pazopanib between 20 m g/mL and 22.5 m g/mL shows an increasing reduction of RPE cell viability.
In?vivo
The mice treated with 30 mg/kg or 100\u2009mg/kg Pazopanib reveals a significant decrease in tumor burden compared with the mice treated with vehicle or 10\u2009mg/kg Pazopanib. Treatment with Pazopanib is well-tolerated and there is no significant difference in the body weight among the mice in each group.
Cell?Data
cell?lines：
Concentrations：0-10 μM
Incubation?Time：1 hour
Powder?Purity:≥99%
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關(guān)鍵字： 5-(4-((2,3-dimethyl-2H-indazol-6-yl)(methyl)amino)pyrimidin-2-ylamino)-2-methylbenzenesulfonamide hydrochloride
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