Catalog No.S3012 Synonyms: GW786034
Molecular Weight(MW): 437.52
Pazopanib 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 in cell-free assays, respectively.
Cited by 6 Publications
2 Customer Reviews
Three RCC cell lines treated with different concentrations of TKI and HDIL-2 and incubated for 48 h. Microscopic images show apoptotic materials 48 h following treatment (arrows show the apoptotic materials in the pazopanib-treated cells).
Expert Opin Pharmacother 2014 15(11), 1489-99. Pazopanib purchased from Selleck.
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2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
|Description||Pazopanib 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 in cell-free assays, respectively.|
Pazopanib potently inhibits VEGF-induced phosphorylation of VEGFR2 in HUVEC cells with IC50 of 8 nM.  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.  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 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. |
|In vitro||DMSO||87 mg/mL (198.84 mM) warming|
* 1 mg/ml means slightly soluble or insoluble.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02342600||Not yet recruiting||Gastrointestinal Stromal Tumors||Sarcoma Alliance for Research through Collaboration|Novartis||January 2017||Phase 2|
|NCT02810756||Not yet recruiting||Pharmacokinetics of Pazopanib||The Netherlands Cancer Institute||September 2016||Phase 0|
|NCT02348398||Not yet recruiting||Cervical Cancer||M.D. Anderson Cancer Center|GlaxoSmithKline||August 2016||Phase 2|
|NCT02795819||Recruiting||Renal Cell Carcinoma|Soft Tissue Sarcoma|Metastatic Disease||Virginia Commonwealth University|Arno Therapeutics|National Cancer Institute (NCI)||July 2016||Phase 1|
|NCT02691767||Not yet recruiting||Refractory Solid Tumors||Samsung Medical Center||May 2016||--|
|NCT02729194||Not yet recruiting||Carcinoma, Renal Cell||University of Michigan Cancer Center||April 2016||Phase 0|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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