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|
|NCT02300545||Recruiting||Sarcoma, Soft Tissue|Soft Tissue Sarcoma||Washington University School of Medicine||April 8, 2015||Phase 2|
|NCT00674024||Completed||Neoplasms|Lymphoma||National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)||October 7, 2008||Phase 1|
|NCT01716416||Recruiting||Squamous Cell Carcinoma of the Head and Neck||Washington University School of Medicine||May 31, 2013||Phase 1|
|NCT01462630||Recruiting||Adult Angiosarcoma|Recurrent Adult Soft Tissue Sarcoma|Stage III Adult Soft Tissue Sarcoma|Stage IV Adult Soft Tissue Sarcoma||Fox Chase Cancer Center|National Cancer Institute (NCI)||November 3, 2011||Phase 2|
|NCT01468922||Completed||Sarcoma|Stomach Neoplasms|Neoplasms||National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)||October 24, 2011||Phase 1|
|NCT02342600||Not yet recruiting||Gastrointestinal Stromal Tumors||Sarcoma Alliance for Research through Collaboration|Novartis||January 2017||Phase 2|
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