Pazopanib HCl (GW786034 HCl)
For research use only.
Molecular Weight(MW): 473.98
Pazopanib HCl (GW786034 HCl) 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 induces autophagic Type II cell death.
Selleck's Pazopanib HCl (GW786034 HCl) has been cited by 18 publications
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IC50 of Pazopanib that block ANDV-induced EC permeability. Endothelial cells were ANDV infected, and 3 days postinfection the permeability of cells in response to VEGF addition was determined in the presence or absence of increasing amounts of kinase inhibitor. (B): VEGFR2-Src inhibitors block ANDV-induced permeability. Endothelial cells were plated on vitronectin-coated Transwell inserts and infected at an MOI of 0.5 in triplicate with ANDV. Three days postinfection, the permeability of ANDV- and mock-infected endothelial cell monolayers was determined at indicated times in the presence or absence of Pazopanib.
J Virol, 2011, 85(5): 2296-303. Pazopanib HCl (GW786034 HCl) purchased from Selleck.
Effect of HDIL-2/TKI on apoptosis of RCC cells. Three RCC cell lines treated with different concentrations of Pazopanib 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 HCl (GW786034 HCl) purchased from Selleck.
MRC5 non-transformed human lung fibroblasts were infected with influenza viruses (100 multiplicity of infection). Two hours after infection the cells were treated with vehicle control; sorafenib tosylate (2mM); pazopanib (2mM); OSU-03012 (2mM); and AR-13 (2mM). Twenty-four hours after infection the cells are treated with live/dead agent where green cells are viable and cells staining yellow or red are considered dead. Cells are examined at 10 magnification in a Hermes wide-field microscope (n¼3 SEM) P<0.05 less than vehicle control level of virus-mediated cell killing.
J Cell Physiol, 2016, 231(10):2286-302.. Pazopanib HCl (GW786034 HCl) purchased from Selleck.
Purity & Quality Control
Choose Selective VEGFR Inhibitors
|Description||Pazopanib HCl (GW786034 HCl) 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 induces autophagic Type II cell death.|
|Features||A multi-kinase inhibitor.|
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 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. |
Kinase enzyme assays:VEGFR enzyme assays for VEGGR1, VEGFR2, and VEGFR3 are run in homogeneous time-resolved fluorescence (HTRF) format in 384-well microtiter plates using a purified, baculovirus-expressed glutathione-S-transferase (GST) fusion protein encoding the catalytic c-terminus of human VEGFR receptor kinases 1, 2, or 3. Reactions are initiated by the addition of 10 μL of activated VEGFR2 kinase solution [final concentration, 1 nM enzyme in 0.1 M HEPES, pH 7.5, containing 0.1 mg/mL bovine serum albumin (BSA), 300 μM dithiothreitol (DTT)] to 10 μL substrate solution [final concentration, 360 nM peptide, (biotin-aminohexyl-EEEEYFELVAKKKK-NH2), 75 μM ATP, 10 μM MgCl2], and 1 μL of titrated Pazopanib in DMSO. Plates are incubated at room temperature for 60 min, and then the reaction is quenched by the addition of 20 μL of 100 mM ethylene diamine tetraacetic acid (EDTA). After quenching, 20 μL HTRF reagents (final concentration, 15 nM Streptavidin-linked allophycocyanin, 1 nM Europium-labeled antiphosphotyrosine antibody diluted in 0.1 mg/mL BSA, 0.1 M HEPES, pH 7.5) is added and the plates incubated for a minimum of 10 min. The fluorescence at 665 nM is measured with a Wallac Victor plate reader using a time delay of 50 μs.
|In vitro||DMSO||17 mg/mL (35.86 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation ()|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Molecular Weight Calculator
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03735758||Recruiting||Drug: pazopanib or guideline conform chemotherapy||Soft Tissue Sarcoma Adult||GWT-TUD GmbH||November 2 2018||Phase 4|
|NCT03334409||Recruiting||Drug: Ascorbic Acid|Drug: Pazopanib Hydrochloride||Clear Cell Renal Cell Carcinoma|Metastatic Clear Cell Renal Cell Carcinoma|Stage III Renal Cell Cancer AJCC v8|Stage IV Renal Cell Cancer AJCC v7|Unresectable Renal Cell Carcinoma||Academic and Community Cancer Research United|National Cancer Institute (NCI)||February 16 2018||Phase 2|
|NCT03149120||Withdrawn||Biological: Nivolumab|Drug: Pazopanib||Soft Tissue Sarcomas||NYU Langone Health|Bristol-Myers Squibb||August 2017||Phase 2|
|NCT03091465||Completed||--||Metastatic Renal Cell Carcinoma||Spanish Oncology Genito-Urinary Group||December 20 2016||--|
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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