Pazopanib HCl (GW786034 HCl)

Pazopanib (GW786034) 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.

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Pazopanib HCl (GW786034 HCl) Chemical Structure

Pazopanib HCl (GW786034 HCl) Chemical Structure
Molecular Weight: 473.98

Validation & Quality Control

Customer Reviews(2)

Quality Control & MSDS

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    Combination Therapy

Product Description

Biological Activity

Description Pazopanib (GW786034) 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.
Targets VEGFR1 [1] VEGFR2 [1] VEGFR3 [1] FGFR [1] PDGFR [1]

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IC50 10 nM 30 nM 47 nM 74 nM 84 nM
In vitro Pazopanib potently inhibits VEGF-induced phosphorylation of VEGFR2 in HUVEC cells with IC50 of 8 nM. [1] 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. [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]
Features A multi-kinase inhibitor.

Protocol(Only for Reference)

Kinase Assay:

[1]

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.

Cell Assay:

[1]

Cell lines HUVEC cells
Concentrations 0-10 μM
Incubation Time 1 hour
Method

Phosphorylation of VEGFR2 is assessed in HUVEC stimulated with VEGF. HUVEC are plated in type-I collagen-coated 10 cm plates in Clonetics EGM-MV medium at 1.0-1.5 × 106 cells/plate. After 24 hours, the confluent cells are serum starved overnight by replacing the growth medium with Clonetics EBM medium containing 0.1% BSA, 500 μg/mL hydrocortisone. Cells are treated with Pazopanib at various concentrations for 1 hour, followed by addition of 10 ng/mL VEGF or vehicle for 10 min. Cells are solubilized in lysis buffer. VEGFR2 is immunoprecipitated using antiflk-1 antibody and analyzed by sodium dodecyl sulfate polyacrylamide gel electrophoresis (SDS-PAGE) followed by Western blotting and detection with antiflk-1 or with antiphosphotyrosine (anti-P-tyr-biotin) antibody. The VEGFR2 phosphorylation level is quantified by densitometry and normalized to the total VEGFR2 level.

Animal Study:

[2]

Animal Models Immunodeficient mice bearing SYO-1 cells
Formulation
Dosages 0 mg/kg, 10 mg/kg, 30 mg/kg, or 100 mg/kg
Administration Oral administration
Solubility 30% PEG400/0.5% Tween80/5% propylene glycol, , 30 mg/mL
* 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.
1

References

[1] Harris PA, et al. J Med Chem. 2008, 51(15), 4632-4640.

[2] Hosaka S, et al. J Orthop Res. 2012.

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Clinical Trial Information( data from http://clinicaltrials.gov)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT01684397 Recruiting Clear Cell Renal Cell Carcinoma|Stage IV Renal Cell Cancer Roswell Park Cancer Institute|National Cancer Institute (NCI)|GlaxoSmithKline 2012-10 Phase 1|Phase 2
NCT01713972 Recruiting Unspecified Adult Solid Tumor, Protocol Specific Ohio State University Comprehensive Cancer Center|Manisha Shah|National Comprehensive Cancer Network 2012-11 Phase 1
NCT01767636 Recruiting Recurrent Renal Cell Cancer|Stage IV Renal Cell Cancer|Type 1 Papillary Renal Cell Carcinoma|Type 2 Papillary Renal Cell Carcinoma Mayo Clinic 2013-05 Phase 2
NCT01716416 Recruiting Squamous Cell Carcinoma of the Head and Neck Washington University School of Medicine 2013-05 Phase 1
NCT01841736 Recruiting Metastatic Gastrointestinal Carcinoid Tumor|Pulmonary Carcinoid Tumor|Recurrent Gastrointestinal Carcinoid Tumor|Recurrent Neuroendocrine Carcinoma of the Skin|Regional Gastrointestinal Carcinoid Tumor|Stage III Neuroendocrine Carcinoma of the Skin|Stage IV Neuroendocrine Carcinoma of the Skin|Thyroid Gland Medullary Carcinoma National Cancer Institute (NCI) 2013-06 Phase 2

Chemical Information

Download Pazopanib HCl (GW786034 HCl) SDF
Molecular Weight (MW) 473.98
Formula

C21H23N7O2S.HCl

CAS No. 635702-64-6
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Synonyms
Solubility (25°C) * In vitro DMSO 17 mg/mL (35 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 30% PEG400/0.5% Tween80/5% propylene glycol, 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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.
Chemical Name 5-(4-((2,3-dimethyl-2H-indazol-6-yl)(methyl)amino)pyrimidin-2-ylamino)-2-methylbenzenesulfonamide hydrochloride

Research Area

Customer Reviews (2)


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Rating
Source J Virol 2011 85, 2296–2303. Pazopanib HCl (GW786034 HCl) purchased from Selleck
Method Endothelial cell permeability assay
Cell Lines Endothelial cell
Concentrations 0-100 nM
Incubation Time 15-60 min
Results Figure A defines concentrations of kinase inhibitors which block ANDV-induced EC permeability approximately 50% (IC50s).The IC50s of pazopanib is 100 nM. we assessed the abilities of VEGFR2 and SFK inhibitors to block ANDV-induced permeability at their IC50s from 15 to 60 min after VEGF addition. The VEGFR2 kinase inhibitor pazopanib inhibited ANDV-induced permeability by 40 to 60% at nanomolar IC50 levels (Figure B).

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Rating
Source J Virol 2011 85, 2296–2303. Pazopanib HCl (GW786034 HCl) purchased from Selleck
Method VE-cadherin internalization
Cell Lines endothelial cell
Concentrations 100 nM
Incubation Time 15 min
Results We found that dasatinib and pazopanib inhibited ANDV-induced VE-cadherin internalization 65 to 70% and resulted in VE-cadherin localization nearly identical to that of mock-infected cells.

Product Citations (1)

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