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GW786034B

SKU: orb1300336

Description

Pazopanib Hydrochloride

Research Area

Cardiovascular Research, Cell Biology, Signal Transduction

Images & Validation

Key Properties

CAS Number635702-64-6
MW473.98
Purity99.87%
FormulaC21H23N7O2S·HCl
SMILESCl.CN(C1=CC2=NN(C)C(C)=C2C=C1)C1=NC(NC2=CC=C(C)C(=C2)S(N)(=O)=O)=NC=C1
TargetAutophagy,FGFR,c-Fms,c-Kit,VEGFR,PDGFR
Solubility10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.11 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);DMSO:7.5 mg/mL (15.82 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

Target IC50
c-Kit:140 nM|PDGFR:84 nM|c-Fms:146 nM|VEGFR1:10 nM|VEGFR2:30 nM|VEGFR3:47 nM|FGFR:74 nM
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
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.
Cell Research
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. (Only for Reference)

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

SCFR, PDGFR, VEGFR1, VEGFR2, VEGFR3, VEGFR, Votrient HCl, FGFR, GW 786034, GW-786034, GW786034 HCl, Pazopanib, Pazopanib HCl, Pazopanib Hydrochloride, Autophagy, c-Kit, cKit, CD117, c-Fms, cFms
Quality Guarantee

Quality Guarantee

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Key Properties

No computed properties available.

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GW786034B (orb1300336)

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1 ml x 10 mM (in DMSO)
$ 70.00
10 mg
$ 80.00
25 mg
$ 110.00
50 mg
$ 140.00
100 mg
$ 190.00
500 mg
$ 420.00
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