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Pazopanib

Catalog No. T0097L   CAS 444731-52-6
Synonyms: GW786034

Pazopanib (GW786034), a small molecule inhibitor, inhibits multiple protein tyrosine kinases with potential antineoplastic activity. Pazopanib selectively inhibits VEGFR-1, -2 and -3, c-kit and PDGF-R, which may result in inhibition of angiogenesis in tumors in which these receptors are upregulated.

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Pazopanib Chemical Structure
Pazopanib, CAS 444731-52-6
Pack Size Availability Price/USD Quantity
10 mg In stock $ 42.00
25 mg In stock $ 67.00
50 mg In stock $ 97.00
100 mg In stock $ 148.00
200 mg In stock $ 249.00
500 mg In stock $ 349.00
1 mL * 10 mM (in DMSO) In stock $ 54.00
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Purity: 99.84%
Purity: 99.29%
Purity: 98.78%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Pazopanib (GW786034), a small molecule inhibitor, inhibits multiple protein tyrosine kinases with potential antineoplastic activity. Pazopanib selectively inhibits VEGFR-1, -2 and -3, c-kit and PDGF-R, which may result in inhibition of angiogenesis in tumors in which these receptors are upregulated.
Targets&IC50 VEGFR2:30 nM, VEGFR3:47 nM, VEGFR1:10 nM, PDGFR:84 nM, c-Kit:74 nM
Kinase Assay 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 4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid (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 compound 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[1].
Cell Research Pazopanib is prepared in DMSO and then diluted to final concentration in medium[1]. The effect of Pazopanib on cell proliferation is measured using 5-bromo-2-deoxyuridine (BrdU) incorporation method using commercially available kits. HUVEC is seeded in medium containing 5% fetal bovine serum (FBS) in type 1 collagen coated 96-well plates and incubated overnight at 37°C, 5% CO2. The medium is aspirated from the cells, and various concentrations of Pazopanib in serum-free medium are added to each well. After 30 min, either VEGF (10 ng/mL) or bFGF (0.3 ng/mL) is added to the wells. Cells are incubated for an additional 72 h and BrdU (10 μM) is added during the last 18 to 24 h of incubation. At the end of incubation, BrdU incorporation in cells is measured by ELISA. Data are fitted with a curve described by the equation, y=Vmax(1?(x/(K+x))), where K is equal to the IC50[1].
Synonyms GW786034
Molecular Weight 437.52
Formula C21H23N7O2S
CAS No. 444731-52-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 81 mg/mL (185.1 mM)

TargetMolReferences and Literature

1. Harris PA, et al. J Med Chem. 2008, 51(15), 4632-4640. 2. Hosaka S, et al. J Orthop Res. 2012. 3. Kernt M, et al. Retina. 2012.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Anti-Cancer Drug Library Anti-Cancer Approved Drug Library Tyrosine Kinase Inhibitor Library Anti-Cancer Clinical Compound Library Inhibitor Library Anti-Lung Cancer Compound Library Pediatric Drug Library ReFRAME Related Library Reprogramming Compound Library

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Keywords

Pazopanib 444731-52-6 Angiogenesis Autophagy Tyrosine Kinase/Adaptors VEGFR FGFR PDGFR c-Kit Platelet-derived growth factor receptor GW 786034 Vascular endothelial growth factor receptor CD117 inhibit GW786034 Fibroblast growth factor receptor GW-786034 Inhibitor SCFR inhibitor

 

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