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Pazopanib

SKU: orb1310940
FeaturedFeatured Product

Description

Pazopanib

Research Area

Cardiovascular Research, Cell Biology, Pharmacology & Drug Discovery, Signal Transduction

Images & Validation

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Pazopanib

Key Properties

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CAS Number444731-52-6
MW437.5
Purity>98%
FormulaC21H23N7O2S
SMILESCN(c1ccc2c(C)n(C)nc2c1)c1ccnc(Nc2ccc(C)c(c2)S(N)(=O)=O)n1
TargetKinase
SolubilitySoluble in DMSO (up to 16 mg/ml).

Bioactivity

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Target IC50
VEGFR2:30 nM|VEGFR3:47 nM|c-Fms:146 nM|VEGFR1:10 nM|PDGFR:84 nM|FGFR1:140 nM|c-Kit:74 nM
In Vivo
METHODS: To assay anti-tumor activity in vivo, Pazopanib (30 mg/kg, suspended in 0.5% hydroxypropylmethyl cellulose and 0.1% Tween-80 in water) was administered by gavage to NOD-SCID mice bearing NCI-H446 xenografts The drug was administered once daily for two weeks. RESULTS: Administration of Pazopanib significantly inhibited the growth of NCI-H446 xenografts.
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In Vitro
METHODS: SCLC cell lines NCI-H446 and NCI-H82 were treated with Pazopanib (0.01-30 µM) for 24-72 h. Cell viability was measured by CCK-8 assay. RESULTS: Pazopanib significantly reduced the proliferation of NCI-H446 cells in a dose- and time-dependent manner, with an IC50 value of 1.05 µM at 24 h. Pazopanib also induced potent cell death in NCI-H82 cells in a dose- and time-dependent manner, with an IC50 of 1.298 µM at 24 h. Pazopanib significantly antagonized the proliferation of small cell lung cancer cells. METHODS: Human colorectal cancer cells HCT-116 were treated with Pazopanib (1-20 µM) for 3-24 h, and the expression levels of target proteins were detected by Western Blot. RESULTS: Pazopanib significantly induced the expression of PUMA in a time- and dose-dependent manner.
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Cell Research
Pazopanib is prepared in DMSO and then diluted to final concentration in medium. 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.
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Storage & Handling

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Storage-20°C
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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GSK-VEG10003; GW786034B

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Compound Identifiers

PubChem CID
10113978 ↗

Key Properties

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No computed properties available.

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Pazopanib (orb1310940)

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$ 160.00
50 mg
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