Pazopanib

SKU: orb1310940

Description

Pazopanib

Research Area

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

Key Properties

• CAS Number: 444731-52-6
• MW: 437.5
• Purity: >98%
• Formula: C₂₁H₂₃N₇O₂S
• SMILES: CN(C1=CC2=NN(C)C(C)=C2C=C1)C1=NC(NC2=CC=C(C)C(=C2)S(N)(=O)=O)=NC=C1
• Target: Kinase
• Solubility: Soluble in DMSO (up to 16 mg/ml).

Bioactivity

• 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

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GSK-VEG10003; GW786034B

Compound Identifiers

PubChem CID

10113978