Pazopanib

SKU: orb1310940

Description

Pazopanib

Research Area

Cardiovascular Research, Cell Biology, Signal Transduction

Key Properties

• CAS Number: 444731-52-6
• MW: 437.52
• Purity: 99.85%
• Formula: C₂₁H₂₃N₇O₂S
• SMILES: CN(c1ccc2c(C)n(C)nc2c1)c1ccnc(Nc2ccc(C)c(c2)S(N)(=O)=O)n1
• Target: FGFR,VEGFR,PDGFR,c-Kit,Autophagy
• Solubility: DMSO:25 mg/mL (57.14 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.57 mM)

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.
• 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.
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PDGFR, SCFR, Platelet-derived growth factor receptor, VEGFR, VEGFR1, VEGFR2, VEGFR3, Vascular endothelial growth factor receptor, Fibroblast growth factor receptor, FGFR, GW786034, GW-786034, GW 786034, Inhibitor, Pazopanib, inhibit, Autophagy, CD117, cKit, c-Kit

Compound Identifiers

PubChem CID

10113978