Pazopanib (GW786034) is an inhibitor of protein tyrosine kinases that inhibits VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms (IC₅₀=10/30/47/84/74/140/146 nM). Pazopanib has antitumor activity.

VEGFR3:47 nM, VEGFR2:30 nM, c-Fms:146 nM, c-Kit:74 nM, VEGFR1:10 nM, PDGFR:84 nM, FGFR1:140 nM

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. [1]
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. [2]

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. [1]

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 activate

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