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Pazopanib

CAS No. : 444731-52-6

MCE 站：Pazopanib

产品活性：Pazopanib (GW786034) 是多靶点抑制剂，抑制 VEGFR1，VEGFR2，VEGFR3，PDGFRβ，c-Kit，FGFR1，c-Fms的IC₅₀分别为10，30，47，84，74，140，146 nM。

研究领域：Protein Tyrosine Kinase/RTK  |  Autophagy

作用靶点：VEGFR  |  c-Kit  |  PDGFR  |  Autophagy  |  FGFR

In Vitro: Pazopanib shows good potency against all the human VEGFR receptors with an IC₅₀ of 10, 30, ａnd 47 nM for VEGFR-1, -2, ａnd -3, respectively. Significant activity is also seen against the closely related tyrosine receptor kinases PDGFRβ, c-Kit, FGF-R1, ａnd c-fms with IC₅₀s of 84, 74, 140, ａnd 146 nM, respectively. In cellular assays, in addition to inhibiting the VEGF-induced proliferation of HUVECs, Pazopanib potently inhibits VEGF-induced phosphorylation of VEGFR-2 in HUVEC cells with an IC₅₀ of ~8 nM. Pazopanib possesses good pharmacokinetics in rat, dog, ａnd monkey with low clearances (1.4-1.7 mL/min/kg) ａnd good oral bioavailabilities (72, 47, 65%) dosed at 10, 1, ａnd 5 mg/kg, respectively. The cytochrome P450 profile is also improved with inhibition >10 μM against the isozymes tested, with the exception of 2C9 (7.9 μM).

In Vivo: Treatment of mice with 100 mg/kg of Pazopanib twice daily for five days results in significant inhibition in the degree of vascularization. The antiangiogenic activity of Pazopanib is examined in mice bearing established human xenografts (200−250 mm³) using HT29 (colon carcinoma), A375P (melanoma), ａnd HN5 (head ａnd neck carcinoma) tumors following a standard three-week course of therapy. The HN5 ａnd HT29 xenografts responded better at all doses compared to the A375P model, which is historically more resistant to VEGFR-2 inhibitors. As support that the observed inhibition of xenograft growth is working through an antiangiogenic rather than antitumor mechanism, no antiproliferative activity is observed below 10 μM for Pazopanib against these human tumor lines (HT29, HN5, A375P) growing in serum-containing media. No significant effect on the body weight of mice is observed, ａnd the animals appeared healthy ａnd active throughout the study duration. The quantity of adherent leukocytes in the Pazopanib eye drops group is less than untreated diabetic animals ａnd more than the healthy animals. Average leukocytes adhered to the retinal vasculature in healthy animals is 37.2±7.8, whereas diabetic animals have an average value of 102±15.6, approximately 3-fold higher than healthy animals. Animals treated with 0.5 % w/v Pazopanib suspension demonstrate 69.5±9.5 leukocytes adhered in their retinal vasculature, which is found to be significantly lower than diabetic animals.

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