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Telatinib mesylate

CAS No. : 332013-26-0

MCE 国际站：Telatinib mesylate

产品活性：Telatinib mesylate (Bay 57-9352 mesylate) 是一种有效的的口服活性的 VEGFR2，VEGFR3，PDGFα 和 c-Kit 抑制剂，IC₅₀ 分别为 6 nM，4 nM，15 nM 和 1 nM。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：VEGFR  |  PDGFR  |  c-Kit

In Vitro: Telatinib enhances the anticancer activity of ABCG2 substrate anticancer drugs by inhibiting ATP-binding cassette G2 (ABCG2) efflux transporter activity. Co-incubation of ABCG2-overexpressing drug resistant cell lines with Telatinib and ABCG2 substrate anticancer drugs significantly reduces cellular viability, whereas Telatinib alone does not significantly affect drug sensitive and drug resistant cell lines. Telatinib at 1 μM does not significantly alter the expression of ABCG2 in ABCG2-overexpressing cell lines. Telatinib at 1 μM significantly enhances the intracellular accumulation of [³H]-mitoxantrone (MX) in ABCG2-overexpressing cell lines.
Telatinib at 1 μM significantly reduces the rate of [³H]-MX efflux from ABCG2-overexpressing cells. Furthermore, Telatinib significantly inhibits ABCG2-mediated transport of [³H]-E₂17βG in ABCG2 overexpressing membrane vesicles.

In Vivo: Telatinib (15 mg/kg; oral dministration; every 2nd and 3rd day; total 12 times; male athymic NCR (nu/nu) nude mice) with Doxorubicin (1.8 mg/kg) significantly decreases the growth rate and tumor size of ABCG2 overexpressing tumors in a xenograft nude mouse model.

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