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Vismodegib

CAS No. : 879085-55-9

MCE 国际站：Vismodegib

产品活性：Vismodegib (GDC-0449) 是一种具有口服活性的 hedgehog 抑制剂，IC₅₀ 值为 3 nM；还可抑制 P-gp 和 ABCG2 的活性，IC₅₀ 值分别为 3.0 μM 和 1.4 μM。

研究领域：Stem Cell/Wnt  |  Autophagy

作用靶点：Hedgehog  |  Autophagy

In Vitro: Vismodegib (HhAntag691) is an ABCG2 inhibitor and can increase the effective intracellular concentration of NSC 279836, another ABCG2 substrate, through blocking its export in HEK293 cells. Vismodegib (HhAntag691, 10 μM), resensitizes MDCKII/Pgp cells and MDCKII/MRP1 cells to NSC757 treatment. Vismodegib (25 μM or 50 μM) concentration-dependently inhibits HCC and H1339 cells.

In Vivo: Vismodegib (0.3 to 75 mg/kg, p.o.) is highly efficacious in medulloblastoma allograft tumors. Vismodegib (> 46 mg/kg, p.o.) causes growth delay in patient-derived colorectal xenografts.

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