RK-287107,2171386-10-8

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RK-287107

CAS No. : 2171386-10-8

MCE 国际站：RK-287107

产品活性：RK-287107 是一种有效的特异性 tankyrase 抑制剂，抑制 tankyrase-1 和 tankyrase-2，IC₅₀ 分别为 14.3 和 10.6 nM。RK-287107 可阻断结直肠癌细胞生长。

研究领域：Cell Cycle/DNA Damage  |  Epigenetics

作用靶点：PARP

In Vitro: RK-87107 (0.01-10 μM; 12 hours) shows an antiproliferative effect on colorectal cancer cells harboring short adenomatous polyposis coli (APC) mutations. The 50% growth inhibition (GI₅₀) value of RK-287107 on COLO-320DM cells is 0.449 μM.
RK-287107 (0.03-10 μM; 16 hours) causes accumulation of tankyrase and Axin1/2.
RK-287107 (0.03-10 μM; 16 hours) also downregulates β-catenin signaling in cultured cells.

In Vivo: RK-287107 (100 and 300 mg/kg; i.p. administration; once per day; 5-days on/ 2-days off schedule for 2 weeks) inhibits tumor growth in a mouse xenograft model.

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