RK-287107 产品说明书 Chemicals
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产品编号 DC12436
名称 RK-287107

化学性质

CAS 2171386-10-8
分子式 C22H26F2N4O2
分子量 416.473
存储条件 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

生物活性

Description
In Vivo
In Vitro

化合物的使用

Kinase Assay
Cell Assay
Animal Administration

参考文献


RK-287107 (RK287107) is a novel potent, tankyrase-specific inhibitor with IC50 of 14.3 and 10.6 nM for tankyrase-1 and tankyrase-2, respectively, shows no activity against PARP-1;shows 4-8-fold more potency than G007-LK; causes Axin2 accumulation and downregulates β-catenin, T-cell factor/lymphoid enhancer factor reporter activity and the target gene expression in colorectal cancer cells harboring the shortly truncated APC mutations; inhibits the growth of APC-mutated (β-catenin-dependent) colorectal cancer COLO-320DM and SW403 cells but not the APC-wild (β-catenin-independent) colorectal cancer RKO cells; suppresses COLO-320DM tumor growth in NOD-SCID mice (intraperitoneal or oral administration).
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