RK-287107 是一种有效且特异性的 tankyRase 抑制剂，可阻断结直肠癌细胞生长，对tankyRase-1和tankyRase-2的IC50分别为 14.3 和 10.6 nM。

RK-287107 is an effective and specific inhibitor of tankyrase (IC50s: 14.3 and 10.6 nM for tankyrase-1 and tankyrase-2, respectively).

RK-287107 (0.03-10 μM; 16 hours) also downregulates β-catenin signaling in cultured cells. 287107 (0.03-10 μM; 16 hours) induces the accumulation of tankyrase and Axin1/2. RK-87107 (0.01-10 μM; 12 hours) displays an antiproliferative effect on colorectal cancer cells harboring short adenomatous polyposis coli mutations. The 50% growth inhibition (GI50) value of RK-287107 on COLO-320DM cells is 0.449 μM. RK- [1].

In a mouse xenograft model, 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 [1].

2171386-10-8

C22H26F2N4O2

416.46

DMSO:120 mg/mL (288.14 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years