产品
编 号:F275505
分子式:C22H26F2N4O2
分子量:416.46
产品类型
结构图
CAS No: 2171386-10-8
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产品详情
生物活性:
RK-287107 is a potent and specific tankyrase inhibitor with IC50s of 14.3 and 10.6 nM for tankyrase-1 and tankyrase-2, respectively. RK-287107 blocks colorectal cancer cell growth.
体内研究:
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.Animal Model:6-week-old female NOD.CB17-Prkdcscid/J mice with colorectal cancer COLO-320DM
Dosage:100 and 300 mg/kg
Administration:Administration i.p.; once per day; 5-days on/ 2-days off schedule for 2 weeks
Result:100 and 300 mg/kg resulted in 32.9% and 44.2% TGI, respectively.
体外研究:
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.