RK-287107 是一种有效且特异性的 tankyrase 抑制剂，对 tankyrase-1 和 tankyrase-2 的 IC50 分别为 14.3 和 10.6 nM。 RK-287107 阻断结直肠癌细胞生长。
| Cas No. | 2171386-10-8 |
| Canonical SMILES | O=C1NC(N2CCC3(CC2)CN(CCO)C4=C3C(F)=CC(F)=C4)=NC5=C1CCCC5 |
| 分子式 | C22H26F2N4O2 |
| 分子量 | 416.46 |
| 溶解度 | Soluble in DMSO |
| 储存条件 | 4°C, protect from light |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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[1].
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[1].
RK-287107 (0.03-10 μM; 16 hours) causes accumulation of tankyrase and Axin1/2[1].
RK-287107 (0.03-10 μM; 16 hours) also downregulates β-catenin signaling in cultured cells[1].
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[1].
Reference：
[1]. Mizutani A, et al. RK-287107, a potent and specific tankyrase inhibitor, blocks colorectal cancer cell growth in a preclinical model. Cancer Sci. 2018 Dec;109(12):4003-4014. |
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