CAS NO: | 130017-40-2 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | K-756 is a direct and selectivetankyrase(TNKS) inhibitor, which inhibits the ADP-ribosylation activity ofTNKS1andTNKS2withIC50s of 31 and 36 nM, respectively. | ||||||||||||||||
IC50& Target |
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体外研究 (In Vitro) | K-756 is a novel and selective Wnt/β-catenin pathway inhibitor targeting tankyrase (TNKS). TNKS is one of the members of the PARP family (it is also known as PARP5). K-756 binds to the induced pocket of TNKS and inhibits its enzyme activity. To study the isoform selectivity of K-756, the PARP family enzyme inhibitory activity at 10 μM is evaluated. K-756 inhibits TNKS1 and TNKS2 by 97% and 100%, respectively. In contrast, the inhibitory activity of K-756 against PARP1, PARP2, PARP3, PARP6, PARP7, and PARP11 is less than 13%. K-756 inhibits the cell growth of APC-mutant colorectal cancer COLO 320DM and SW403 cells by inhibiting the Wnt/β-catenin pathway. K-756 strongly inhibits the reporter activity in DLD-1/TCF-Luc cells with an IC50of 110 nM, but does not inhibit DLD-1/mtTCF-Luc cells, even at 1,000 nM. APC-mutant colorectal cancer cell line COLO 320DM and SW403 cells are treated with K-756 and after 144 hours, cell growth inhibition is measured by an XTT assay. The application of K-756 inhibits the cell growth of COLO 320DM with a GI50of 780 nM. K-756 also inhibits SW403 with a GI50of 270 nM[1]. | ||||||||||||||||
体内研究 (In Vivo) | DLD-1/TCF-Luc cell xenografts are created in SCID mice. Vehicle (0.5% MC400) or K-756 is administered orally once a day for 3 days at 100, 200, and 400 mg/kg. The Wnt/β-catenin signal inhibition in the tumor is detected by measuringFGF20andLGR5and luciferase activity. The expression ofFGF20and reporter activity are significantly decreased at doses of 100 mg/kg and above at 3-day administration. The expression ofLGR5is significantly decreased at doses of 200 mg/kg and above at 3-day administration. The maximum inhibitory activity is reached with the administration of K-756 at a dose of 400 mg/kg at 3-day administration. The Wnt/β-catenin signal inhibition at a dose of 400 mg/kg is observed from 1-day administration[1]. | ||||||||||||||||
分子量 | 433.50 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C24H27N5O3 | ||||||||||||||||
CAS 号 | 130017-40-2 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 4.55 mg/mL(10.50 mM;Need ultrasonic) 配制储备液
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以下溶剂前显示的百
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