MSC2504877

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

MSC2504877 是一种坦科聚合酶抑制剂，可增强临床 CDK4/6 抑制剂的效果。 MSC2504877 抑制 palbociclib 引起的 Cyclin D2 和 Cyclin E2 上调，并增强对磷酸 Rb 的抑制。

MSC2504877 is an inhibitor of tankyrase and enhances the effects of clinical CDK4/6 inhibitors. MSC2504877 suppresses the upregulation of Cyclin D2 and Cyclin E2 caused by palbociclib and enhances the suppression of phospho-Rb.

Western Blot Analysis Cell Line:APC mutant COLO320DM colorectal tumour cells Concentration:1, 3, 10 μM Incubation Time:24 h Result:Increased AXIN2 protein levels and decreased β-catenin levels.

Animal Model:CB17 SCID mice (APC mutant COLO320DM tumour cell xenografts)Dosage:30 mg/kg Administration:P.o.; once Result:Elicited an increase in both TNKS and AXIN2 levels in tumours, peaking at 6–10?hours after drug administration and falling 18?hours after.Animal Model:Villin-CreERT2; Apcfl/fl mice Dosage:50 mg/kg +?palbociclib (150?mg/kg) Administration:P.o.; once Result:Suppressed the expression of the archetypal Wnt target gene and stem cell marker Lgr5 and combination drug treatment caused a profound increase in nuclear p21.

3-(4-(2-Hydroxypropan-2-yl)phenyl)-6-methylpyrrolo[1,2-a]pyrazin-1(2H)-one

Others

Other Targets

PTP1B

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1460286-21-8

282.34

C17H18N2O2

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (442.73 mM)

O=C1NC(=CN2C1=CC=C2C)C=3C=CC(=CC3)C(O)(C)C

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(-20℃)

With Ice Pack

≥ 2 years