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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-PARP-MSC2504877
MSC2504877

Chemical Structure : MSC2504877

CAS No.: 1460286-21-8

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MSC2504877 (MSC-2504877;MSC 2504877;M2912)

货号: PC-36007Not For Human Use, Lab Use Only.

MSC2504877 (MSC-2504877) a novel small molecule selective tankyrase inhibitor with IC50 of 0.7/0.8 nM against TNKS1/2, shows 771-fold selectivity for TNKS1 over PARP1 (IC50=0.54 uM).

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10 mg ￥2580 In stock
25 mg ￥3980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

MSC2504877 (MSC-2504877) a novel small molecule selective tankyrase inhibitor with IC50 of 0.7/0.8 nM against TNKS1/2, shows 771-fold selectivity for TNKS1 over PARP1 (IC50=0.54 uM).
MSC2504877 increased AXIN2 protein levels and decreased β-catenin levels in APC mutant COLO320DM colorectal tumour cells, suppressed canonical Wnt signalling in SW480 cell line, inhibits the growth of APC mutant colorectal tumour cells.
MSC2504877 enhances G1 cell cycle arrest and cellular senescence in tumour cells when combined with CDK4/6 inhibitor Palbociclib, suppresses the upregulation of Cyclin D2 and Cyclin E2 caused by palbociclib and enhances the suppression of pRb.
Palbociclib plus MSC2504877 combination suppresses hyperproliferation in Apc defective cells in vivo.

物理化学性质&存储条件

分子量 282.343
分子式 C17H18N2O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

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

参考文献

1. Menon M, et al. Sci Rep. 2019 Jan 17;9(1):201.

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