| Bioactivity | MSC2504877 (M2912) is a potent and orally active tankyrase inhibitor with IC50s of 0.0007, 0.0008, 0.54 µM for TNKS, TNKS2, PARP1, respectively. MSC2504877 increases the expression of AXIN2 and TNKS protein levels and decreases β-catenin levels. MSC2504877 shows anti-tumor activity[1]. | |||||||||
| Invitro | MSC2504877 (1, 3, 10 µM；24 小时) 增加 APC 突变体 COLO320DM 结直肠肿瘤细胞中 AXIN2 和 TNKS 蛋白水平的表达并降低 β-catenin 蛋白水平[1]。MSC2504877 (0-100 µM；5 天) 抑制 APC−/− 细胞和 COLO320DM 细胞的存活[1]。MSC2504877 (1 µM；24 小时) 与 albociclib (HY-50767) (0.03 µM) 联合使用可诱导细胞周期停滞在 G1 期[1]。 Western Blot Analysis[1] Cell Line: | |||||||||
| In Vivo | MSC2504877 (30 mg/kg；口服；一次) 抑制小鼠体内的 TNKS 和 Wnt 信号传导[1]。MSC2504877 (50 mg/kg+palbociclib (HY-50767) 150mg/kg；口服；一次) 抑制体内 Apc 缺陷细胞的过度增殖[1]。 Animal Model: | |||||||||
| Name | MSC2504877 | |||||||||
| CAS | 1460286-21-8 | |||||||||
| Formula | C17H18N2O2 | |||||||||
| Molar Mass | 282.34 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [1]. Menon M, et al. A novel tankyrase inhibitor, MSC2504877, enhances the effects of clinical CDK4/6 inhibitors. Sci Rep. 2019 Jan 17;9(1):201. |
MSC2504877
CAS: 1460286-21-8 F: C17H18N2O2 W: 282.34
MSC2504877 (M2912) is a potent and orally active tankyrase inhibitor with IC50s of 0.0007, 0.0008, 0.54 µM for TNKS, TN
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