MSC2504877 (M2912) is a potent and orally active tankyrase inhibitor with IC 50 s 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 In Vitro MSC2504877 (1, 3, 10 µM; 24 h) increases the expression of AXIN2 and TNKS protein levels and decreases β-catenin levels in APC mutant COLO320DM colorectal tumor cells. MSC2504877 (0-100 µM; 5 days) inhibits the survival of APC −/− cells and COLO320DM cells. MSC2504877 (1 µM; 24 h) combinant with albociclib (0.03 µM) induces cell cycle arrest at G1 phase. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell 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. In Vivo MSC2504877 (30 mg/kg; p.o.; once) inhibits TNKS and Wnt signalling in mice . MSC2504877 (30 mg/kg+ palbociclib 150 mg/kg; p.o.; once) suppresses hyperproliferation in Apc defective cells in vivo . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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. Form:Solid IC50& Target:PARP1 0.54 μM (IC 50 ) TNKS 0.0007 μM (IC 50 ) TNKS2 0.0008 μM (IC 50 )
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MSC2504877
CAS number：1460286-21-8 molecular formula：C17H18N2O2
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| Chinese alias | - | ||
| English alias | - | ||
| CAS number | 1460286-21-8 | molecular formula | C17H18N2O2 |
| molecular weight | 282.34 g/mol | Exact mass | ≥98% |
| PSA | - | logp | - |
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