MSC2504877

• CAT Number: I032829
• CAS Number: 1460286-21-8
• Molecular Formula: C17H18N2O2
• Molecular Weight: 282.34
• Purity: ≥95%
• Synonyms: 3-[4-(2-hydroxypropan-2-yl)phenyl]-6-methyl-2H-pyrrolo[1,2-a]pyrazin-1-one
• InChI: InChI=1S/C17H18N2O2/c1-11-4-9-15-16(20)18-14(10-19(11)15)12-5-7-13(8-6-12)17(2,3)21/h4-10,21H,1-3H3,(H,18,20)
• InChIKey: MPXAEYSGFKRDQM-UHFFFAOYSA-N
• SMILES: CC1=CC=C2N1C=C(NC2=O)C3=CC=C(C=C3)C(C)(C)O

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].
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[1].
MSC2504877 (0-100 µM; 5 days) inhibits the survival of APC−/− cells and COLO320DM cells[1].
MSC2504877 (1 µM; 24 h) combinant with albociclib (HY-50767) (0.03 µM) induces cell cycle arrest at G1 phase[1].
MSC2504877 (30 mg/kg; p.o.; once) inhibits TNKS and Wnt signalling in mice[1].
MSC2504877 (30 mg/kg+ palbociclib (HY-50767) 150 mg/kg; p.o.; once) suppresses hyperproliferation in Apc defective cells in vivo[1].

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.
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