MSC2504877 manufacturers
- MSC2504877
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- $39.00
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2026-07-14
- CAS:1460286-21-8
- Purity: 99.72%
- Supply Ability: 10g
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| | MSC2504877 Basic information |
| Product Name: | MSC2504877 | | Synonyms: | MSC2504877;MSC2504877（M2912）;Pyrrolo[1,2-a]pyrazin-1(2H)-one, 3-[4-(1-hydroxy-1-methylethyl)phenyl]-6-methyl-;MSC2504877, 10 mM in DMSO;3-(4-(2-Hydroxypropan-2-yl)phenyl)-6-methylpyrrolo[1,2-a]pyrazin-1(2H)-one;M2912 ，E1069 | | CAS: | 1460286-21-8 | | MF: | C17H18N2O2 | | MW: | 282.34 | | EINECS: | | | Product Categories: | | | Mol File: | 1460286-21-8.mol |  |
| | MSC2504877 Chemical Properties |
| Boiling point | 444.1±45.0 °C(Predicted) | | density | 1.20±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO: 56 mg/mL (198.34 mM);Ethanol: 6 mg/mL (21.25 mM) | | pka | 10.92±0.40(Predicted) | | form | Solid | | color | Off-white to light yellow | | Water Solubility | Water: Insoluble |
| | MSC2504877 Usage And Synthesis |
| Uses | 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]. | | Biological Activity | M2912 (MSC2504877) is a very potent TNKS1/TNKS2 inhibitor (IC50=0.6 nM for TNKS1) with exquisite selectivity over other PARP family enzymes and favorable compound properties. This inhibitor potently modulates the Wnt/β-catenin pathway by elevating the levels of axin2 (EC50=17 nM) and tankyrase in DLD1 cells in a dose-dependent manner resulting in reduced cellular Wnt reporter activity. | | in vivo | MSC2504877 (30 mg/kg; p.o.; once) inhibits TNKS and Wnt signalling in mice[1].
MSC2504877 (30 mg/kg+palbociclib (HY-50767) 150mg/kg; p.o.; once) suppresses hyperproliferation in Apc defective cells in vivo[1]. | Animal Model: | CB17 SCID mice (APC mutant COLO320DM tumour cell xenografts)[1] | | Dosage: | 30 mg/kg | | Administration: | P.o.; once | | Result: | Elicited an increase in both TNKS and AXIN2 levels in tumours, peaking at 6–10hours after drug administration and falling 18hours after. |
| Animal Model: | Villin-CreERT2; Apcfl/fl mice[1] | | Dosage: | 50 mg/kg +palbociclib (150mg/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. |
| | IC 50 | PARP1: 0.54 μM (IC50); TNKS: 0.0007 μM (IC50); TNKS2: 0.0008 μM (IC50) | | References | [1] Buchstaller HP, et al. J Med Chem. 2021 Jul 22;64(14):10371-10392. |
| | MSC2504877 Preparation Products And Raw materials |
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