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MSC2504877
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Catalog No. T60098Cas No. 1460286-21-8
Alias 3-(4-(2-Hydroxypropan-2-yl)phenyl)-6-methylpyrrolo[1,2-a]pyrazin-1(2H)-one
MSC2504877 is an inhibitor of tankyrase and enhances the effects of clinical CDK4/6 inhibitors. MSC2504877 suppresses the upregulation of Cyclin D2 and Cyclin E2 caused by palbociclib and enhances the suppression of phospho-Rb.
MSC2504877
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Purity: 99.72%
Catalog No. T60098Alias 3-(4-(2-Hydroxypropan-2-yl)phenyl)-6-methylpyrrolo[1,2-a]pyrazin-1(2H)-oneCas No. 1460286-21-8
MSC2504877 is an inhibitor of tankyrase and enhances the effects of clinical CDK4/6 inhibitors. MSC2504877 suppresses the upregulation of Cyclin D2 and Cyclin E2 caused by palbociclib and enhances the suppression of phospho-Rb.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 5 mg | $39 | In Stock | In Stock | |
| 10 mg | $61 | In Stock | In Stock | |
| 25 mg | $119 | In Stock | In Stock | |
| 50 mg | $173 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $39 | In Stock | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.72%
Appearance:Solid
Color:White
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Product Introduction
MSC2504877 AI Summary
MSC2504877 exhibits potent inhibitory activity against tankyrase enzymes, specifically TNKS1 with an IC50 of 0.6 nM and TNKS2 with an IC50 of 0.9 nM, as determined by ELISA assays. It also shows moderate inhibitory activity against PARP1 with an IC50 of 928.0 nM, as determined by a fluorescence-based multimode plate reader method. Additionally, MSC2504877 modulates the Wnt/beta-catenin signaling pathway in human DLD-1 cells with an EC50 of 16.0 nM and demonstrates good apparent permeability across cell membranes with a Papp value of 28.6 x 10^-6 cm/s in human Caco-2 cells. It selectively inhibits PARP-1 over TNKS1 and TNKS2, exhibiting moderate inhibition of various PARP enzymes, including PARP2, PARP3, and PARP7, with IC50 values ranging from 110.0 nM to 330.0 nM. This compound has a half-life of 6.9 hours in humans and shows moderate to high oral bioavailability in animal models, ranging from 37.0% in dogs to 77.0% in mice, indicating potential for sustained activity and good oral administration prospects..
Note: Summary generated by AI. Data source: ChEMBL 
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | MSC2504877 is an inhibitor of tankyrase and enhances the effects of clinical CDK4/6 inhibitors. MSC2504877 suppresses the upregulation of Cyclin D2 and Cyclin E2 caused by palbociclib and enhances the suppression of phospho-Rb. |
| Targets&IC50 | PARP1:0.54 μM, TNKS:0.0007 μM, TNKS2:0.0008 μM |
| Synonyms | 3-(4-(2-Hydroxypropan-2-yl)phenyl)-6-methylpyrrolo[1,2-a]pyrazin-1(2H)-one |
| Molecular Weight | 282.34 |
| Formula | C17H18N2O2 |
| Cas No. | 1460286-21-8 |
| Smiles | Cc1ccc2n1cc([nH]c2=O)-c1ccc(cc1)C(C)(C)O |
| Relative Density. | 1.20 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||
| Solubility Information | DMSO: 3.6 mg/mL (12.75 mM), Sonication is recommended.  | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
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Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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