2. Cell Cycle/DNA Damage Epigenetics
  3. PARP
  4. MSC2504877

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.

For research use only. We do not sell to patients.

MSC2504877 Chemical Structure

MSC2504877 Chemical Structure

CAS No. : 1460286-21-8

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Based on 1 publication(s) in Google Scholar

MSC2504877 Related Antibodies

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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Description

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].

IC50 & Target[1]

PARP1

0.54 μM (IC50)

TNKS

0.0007 μM (IC50)

TNKS2

0.0008 μM (IC50)

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[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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

MSC2504877 Related Antibodies

Western Blot Analysis[1]

Cell 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[1].
MSC2504877 (30 mg/kg+ palbociclib (HY-50767) 150 mg/kg; p.o.; once) suppresses hyperproliferation in Apc defective cells in vivo[1].

MedChemExpress (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)[1]
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[1]
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.
Molecular Weight

282.34

Formula

C17H18N2O2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C1C2=CC=C(C)N2C=C(C3=CC=C(C(C)(O)C)C=C3)N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (442.73 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.5418 mL 17.7091 mL 35.4183 mL
5 mM 0.7084 mL 3.5418 mL 7.0837 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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This equation is commonly abbreviated as: C1V1 = C2V2

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Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.5418 mL 17.7091 mL 35.4183 mL 88.5457 mL
5 mM 0.7084 mL 3.5418 mL 7.0837 mL 17.7091 mL
10 mM 0.3542 mL 1.7709 mL 3.5418 mL 8.8546 mL
15 mM 0.2361 mL 1.1806 mL 2.3612 mL 5.9030 mL
20 mM 0.1771 mL 0.8855 mL 1.7709 mL 4.4273 mL
25 mM 0.1417 mL 0.7084 mL 1.4167 mL 3.5418 mL
30 mM 0.1181 mL 0.5903 mL 1.1806 mL 2.9515 mL
40 mM 0.0885 mL 0.4427 mL 0.8855 mL 2.2136 mL
50 mM 0.0708 mL 0.3542 mL 0.7084 mL 1.7709 mL
60 mM 0.0590 mL 0.2952 mL 0.5903 mL 1.4758 mL
80 mM 0.0443 mL 0.2214 mL 0.4427 mL 1.1068 mL
100 mM 0.0354 mL 0.1771 mL 0.3542 mL 0.8855 mL
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MSC2504877 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MSC25048771460286-21-8M2912MSC 2504877MSC-2504877M 2912M-2912PARPpoly ADP ribose polymeraseAXIN2TNKSβ-cateninalbociclibG1 phaseanti-tumorInhibitorinhibitorinhibit

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