MSC2504877 - ≥98% , CAS No.1460286-21-8

CAS: 1460286-21-8 Cat. No.: M651380 Molecular Weight: 282.34

GRADE & PURITY ≥98%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Overview

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 )

Specifications

Specifications & Purity

≥98%

Biochemical and Physiological Mechanisms

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. MSC250

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

INHIBITOR

Purity

≥98%

Names and Identifiers

• Molecular Weight: 282.34

Chemical and Physical Properties

• Solubility: DMSO : 125 mg/mL (442.73 mM; Need ultrasonic)