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

CAS: 1460286-21-8 Cat. No.: M651380 Formule: C₁₇H₁₈N₂O₂ Poids moléculaire: 282.34

GRADE & PURITY ≥98%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Vue d’ensemble

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

Spécifications et pureté

≥98%

Mécanismes biochimiques et physiologiques

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

Conditions de stockage de stockage

Store at -20°C

Expédié en

Ice chest + Ice pads

Ce produit nécessite l'expédition en chaîne froide. Les services terrestres et autres services économiques ne sont pas disponibles.

Type d'action

INHIBITOR

Pureté

≥98%

Noms et identifiants

• Poids moléculaire: 282.34

Propriétés chimiques et physiques

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

Foire aux questions

What is the purity of this product?

This product is supplied at ≥98% purity (chemical assay). Lot-specific values are stated on the Certificate of Analysis.

How should this product be stored?

Store at ?20 °C. Freezer storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships in an insulated container with ice pads. Unpack on arrival and transfer it to the storage condition stated above.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 1460286-21-8, the molecular formula is C17H18N2O2, and the molecular weight is 282.34 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.