MSC2504877 free base · Synonyms: MSC-2504877 · MSC 2504877

MSC2504877 is a novel small molecule selective tankyrase inhibitor.

For research use only. Not for human or veterinary use.

Target PARP

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

MSC2504877 structure

CAS No.: 1460286-21-8

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 480.00	BP-02156-100mg	In stock	Get quote
250 mg	USD 950.00	BP-02156-250mg	In stock	Get quote
500 mg	USD 1,500.00	BP-02156-500mg	In stock	Get quote
1 g	USD 2,400.00	BP-02156-1g	In stock	Get quote
2 g	USD 3,700.00	BP-02156-2g	In stock	Get quote

Need another size or custom synthesis? Request a quote.

Description

MSC2504877 is a novel small molecule selective tankyrase inhibitor with IC50 of 0.7/0.8 nM against TNKS1/2, shows 771-fold selectivity for TNKS1 over PARP1 (IC50=0.54 uM).

Biological 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 (HY-50767) (0.03 µM) induces cell cycle arrest at G1 phase. In Vivo MSC2504877 (30 mg/kg; p.o.; once) inhibits TNKS and Wnt signalling in mice. MSC2504877 (30 mg/kg+ palbociclib (HY-50767) 150 mg/kg; p.o.; once) suppresses hyperproliferation in Apc defective cells in vivo.

Identifiers

SMILES: O=C1C2=CC=C(C)N2C=C(C3=CC=C(C(C)(O)C)C=C3)N1
InChIKey: MPXAEYSGFKRDQM-UHFFFAOYSA-N

Specifications

MW (average): 282.3370
Formula: C₁₇H₁₈N₂O₂
CAS No.: 1460286-21-8
Physical state: Solid
Color: Off-white to light yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 3 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO 125 mg/mL

Documents

References

[1]. Menon, Malini et al. A novel tankyrase inhibitor, MSC2504877, enhances the effects of clinical CDK4/6 inhibitors. Scientific reports vol. 9,1 201. 17 Jan. 2019, doi:10.1038/s41598-018-36447-4

Same target

Search PARP

Same research area

Search Cancer