AS1810722

AS1810722 is an orally active and potent STAT6 inhibitor with an IC50 of 1.9 nM. AS1810722 shows a good profile of CYP3A4 inhibition. AS1810722, a derivative of fused bicyclic pyrimidine, has the potential for allergic diseases such as asthma and atopic diseases research.

Product information

CAS Number: 909561-15-5

Molecular Weight: 477.51

Formula: C25H25F2N7O

Chemical Name: 2-{4-[4-({7-[(3, 5-difluorophenyl)methyl]-7H-pyrrolo[2, 3-d]pyrimidin-2-yl}amino)phenyl]piperazin-1-yl}acetamide

Smiles: NC(=O)CN1CCN(CC1)C1C=CC(=CC=1)NC1=NC2=C(C=N1)C=CN2CC1C=C(F)C=C(F)C=1

InChiKey: IJFRMEXSGYTWGY-UHFFFAOYSA-N

InChi: InChI=1S/C25H25F2N7O/c26-19-11-17(12-20(27)13-19)15-34-6-5-18-14-29-25(31-24(18)34)30-21-1-3-22(4-2-21)33-9-7-32(8-10-33)16-23(28)35/h1-6,11-14H,7-10,15-16H2,(H2,28,35)(H,29,30,31)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 62.5 mg/mL (130.89 mM; Need ultrasonic)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

AS1810722 (compound 24) inhibits production of IL-4 with an IC50 of 2.4 nM, but shows no effect on production of IFN-γ.

In Vivo:

AS1810722 (compound 24; 0.03-0.3 mg/kg; orally; 30 min before, and 24h and 48 h after OVA exposure) suppress eosinophil infiltration in the lung in a dose-dependent manner in an antigen-induced mouse asthmatic model. AS1810722 inhibits in vitro Th2 differentiation with an IC50 of 2.4 nM without affecting type 1 helper T (Th1) cell differentiation and eosinophil infiltration in an antigen-induced mouse asthmatic model after oral administration.

References:

1. Shinya Nagashima, et al. Novel 7H-pyrrolo[2,3-d]pyrimidine derivatives as potent and orally active STAT6 inhibitors. Bioorg Med Chem. 2009 Oct 1;17(19):6926-36.

Products are for research use only. Not for human use.