AS601245

AS601245 is an orally active, selective, ATP competitive JNK (c-Jun NH2-terminal protein kinase) inhibitor with IC50s of 150, 220, and 70 nM for three JNK human isoforms (hJNK1, hJNK2, and hJNK3), respectively. AS601245 exhibits 10- to 20-fold selectivity over c-src, CDK2, and c-Raf and more than 50- to 100-fold selectivity over a range of Ser/Thr- and Tyr-protein kinases. Neuroprotective properties.

Product information

CAS Number: 345987-15-7

Molecular Weight: 372.45

Formula: C20H16N6S

Chemical Name: 2-(1, 3-benzothiazol-2-yl)-2-(2-{[2-(pyridin-3-yl)ethyl]amino}pyrimidin-4-yl)acetonitrile

Smiles: N#CC(C1=NC2=CC=CC=C2S1)C1=CC=NC(NCCC2C=NC=CC=2)=N1

InChiKey: RCYPVQCPYKNSTG-UHFFFAOYSA-N

InChi: InChI=1S/C20H16N6S/c21-12-15(19-25-17-5-1-2-6-18(17)27-19)16-8-11-24-20(26-16)23-10-7-14-4-3-9-22-13-14/h1-6,8-9,11,13,15H,7,10H2,(H,23,24,26)

Technical Data

Appearance: Solid Power

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

Solubility: DMSO : 10 mg/mL (26.85 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:

AS601245, an anti-Inflammatory JNK inhibitor, and Clofibrate have a synergistic effect in inducing cell responses and in affecting the gene expression profile in CaCo-2 colon cancer cells.

In Vivo:

AS601245 (40, 60, and 80 mg/kg; i.p.) provides significant protection against the delayed loss of hippocampal CA1 neurons in a gerbil model of transient global ischemia. AS601245 (0.3-10 mg/kg; p.o.) is a potent inhibitor of LPS-induced TNF-α release in mice.

References:

1. Carboni S, et al. AS601245 (1,3-benzothiazol-2-yl (2-[[2-(3-pyridinyl) ethyl] amino]-4 pyrimidinyl) acetonitrile): a c-Jun NH2-terminal protein kinase inhibitor with neuroprotective properties. J Pharmacol Exp Ther. 2004;310(1):25-32.

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