| Identification | Back Directory | [Name]
AS601245.2TFA (345987-15-7 free base) | [CAS]
345987-16-8 | [Synonyms]
AS601245.2TFA (345987-15-7 free base) | [Molecular Formula]
C20H16N6S.2C2HF3O2 | [MOL File]
345987-16-8.mol | [Molecular Weight]
600.49 |
| Hazard Information | Back Directory | [Uses]
AS601245 TFA 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 TFA 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[1][2]. | [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[1].
AS601245 (0.3-10 mg/kg; p.o.) is a potent inhibitor of LPS-induced TNF-α release in mice[1]. | Animal Model: | C3H/HEN mice[1] | | Dosage: | 0.3, 1, 3, or 10 mg/kg | | Administration: | P.o. | | Result: | Decreased the TNF-α release in a dose-dependent manner.
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| [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. DOI:10.1124/jpet.103.064246 |
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