| Identification | Back Directory | [Name]
RK-20449 trihydrochloride | [CAS]
1435934-25-0 | [Synonyms]
A 419259 3HCl
RK20449 trihydrochloride
A-419259 (hydrochloride)
RK 20449 trihydrochloride
RK-20449 trihydrochloride
A419259; A-419259 TRIHYDROCHLORIDE
7-((1r,4r)-4-(4-methylpiperazin-1-yl)cyclohexyl)-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine trihydrochloride
7-[trans-4-(4-Methyl-1-piperazinyl)cyclohexyl]-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine hydrochloride (1:3)
A419259 TRIHYDROCHLORIDE;A-419259 TRIHYDROCHLORIDE;RK 20449 TRIHYDROCHLORIDE;RK20449 TRIHYDROCHLORIDE;RK-20449 TRIHYDROCHLORIDE | [Molecular Formula]
C29H37Cl3N6O | [MOL File]
1435934-25-0.mol | [Molecular Weight]
592.003 |
| Hazard Information | Back Directory | [Uses]
A 419259 Trihydrochloride is the hydrochloride form of A 419259 which is a Src kinase inhibitor and can be used in treatment of chronic myelogenous leukemia, lymphangioleiomyomatosis and tuberous sclerosis. | [Biological Activity]
a 419259 trihydrochloride is an orally available inhibitor of lck with ic50 value of 15 nm [1].lck is a src family tyrosine kinase. inhibition of this enzyme results in a prevention of t-cell activation and provides an application for treating t-cell dependent processes such as autoimmune and inflammatory diseases. a 419259 trihydrochloride is screened out by its potent inhibitory activity against the recombinant lck (64–509) with ic50 value of 15nm. it is also a selective inhibitor. it shows inactive against a panel of other kinases including cmet, igfr, pkc and pdgfr. besides that, a 419259 trihydrochloride is found to inhibit the production of il-2 with ic50 value of 25nm in jurkat cells. moreover, administration of a 419259 trihydrochloride reduces il-2 production in mice with ed50 value of 2.5 mg/kg. a 419259 trihydrochloride also has efficacy of the antigen specific t-cell immune response. administration of this compound inhibits ifn-γ production during the in vivo priming phase [1]. | [storage]
Desiccate at RT | [References]
[1] calderwood d j, johnston d n, munschauer r, et al. pyrrolo [2, 3-d] pyrimidines containing diverse n-7 substituents as potent inhibitors of lck. bioorganic & medicinal chemistry letters, 2002, 12(12): 1683-1686. |
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