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A 419259 trihydrochloride LCK inhibitor, orally available

Catalog No.B1301
Size Price Stock Qty
10mg
$185.00
In stock
50mg
$551.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & MSDS

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Chemical structure

A 419259 trihydrochloride

A 419259 trihydrochloride Dilution Calculator

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Chemical Properties

Cas No. 1435934-25-0 SDF Download SDF
Chemical Name 7-((1r,4r)-4-(4-methylpiperazin-1-yl)cyclohexyl)-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine trihydrochloride
Canonical SMILES CN1CCN([[email protected]@]2([H])CC[[email protected]@](N3C=C(C(C3=NC=N4)=C4N)C5=CC=C(OC6=CC=CC=C6)C=C5)([H])CC2)CC1.Cl.Cl.Cl
Formula C29H37Cl3N6O M.Wt 592
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
Physical Appearance A crystalline solid Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

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].

Reference:
[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.