A 419259 (trihydrochloride)

Cas No.:	1435934-25-0
Chemical Name:	7-[trans-4-(4-methyl-1-piperazinyl)cyclohexyl]-5-(4-phenoxyphenyl )-7h-pyrrolo[2,3-d]pyrimidin-4-amine Trihydrochloride
Synonyms:	7-[trans-4-(4-Methyl-1-piperazinyl)cyclohexyl]-5-(4-phenoxyphenyl )-7H-pyrrolo[2,3-d]pyrimidin-4-amine trihydrochloride;A 419259 trihydrochloride;A-419259 trihydrochloride;RK 20449 trihydrochloride;RK-20449 trihydrochloride;A 419259 (trihydrochloride)
SMILES:	NC1=C2C(N([C@H]3CC[C@H](N4CCN(C)CC4)CC3)C=C2C5=CC=C(OC6=CC=CC=C6)C=C5)=NC=N1.[H]Cl.[H]Cl.[H]Cl
Formula:	C29H37Cl3N6O
M.Wt:	592.002683401108
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

A 419259 trihydrochloride is a Src family kinases inhibitor with IC50s of 9 nM, 3 nM and 3 nM for Src, Lck and Lyn, respectively.

In Vitro:

A 419259 Trihydrochloride is a second-generation pyrrolo-pyrimidine designed to enhance selectivity towards the Src family relative to other cytoplasmic tyrosine kinases. A-419259 inhibits K-562 cells with an IC50 between 0.1 and 0.3 μM, and Meg-01 proliferation with an IC50 of approximately 0.1 μM. A-419259 also potently induces apoptosis in K-562 cells beginning at 0.1 μM and increasing in a dose-dependent manner. PP2 inhibits Src kinase autophosphorylation in both Ph+ cell lines (K-562 and Meg-01) with an IC50 between 3 and 10 μM, while A-419259 blocks kinase activation between 0.1 and 0.3 μM. A-419259 strongly inhibits DAGM/Bcr-Abl cell proliferation in the absence of IL-3 with an IC50 between 0.1 and 0.3 μM[1]. A-419259 is a broad-spectrum pyrrolo-pyrimidine inhibitor, and blocks proliferation and induces apoptosis in CML cell lines. A-419259 inhibits overall SFK activity in K562 and other CML cell lines with an IC50 value of 0.1-0.3 μM[2].