A 419259 - CAS 364042-47-7
Not Intended for Therapeutic Use. For research use only.
Category:
Inhibitor
Product Name:
A 419259
Catalog Number:
364042-47-7
Synonyms:
A419259; A-419259; RK 20449; RK20449; RK-20449
CAS Number:
364042-47-7
Description:
A-419259 is a potent inhibitor of Src family kinases. IC50 values for src, lck, blk, csk, fyn and lyn range between 15 and 50 nM.
Molecular Weight:
482.62
Molecular Formula:
C29H34N6O
COA:
Inquire
MSDS:
Inquire
Targets:
Src
Chemical Structure
CAS 364042-47-7 A 419259

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Reference Reading


1.An inhibitor-resistant mutant of Hck protects CML cells against the antiproliferative and apoptotic effects of the broad-spectrum Src family kinase inhibitor A-419259.
Pene-Dumitrescu T1, Peterson LF, Donato NJ, Smithgall TE. Oncogene. 2008 Nov 27;27(56):7055-69. doi: 10.1038/onc.2008.330. Epub 2008 Sep 15.
Chronic myelogenous leukemia (CML) is driven by Bcr-Abl, a constitutively active protein-tyrosine kinase that stimulates proliferation and survival of myeloid progenitors. Global inhibition of myeloid Src family kinase (SFK) activity with the broad-spectrum pyrrolo-pyrimidine inhibitor, A-419259, blocks proliferation and induces apoptosis in CML cell lines, suggesting that transformation by Bcr-Abl requires SFK activity. However, the contribution of Hck and other individual SFKs to Bcr-Abl signaling is less clear. Here, we developed an A-419259-resistant mutant of Hck by replacing the gatekeeper residue (Thr-338; c-Src numbering) in the inhibitor-binding site with a bulkier methionine residue (Hck-T338M). This substitution reduced Hck sensitivity to A-419259 by more than 30-fold without significantly affecting kinase activity in vitro. Expression of Hck-T338M protected K-562 CML cells and Bcr-Abl-transformed TF-1 myeloid cells from the apoptotic and antiproliferative effects of A-419259.