A 419259

• CAT Number: I003339
• CAS Number: 364042-47-7
• Molecular Formula: C29H34N6O
• Molecular Weight: 482.62
• Purity: ≥95%
• Synonyms: 7-((1r,4r)-4-(4-methylpiperazin-1-yl)cyclohexyl)-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine
• Target: Apoptosis
• Solubility: 10 mM in DMSO
• Storage: Store at -20℃
• IC50: 9 nM (Src); <3 nM (Lck); <3 nM (Lyn); 3 uM (Abl) [1]
• IUPAC Name: 7-[4-(4-methylpiperazin-1-yl)cyclohexyl]-5-(4-phenoxyphenyl)pyrrolo[2,3-d]pyrimidin-4-amine
• InChI: InChI=1S/C29H34N6O/c1-33-15-17-34(18-16-33)22-9-11-23(12-10-22)35-19-26(27-28(30)31-20-32-29(27)35)21-7-13-25(14-8-21)36-24-5-3-2-4-6-24/h2-8,13-14,19-20,22-23H,9-12,15-18H2,1H3,(H2,30,31,32)
• InChIKey: FDVSOQRNTAPCHB-UHFFFAOYSA-N
• SMILES: CN1CCN(CC1)C2CCC(CC2)N3C=C(C4=C(N=CN=C43)N)C5=CC=C(C=C5)OC6=CC=CC=C6

A 419259 (Cat.No:I003339) is a small molecule inhibitor of protein kinase D (PKD), a serine/threonine kinase involved in diverse cellular processes such as signal transduction, gene expression, and vesicular trafficking. It has shown promising results in preclinical studies as a potential therapeutic agent for various diseases, including cancer and cardiovascular disorders.

Reference

[1]. Wilson MB, et al. Selective pyrrolo-pyrimidine inhibitors reveal a necessary role for Src family kinases in Bcr-Abl signal transduction and oncogenesis. Oncogene. 2002 Nov 21;21(53):8075-88.

[2]. Zhang X, et al. c-Yes Tyrosine Kinase Is a Potent Suppressor of ES Cell Differentiation and Antagonizes the Actions of Its Closest Phylogenetic Relative, c-Src. ACS Chem Biol. 2013 Aug 15.

[3]. Zhang Q, et al. SRC family kinases mediate epidermal growth factor receptor ligand cleavage, proliferation, and invasion of head and neck cancer cells. Cancer Res. 2004 Sep 1;64(17):6166-73.