Drug intelligence / Profile preview

PD-173952

Development stage
Preclinical
Modality
Small Molecules
01

Overview

PD-173952 is a potent and selective small molecule inhibitor of multiple tyrosine kinases. It is best characterized as an inhibitor of the Src family kinases (notably Lyn, Abl/Bcr-Abl, and Csk), with reported IC50 values of 0.3 nM for Lyn kinase, 1.7 nM for Abl kinase (including Bcr-Abl fusion protein), and 6.6 nM for Csk kinase[3][5][6]. It also inhibits Myt1 kinase[1][2]. By targeting these kinases, especially Bcr-Abl and Src family members implicated in cancer cell proliferation and survival pathways, PD‑173952 induces apoptosis in Bcr-Abl-dependent hematopoietic cells and has been studied primarily as an experimental agent in oncology research—particularly chronic myelogenous leukemia (CML) and other malignancies where aberrant tyrosine kinase signaling drives disease progression[5][8]. The compound belongs to the pyridopyrimidinone chemical class.

Other names
6-(2,6-dichlorophenyl)-8-methyl-2-(4-morpholin-4-ylanilino)pyrido[2,3-d]pyrimidin-7-one6-(2,6-Dichlorophenyl)-8-methyl-2-(4-morpholinylphenylamino)-8H-pyrido[2,3-d]pyrimidin-7-one
02

Targets

LYN (LYN proto-oncogene, Src family tyrosine kinase)PKMYT1 (Protein kinase membrane associated tyrosine/threonine 1)CSK (C-terminal Src kinase)ABL2 (ABL proto-oncogene 2, non-receptor tyrosine kinase)

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