Drug intelligence / Profile preview

PD173955

Development stage
Preclinical
Lead developer
Memorial Sloan Kettering Cancer Center
Modality
Small Molecules
Administration
Oral
01

Overview

PD173955 is an experimental small molecule inhibitor of several tyrosine kinases. It is a potent ATP‐competitive inhibitor of Bcr-Abl (IC50 = 1–2 nM), Src (IC50 = 22 nM), and Yes kinases. It also inhibits c-Kit autophosphorylation at nanomolar concentrations. Mechanistically, it binds to the ATP-binding pocket of these kinases and can inhibit both open and closed conformations of the activation loop in Abl kinase. PD173955 has demonstrated strong antiproliferative effects in chronic myelogenous leukemia (CML) cell lines and other cancer models by inducing cell cycle arrest in G1 or M phase depending on concentration. The compound was developed as a research tool for studying kinase signaling pathways and as a potential lead for anticancer drug development but has not advanced to clinical use due to limited development beyond preclinical studies[1][4][5][6][7].

Other names
6-(2,6-dichlorophenyl)-8-methyl-2-{[3-(methylthio)phenyl]amino}pyrido[2,3-d]pyrimidin-7(8H)-one6-(2,6-dichlorophenyl)-8-methyl-2-(3-methylsulfanylanilino)pyrido[2,3-d]pyrimidin-7-oneCHEBI:49791DTXSID90332241DTXSID-90332241DTXSID 90332241
02

Targets

LCK (Proto-oncogene tyrosine-protein kinase Lck)SRC (Proto-oncogene tyrosine-protein kinase Src)YES1 (YES proto-oncogene 1 tyrosine kinase)KIT (c-KIT proto-oncogene receptor tyrosine kinase)ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)

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