PD173952

Modify Date: 2025-08-26 18:10:27

PD173952 Structure
PD173952 structure
Common Name PD173952
CAS Number 305820-75-1 Molecular Weight 482.36200
Density N/A Boiling Point N/A
Molecular Formula C24H21Cl2N5O2 Melting Point N/A
MSDS USA Flash Point N/A

 Use of PD173952


PD173952 is a tyrosine kinases inhibitor with IC50s of 0.3, 1.7 and 6.6 nM against Lyn, Abl and Csk, respectively. PD173952 is also a potent Myt1 kinase inhibitor with a Ki of 8.1 nM. PD173952 induces apoptosis[1][2].

 Names

Name 6-(2,6-dichlorophenyl)-8-methyl-2-(4-morpholin-4-ylanilino)pyrido[2,3-d]pyrimidin-7-one
Synonym More Synonyms

 PD173952 Biological Activity

Description PD173952 is a tyrosine kinases inhibitor with IC50s of 0.3, 1.7 and 6.6 nM against Lyn, Abl and Csk, respectively. PD173952 is also a potent Myt1 kinase inhibitor with a Ki of 8.1 nM. PD173952 induces apoptosis[1][2].
Related Catalog
Target

Lyn:0.3 nM (IC50)

Abl:1.7 nM (IC50)

Csk:6.6 nM (IC50)

Myt1:8.1 nM (Ki)

In Vitro PD173952 (0-1000 nM; 12 h) 以浓度依赖方式抑制 K562 细胞中 p210Bcr-Abl 和 CrkL 的酪氨酸磷酸化[1]。 PD173952 (0.5 μM; 1-4 days) 抑制 K562 细胞活力[1]。 PD173952 (0.5 μM; 24 and 48 h) 诱导 K562 和 MEG-01 细胞凋亡[1]。 Western Blot Analysis[1] Cell Line: K562 cells Concentration: 0, 25, 50, 100, 200, 500 and 1000 nM Incubation Time: 12 h Result: Inhibited tyrosine phosphorylation of p210Bcr-Abl and CrkL. Cell Viability Assay[1] Cell Line: K562 cells Concentration: 0.5 μM Incubation Time: 1-4 days Result: Caused cell death in a time-dependent manner. Western Blot Analysis[1] Cell Line: K562 and MEG-01 cells Concentration: 0.5 μM Incubation Time: 24 and 48 h Result: 85-kDa PARP fragment was detected.
References

[1]. Dorsey JF, et al. Interleukin-3 protects Bcr-Abl-transformed hematopoietic progenitor cells from apoptosis induced by Bcr-Abl tyrosine kinase inhibitors. Leukemia. 2002 Sep;16(9):1589-95.  

[2]. Wichapong K, et al. Application of docking and QM/MM-GBSA rescoring to screen for novel Myt1 kinase inhibitors. J Chem Inf Model. 2014 Mar 24;54(3):881-93.  

 Chemical & Physical Properties

Molecular Formula C24H21Cl2N5O2
Molecular Weight 482.36200
Exact Mass 481.10700
PSA 75.51000
LogP 4.36940

 Safety Information

RIDADR NONH for all modes of transport

 Articles1

More Articles
Identification of peptidic substrates for the human kinase Myt1 using peptide microarrays.

Bioorg. Med. Chem. 23 , 4936-42, (2015)

Myt1 kinase is a member of the Wee-kinase family involved in G2/M checkpoint regulation of the cell cycle. So far, no peptide substrate suitable for activity-based screening has been reported, hamperi...

 Synonyms

hms3263e07
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