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
InChIKey XZEJMVDCQZRHLN-UHFFFAOYSA-N
SMILES Cn1c(=O)c(-c2c(Cl)cccc2Cl)cc2cnc(Nc3ccc(N4CCOCC4)cc3)nc21

 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...

 PD173952Bioassay

View more

Name: Inhibitory activity against avian c-Src tyrosine kinase was determined.
Source: ChEMBL
Target: Proto-oncogene tyrosine-protein kinase Src
External Id: CHEMBL818902
Name: Inhibitory activity against mouse PDGF beta receptor tyrosine kinase
Source: ChEMBL
Target: Platelet-derived growth factor receptor beta
External Id: CHEMBL761279
Name: Kinase Inhibition Assay from Article 10.1021/jm000148t: "Synthesis and structure-acti...
Source: BindingDB
Target: N/A
External Id: BindingDB_593_1
Name: Rescue cell viability in cybrid cells with a genetic mutation in complex 1 of the mit...
Source: ICCB-Longwood/NSRB Screening Facility, Harvard Medical School
Target: N/A
External Id: HMS1315
Name: Inhibitory activity against SW-620 human colon adenocarcinoma cells was determined.
Source: ChEMBL
Target: SW-620
External Id: CHEMBL806228
Name: Inhibitory activity against HCT-8 human colon adenocarcinoma cells was determined.
Source: ChEMBL
Target: HCT-8
External Id: CHEMBL871950
Name: Kinase Assay from Article 10.1016/s0006-2952(00)00405-6: "Biochemical and cellular ef...
Source: BindingDB
Target: N/A
External Id: BindingDB_840_1
Name: Dicer-mediated maturation of pre-microRNA
Source: Center for Chemical Genomics, University of Michigan
Target: N/A
External Id: TargetID_659_CEMA
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 Synonyms

hms3263e07
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