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305820-75-1

305820-75-1 structure
305820-75-1 structure
  • Name: PD173952
  • Chemical Name: 6-(2,6-dichlorophenyl)-8-methyl-2-(4-morpholin-4-ylanilino)pyrido[2,3-d]pyrimidin-7-one
  • CAS Number: 305820-75-1
  • Molecular Formula: C24H21Cl2N5O2
  • Molecular Weight: 482.36200
  • Catalog: Signaling Pathways Apoptosis Apoptosis
  • Create Date: 2016-11-30 03:12:38
  • Modify Date: 2025-08-26 18:10:27
  • 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].

Name 6-(2,6-dichlorophenyl)-8-methyl-2-(4-morpholin-4-ylanilino)pyrido[2,3-d]pyrimidin-7-one
Synonyms hms3263e07
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.  

Molecular Formula C24H21Cl2N5O2
Molecular Weight 482.36200
Exact Mass 481.10700
PSA 75.51000
LogP 4.36940
RIDADR NONH for all modes of transport
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