生物活性

• 靶点

  Hck IC50:5nM

  p56lck IC50:4nM

  p59fynT IC50:5nM

  Src IC50:100nM

• 描述Src and Src-family protein kinases are proto-oncogenes that play key roles in cell morphology, motility, proliferation, and survival^[3]. PP2 is a reversible and ATP-competitive Src family kinases inhibitor with IC50s of 4 and 5 nM for Lck and Fyn, respectively^[4]. At 10 μM, the effect of PP2 on cellular proliferation is not significant, indicating that, at this low concentration, the effect of PP2 on Gemcitabine cytotoxicity does not simply reflect a direct antiproliferative effect, but rather a potentiation of Gemcitabine-induced cytotoxicity. Above 20 μM, growth is increasingly suppressed, a finding consistent with reports in other human cancer cell lines. The tumor growth inhibition rate is 25% in the PP2 treatment group and 5% in the Gemcitabine treatment group (P>0.05). PP2 is the most widely used commercially available Src family kinase inhibitor. PP2 inhibits Src family kinase activity with IC50 of ~5 nM in vitro, concentrations to 10 μM are often necessary to achieve complete Src family kinase inhibition in cell culture^[5].
• 细胞研究
• Cell Data

  Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
  8701-BC cells	10 μM	Function assay	-	Proapoptotic activity against 8701-BC cells at 10 uM by PARP assay	16509573
  A431 cells	-	Function assay	-	Inhibitory effect on phospho-Src/nonphospho after EGF (100 uM) stimulation of A431 cells, IC50=17 μM	15109642
  A431 cells	10 μM	Function assay	-	Inhibition of Src autophosphorylation of Y419 in A431 cells at 10 uM	16509573

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• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT01434472	Post-Transplant Lymphoprolifer... more >>ative Disorder Recurrent Adult Diffuse Large Cell Lymphoma Recurrent B-Cell Non-Hodgkin Lymphoma Recurrent Burkitt Lymphoma Refractory B-Cell Non-Hodgkin Lymphoma Refractory Burkitt Lymphoma Refractory Diffuse Large B-Cell Lymphoma Collapse <<	Phase 2	Recruiting	September 24, 2022	United States, Washington ... more >> Fred Hutch/University of Washington Cancer Consortium Recruiting Seattle, Washington, United States, 98109 Contact: Ajay K. Gopal    206-288-2037    agopal@u.washington.edu    Principal Investigator: Ajay K. Gopal Collapse <<
  NCT00438880	Adult Non-Hodgkin Lymphoma ... more >> Extranodal Marginal Zone Lymphoma of Mucosa-Associated Lymphoid Tissue Nodal Marginal Zone Lymphoma Recurrent Adult Diffuse Large Cell Lymphoma Recurrent Grade 1 Follicular Lymphoma Recurrent Grade 2 Follicular Lymphoma Recurrent Grade 3 Follicular Lymphoma Recurrent Mantle Cell Lymphoma Recurrent Marginal Zone Lymphoma Recurrent Small Lymphocytic Lymphoma Splenic Marginal Zone Lymphoma Waldenstrom Macroglobulinemia Collapse <<	Phase 1 Phase 2	Completed	-	United States, Iowa ... more >> University of Iowa/Holden Comprehensive Cancer Center Iowa City, Iowa, United States, 52242 United States, Minnesota Mayo Clinic Rochester, Minnesota, United States, 55905 Collapse <<
  NCT00119392	B-cell Chronic Lymphocytic Leu... more >>kemia Nodal Marginal Zone B-cell Lymphoma Recurrent Adult Burkitt Lymphoma Recurrent Adult Diffuse Large Cell Lymphoma Recurrent Adult Diffuse Mixed Cell Lymphoma Recurrent Adult Diffuse Small Cleaved Cell Lymphoma Recurrent Adult Grade III Lymphomatoid Granulomatosis Recurrent Adult Immunoblastic Large Cell Lymphoma Recurrent Adult Lymphoblastic Lymphoma Recurrent Grade 1 Follicular Lymphoma Recurrent Grade 2 Follicular Lymphoma Recurrent Grade 3 Follicular Lymphoma Recurrent Mantle Cell Lymphoma Recurrent Marginal Zone Lymphoma Recurrent Small Lymphocytic Lymphoma Splenic Marginal Zone Lymphoma Waldenström Macroglobulinemia Collapse <<	Phase 2	Completed	-	United States, Washington ... more >> Fred Hutchinson Cancer Research Center/University of Washington Cancer Consortium Seattle, Washington, United States, 98109 Collapse <<

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