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PP2

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Chemical Structure| 172889-27-9 同义名 : -
CAS号 : 172889-27-9
货号 : A146866
分子式 : C15H16ClN5
纯度 : 98%
分子量 : 301.774
MDL号 : MFCD01568210
存储条件：

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(165.69 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

IP 2% DMSO+water 0.1 mg/mL clear

PO 0.5% CMC-Na 31 mg/mL suspension

生物活性
靶点

  • Fyn

    Fyn, IC50:5 nM

  • Lck

    LCK, IC50:4 nM
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
细胞系 浓度 检测类型 检测时间 活动说明 数据源
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
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... 展开 >>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 收起 << Phase 2 Recruiting September 24, 2022 United States, Washington ... 展开 >> 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 收起 <<
NCT00438880 Adult Non-Hodgkin Lymphoma ... 展开 >> 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 收起 << Phase 1 Phase 2 Completed - United States, Iowa ... 展开 >> University of Iowa/Holden Comprehensive Cancer Center Iowa City, Iowa, United States, 52242 United States, Minnesota Mayo Clinic Rochester, Minnesota, United States, 55905 收起 <<
NCT00119392 B-cell Chronic Lymphocytic Leu... 展开 >>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 收起 << Phase 2 Completed - United States, Washington ... 展开 >> Fred Hutchinson Cancer Research Center/University of Washington Cancer Consortium Seattle, Washington, United States, 98109 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.31mL

0.66mL

0.33mL

16.57mL

3.31mL

1.66mL

33.14mL

6.63mL

3.31mL
参考文献

[1]Robert Roskoski Jr. Src protein-tyrosine kinase structure and regulation. Biochem Biophys Res Commun. 2004. 324(4), 1155-64.

[2]Hanke JH, et al. Discovery of a novel, potent, and Src family-selective tyrosine kinase inhibitor. Study of Lck-and FynT-dependentT cell activation. J Biol Chem. 1996. 271(2), 695-701.

[3]Summy JM, et al. AP23846, a novel and highly potent Src family kinase inhibitor, reduces vascular endothelial growth factor and interleukin-8 expression in human solid tumor cell lines and abrogates downstream angiogenic processes. Mol Cancer Ther. 2005. 4(12), 1900-11.