| CAS |
No.79756-69-7 |
| 英文名称 |
TPI-1 |
| 分子式 |
C12H6Cl2O2 |
| 分子量 |
253.08 |
| 溶解性 |
Soluble in DMSO ≥5mg/mL(Need ultrasonic) |
| 纯度 |
≥98% |
| 外观(性状) |
Solid |
| 储存条件 |
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| EC |
EINECS 830-085-7 |
| MDL |
MFCD00448731 |
| SMILES |
C1=CC(=C(C=C1Cl)C2=CC(=O)C=CC2=O)Cl |
| InChIKey |
ZKHFYORNAYYOTM-UHFFFAOYSA-N |
| InChI |
InChI=1S/C12H6Cl2O2/c13-7-1-3-11(14)9(5-7)10-6-8(15)2-4-12(10)16/h1-6H |
| PubChem CID |
948589 |
| 靶点 |
SHP-1 |
| 通路 |
Metabolic Enzyme&Protease |
| 背景说明 |
是一种有效的 SHP-1 抑制剂，具有抗癌的活性。 |
| 生物活性 |
TPI-1， also known as Tyrosine Phosphatase Inhibitor 1， is a SHP-1 inhibitor; inhibits recombinant SHP-1 with an IC50 of 40 nM.[1] |
| IC50 |
IC50: 40 nM (recombinant SHP-1)[1] |
| In Vitro |
SHP-1 has been implicated as a potential cancer therapeutic target. TPI-1 is effective starting at 10 ng/mL in increasing SHP-1 phospho-substrates pLck-pY394. TPI-1 selectively increases SHP-1 phospho-substrates (pLck-pY394， pZap70 and pSlp76) in Jurkat T cells but has little effects on pERK1/2 or pLck-pY505. TPI-1 induces mouse splenic-IFNγ+ cells and induces IFNγ+ cells in human peripheral blood[1]. |
| In Vivo |
TPI-1 inhibits the growth of B16 melanoma tumors in mice at a tolerated oral dose in a T cell-dependent manner but has little effects on B16 cell growth in culture. TPI-1 thus also increases pLck-pY394 and IFNγ+ cells in mice. TPI-1 also inhibits B16 tumor growth and prolongs tumor mice survival as a tolerated s.c. agent[1]. |
| 动物实验 |
Mice: For in vivo induction of pLck-pY394 and IFNγ+ cells in mice， C57BL/6J mice are treated with PBS or TPI-1 (1 or 3 mg/kg， s.c.) for 4 days. Spleens are harvested one hour post-treatment on day 4 and processed into splenocytes， which are used for assessing pLck-pY394 levels by SDS-PAGE/Western blotting and for quantification of IFNγ+ cells by ELISPOT assays. Mice are also treated with TPI-1 (10 mg/kg， daily， s.c.) to evaluate the toxicity of the compounds in vivo[1]. |
| 数据来源文献 |
[1]. Kundu S， et al. Novel SHP-1 inhibitors tyrosine phosphatase inhibitor-1 and analogs with preclinical anti-tumor activities as tolerated oral agents. J Immunol. 2010 Jun 1;184(11):6529-36. |
| 规格 |
1mg 2mg 5mg 10mg 25mg |
| 单位 |
瓶 |
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