79756-69-7|TPI-1|CsnPharm

CAS No.: 79756-69-7

TPI-1 Catalog No. CSN20445

Synonyms: Tyrosine Phosphatase Inhibitor 1

TPI-1 is a protein tyrosine phosphatase inhibitor with IC50 of 40nM increased SHP1 phospho-substrates (pLck-pY394, pZap70 and pSlp76) in Jurkat T cells but had little effects on pERK1/2 or pLck-pY505 regulated by phosphatases SHP2 or CD45, respectively. TPI-1 was shown to be more effective than sodium stibogluconate in SHP1 inhibition, immune cell activation and anti-tumor action.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述TPI-1 is a selective SHP-1 inhibitor with IC50 value of 40nM. It dose-dependently increased SHP-1 phospho-substrates (pLck-pY394, pZap70, and pSlp76) in Jurkat T cells at concentration<3μg/ml but had little effects on p-ERK1/2 or pLck-pY505 regulated by phosphatases SHP-2 or CD45, respectively. TPI-1 induced both mouse splenic-IFN-γ⁺ cells and IFN-γ⁺ cells in human peripheral blood in vitro. Significantly, TPI-1 inhibited the growth of B16 melanoma tumors in mice by 83% (but not in athymic nude mice with T cell deficiency) at a tolerated oral dose in a T cell-dependent manner but had little effects on B16 cell growth in culture. TPI-1 also inhibited B16 tumor growth and prolonged tumor mice survival as a tolerated s.c. agent^[2].
动物研究
剂量
Mice: 1 mg/kg - 10 mg/kg^[1] (s.c.)

给药途径
s.c.
参考文献

动物研究
剂量	Mice: 1 mg/kg - 10 mg/kg^[1] (s.c.)
给药途径	s.c.

[1] Kundu S, Fan K, 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.
[2] Kundu S, Fan K, Cao M, Lindner DJ, Zhao ZJ, Borden E, Yi T. 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. doi: 10.4049/jimmunol.0903562. Epub 2010 Apr 26. PMID: 20421638; PMCID: PMC3049920.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.9513 mL
- 19.7565 mL
- 39.5131 mL
- 5 mM
- 0.7903 mL
- 3.9513 mL
- 7.9026 mL
- 10 mM
- 0.3951 mL
- 1.9757 mL
- 3.9513 mL

技术信息

CAS号

79756-69-7

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C12H6Cl2O2

运输

蓝冰

分子量

253.08

别名

Tyrosine Phosphatase Inhibitor 1

溶解度

DMSO	51.0 mg/mL (201.5 mM)
Water	Insoluble
Ethanol	10.0 mg/mL (39.5 mM)

动物实验配方

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