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Ezatiostat

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Chemical Structure| 168682-53-9 同义名 : TLK199;TER199(free base);Terrapin 199;Telintra;TER199
CAS号 : 168682-53-9
货号 : A178200
分子式 : C27H35N3O6S
纯度 : 98%
分子量 : 529.648
MDL号 : MFCD27982957
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(198.24 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

无水乙醇: 100 mg/mL(188.8 mM)，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇
动物实验配方：
生物活性
描述 Myelodysplastic syndrome (MDS) is a clonal stem cell disorder resulting in bone marrow failure and variable cytopenias. While Glutathione S-transferase P1-1 (GSTpi) contributes to the regulation of cell proliferation. Ezatiostat, a tripeptide analog of glutathione, is a selective and orally active inhibitor of GSTP1-1 having the potential for MDS treatment. Ezatiostat causes dissociation of GSTP1-1 from the jun-N-terminal kinase/c-Jun (JNK/JUN) complex, leading to JNK activation by phosphorylation. Activated JNK phosphorylates c-JUN, which ultimately results in the stimulation of all myeloid lineages hematopoietic progenitor’s proliferation and maturation[3]. Chronic exposure of a resistant clone of an HL60 tumor cell line to ezatiostat resulted in elevated activities of c-Jun NH2 terminal kinase (JNK1) and ERK1/ERK2, and allowed the cells to proliferate under stress conditions that induced high levels of apoptosis in the wild type cells. In vivo, administration of ezatiostat stimulated both lymphocyte production and bone marrow progenitor proliferation[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.89mL

0.38mL

0.19mL

9.44mL

1.89mL

0.94mL

18.88mL

3.78mL

1.89mL
参考文献

[1]Galili N, Tamayo P, et al. Prediction of response to therapy with ezatiostat in lower risk myelodysplastic syndrome. J Hematol Oncol. 2012 May 6;5:20.

[2]Raza A, Galili N, et al. A phase 2 randomized multicenter study of 2 extended dosing schedules of oral ezatiostat in low to intermediate-1 risk myelodysplastic syndrome. Cancer. 2012 Apr 15;118(8):2138-47.

[3]Galili N, Tamayo P, Botvinnik OB, Mesirov JP, Brooks MR, Brown G, Raza A. Prediction of response to therapy with ezatiostat in lower risk myelodysplastic syndrome. J Hematol Oncol. 2012 May 6;5:20

[4]Ruscoe JE, Rosario LA, et al. Pharmacologic or genetic manipulation of glutathione S-transferase P1-1 (GSTpi) influences cell proliferation pathways. J Pharmacol Exp Ther. 2001 Jul;298(1):339-45