Home>>Peptides>>Ezatiostat

Ezatiostat Sale

(Synonyms: TER199;TLK199;Telintra) 目录号 : GC18095

An inhibitor of GSTP1-1

Ezatiostat Chemical Structure

Cas No.:168682-53-9

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥704.00
现货
5mg
¥588.00
现货
10mg
¥924.00
现货
25mg
¥1,512.00
现货
50mg
¥2,961.00
现货
100mg
¥4,799.00
现货

电话:400-920-5774 Email: sales@glpbio.cn

Customer Reviews

Based on customer reviews.

Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

View current batch:

产品描述

Ezatiostat is a synthetic tripeptide analog of glutathione that inhibits the glutathione S-transferase P1-1 (GSTP1-1) [1].
Ezatiostat is a glutathione analog prodrug that has been shown to stimulate the proliferation of myeloid precursors. Ezatiostat is metabolized to TLK117 which shows selectivity to inhibit and bind to glutathione S-transferase P1-1 (GST P1-1). In addition, ezatiostat could activate the caspase-dependent pathway that help inhibit the emergence of malignant clones and may also contribute to apoptotic death and elimination by increasing reactive oxygen species (ROS) in dysplastic cells.
Ezatiostat has shown great stimulatory activity in vitro in human bone marrow progenitor cultures, as well as in several preclinical models of myelopoiesis in vivo. A multidose-escalation study of ezatiostat was performed for the treatment of myelodysplastic syndrome. Patients received 10 dose levels of ezatiostat tablets on days 1 to 7 of a 21-day cycle for a maximum of 8 cycles. Forty-five patients with low to intermediate-2 International Prognostic Scoring System risk myelodysplastic syndrome were enrolled. 17 hematologic improvement (HI) responses by International Working Group criteria were observed at dose range of 200 to 6000 mg/day , wherein 11 HI responses at dose range of 4000 to 6000 mg/day [1].
In randomized multicenter study of 2 extended dosing schedules of oral ezatiostat in low to intermediate-1 risk myelodysplastic syndrome. Patients were randomized by 1 stratification factor-baseline cytopenia to 1 of 2 extended dosing schedules. In general, 11 of 38 (29%) HI-Erythroid (HI-E) response was observed in patients who were red blood cell (RBC) transfusion-dependen. The median duration of HI-E response was 34 weeks. Ezatiostat is proven to cause clinically significant and sustained reduction in RBC transfusions, transfusion independence and multilineage responses in MDS patients [2].
References:
[1]. Raza A, Galili N, Smith S, et al. Phase 1 multicenter dose-escalation study of ezatiostat hydrochloride (TLK199 tablets), a novel glutathione analog prodrug, in patients with myelodysplastic syndrome. Blood, 2009, 113(26): 6533-6540.
[2]. Raza A, Galili N, Smith SE, 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, 118(8): 2138-2147.

Chemical Properties

Cas No. 168682-53-9 SDF
别名 TER199;TLK199;Telintra
化学名 ethyl (2S)-2-amino-5-[[(2R)-3-benzylsulfanyl-1-[[(1R)-2-ethoxy-2-oxo-1-phenylethyl]amino]-1-oxopropan-2-yl]amino]-5-oxopentanoate
Canonical SMILES CCOC(=O)C(CCC(=O)NC(CSCC1=CC=CC=C1)C(=O)NC(C2=CC=CC=C2)C(=O)OCC)N
分子式 C27H35N3O6S 分子量 529.65
溶解度 ≥ 26.5mg/mL in DMSO, ≥ 42.6 mg/mL in EtOH 储存条件 Store at -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

制备储备液
1 mg 5 mg 10 mg
1 mM 1.888 mL 9.4402 mL 18.8804 mL
5 mM 0.3776 mL 1.888 mL 3.7761 mL
10 mM 0.1888 mL 0.944 mL 1.888 mL
  • 摩尔浓度计算器

  • 稀释计算器

  • 分子量计算器

质量
=
浓度
x
体积
x
分子量
 
 
 
*在配置溶液时,请务必参考产品标签上、MSDS / COA(可在Glpbio的产品页面获得)批次特异的分子量使用本工具。

计算

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % saline
计算重置