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Ezatiostat

现货
Catalog No.
A8225
(GST) P1-1抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 860.00
现货
5mg
¥ 780.00
现货
10mg
¥ 1,310.00
现货
25mg
¥ 2,280.00
现货
50mg
¥ 3,530.00
现货
100mg
¥ 6,000.00
现货

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Background

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

Physical AppearanceA solid
StorageStore at -20°C
M.Wt529.65
Cas No.168682-53-9
FormulaC27H35N3O6S
SynonymsTER199;TLK199;Telintra
Solubility≥26.5mg/mL in DMSO, ≥42.6 mg/mL in EtOH, <2.02 mg/mL in H2O
Chemical Nameethyl (2S)-2-amino-5-[[(2R)-3-benzylsulfanyl-1-[[(1R)-2-ethoxy-2-oxo-1-phenylethyl]amino]-1-oxopropan-2-yl]amino]-5-oxopentanoate
SDFDownload SDF
Canonical SMILESCCOC(=O)C(CCC(=O)NC(CSCC1=CC=CC=C1)C(=O)NC(C2=CC=CC=C2)C(=O)OCC)N
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

生物活性

Description Ezatiostat(TER199;TLK199)是谷胱甘肽S转移酶(GST)P1-1的谷胱甘肽类似物抑制剂。
靶点 Gutathione S-transferase          
IC50            

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