Ezatiostat
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Ezatiostat是一种合成的谷胱甘肽三肽类似物,抑制谷胱甘肽S转移酶P1-1(GSTP1-1)[1]。
Ezatiostat是一种谷胱甘肽类似物前药,可以刺激骨髓前体细胞增殖。Ezatiostat被代谢为TLK117,该代谢物选择性地结合并抑制谷胱甘肽S转移酶P1-1(GST P1-1)。此外,Ezatiostat能激活caspase依赖性的途径以抑制恶性克隆形成,并且还可以增加不典型增生细胞中的活性氧(ROS)以诱导细胞凋亡。
Ezatiostat在体外对人骨髓祖细胞具有显著的刺激活性,对某些体内的骨髓细胞生成临床前模型也显示出很强的刺激作用。在多剂量递增试验中,Ezatiostat用于治疗骨髓增生异常综合征。试验以21天为一个周期,最多持续8个周期,在每个周期的第1天到第7天,患者接受10种不同剂量水平的Ezatiostat片剂。入组骨髓增生异常综合征患者为45例,均在国际预后评分系统中属于低至中-2风险。在剂量范围为200 ~ 6000 mg/day时,基于国际工作组标准,17例患者出现了血液学改善(HI),其中,11例HI出现在4000 ~ 6000 mg/day的剂量范围下[1]。
在随机多中心试验中,对中-1风险的骨髓增生异常综合征患者采用2种延长的Ezatiostat给药方案。以血细胞减少为分层因素,患者被分配到第一或第二个延长的给药方案。在一般情况下,红细胞(RBC)输血依赖患者的红系反应(HI-E)率为29%(38例中11例)。HI-E反应持续时间的中位数为34周。Ezatiostat在临床中显著并持续减少MDS患者的红细胞输血、输血独立性以及多向应答[2]。
参考文献:
[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.
- 1. Zhao S, Wang B, et al. "Contributions of enzymes and gut microbes to biotransformation of perfluorooctane sulfonamide in earthworms (Eisenia fetida)." Chemosphere. 2019 Aug 19;238:124619. PMID:31450114
- 2. Zhang Q, Liu RX, et al. "Exosomal transfer of p-STAT3 promotes acquired 5-FU resistance in colorectal cancer cells." J Exp Clin Cancer Res. 2019 Jul 19;38(1):320. PMID:31324203
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 529.65 |
Cas No. | 168682-53-9 |
Formula | C27H35N3O6S |
Synonyms | TER199;TLK199;Telintra |
Solubility | ≥26.5 mg/mL in DMSO; insoluble in H2O; ≥42.6 mg/mL in EtOH |
Chemical Name | ethyl (2S)-2-amino-5-[[(2R)-3-benzylsulfanyl-1-[[(1R)-2-ethoxy-2-oxo-1-phenylethyl]amino]-1-oxopropan-2-yl]amino]-5-oxopentanoate |
SDF | Download SDF |
Canonical SMILES | CCOC(=O)C(CCC(=O)NC(CSCC1=CC=CC=C1)C(=O)NC(C2=CC=CC=C2)C(=O)OCC)N |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。溶液形式一般不宜长期储存,请尽快用完。 |
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 |
质量控制和MSDS
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