Ezatiostat (Synonyms: TER199;TLK199;Telintra) |
| カタログ番号GC18095 |
An inhibitor of GSTP1-1
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 168682-53-9
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 168682-53-9 | SDF | |
| 同義語 | TER199;TLK199;Telintra | ||
| 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 | ||
| Canonical SMILES | CCOC(=O)C(CCC(=O)NC(CSCC1=CC=CC=C1)C(=O)NC(C2=CC=CC=C2)C(=O)OCC)N | ||
| Formula | C27H35N3O6S | M.Wt | 529.65 |
| 溶解度 | ≥ 26.5mg/mL in DMSO, ≥ 42.6 mg/mL in EtOH | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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