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| 5mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
Ezatiostat (formerly known as TER199; TLK199; Brand name: Telentra) is a glutathione analog inhibitor of glutathione S-transferase P1-1 (GSTP1-1). It was shown that an ezatiostat response profile contains two miRNAs that regulate expression of genes known to be implicated in MDS disease pathology. Remarkably, pathway analysis of the response profile revealed that the genes comprising the jun-N-terminal kinase/c-Jun molecular pathway, which is known to be activated by ezatiostat, are under-expressed in patients who respond and over-expressed in patients who were non-responders to the drug, suggesting that both the biology of the disease and the molecular mechanism of action of the drug are positively correlated.
| ln Vitro |
When ezatiostat dissociates the enzyme from the jun-N-terminal kinase/c-Jun (JNK/JUN) complex, phosphorylation of JNK results in JNK activation. Ezatiostat appears to have both malignant clone apoptosis and normal myeloid progenitor cell growth as therapeutic effects [1]. Selecting resistant clones of the HL60 tumor cell line through prolonged exposure to ezatiostat (TLK199) causes high levels of apoptosis in cells and increases the activity of c-Jun NH2-terminal kinase (JNK1) and ERK1/ERK2 in cells, allowing them to proliferate under stress conditions in comparison to wild type [2].
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| ln Vivo |
Ezatiostat (TLK199) administration increases the generation of lymphocytes and the proliferation of myeloid progenitor cells (colony forming units, granulocyte macrophages), but only in mice that are glutathione S-transferase P1-1 (GSTP1+/+) and not in GSTP1-/- animals. 2].
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| References |
[1]. Galili N, et al. Prediction of response to therapy with ezatiostat in lower risk myelodysplastic syndrome. J Hematol Oncol. 2012 May 6;5:20
[2]. Ruscoe JE, 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. |
| Molecular Formula |
C27H35N3O6S
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|---|---|
| Molecular Weight |
529.6483
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| CAS # |
168682-53-9
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| Related CAS # |
TLK117;152684-53-2;Ezatiostat hydrochloride;286942-97-0
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| SMILES |
O=C(OCC)[C@@H](N)CCC(N[C@@H](CSCC1=CC=CC=C1)C(N[C@@H](C2=CC=CC=C2)C(OCC)=O)=O)=O
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| InChi Key |
GWEJFLVSOGNLSS-FIXSFTCYSA-N
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| InChi Code |
InChI=1S/C27H35N3O6S/c1-3-35-26(33)21(28)15-16-23(31)29-22(18-37-17-19-11-7-5-8-12-19)25(32)30-24(27(34)36-4-2)20-13-9-6-10-14-20/h5-14,21-22,24H,3-4,15-18,28H2,1-2H3,(H,29,31)(H,30,32)/t21-,22-,24-/m0/s1
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| Chemical Name |
(S)-ethyl 2-amino-5-(((R)-3-(benzylthio)-1-(((S)-2-ethoxy-2-oxo-1-phenylethyl)amino)-1-oxopropan-2-yl)amino)-5-oxopentanoate
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| Synonyms |
TLK199; TLK-199; TLK 199; Ezatiostat; TER-199; TLK-199 hydrochloride; TER 199; TLK 199 hydrochloride; TER199; TLK199 hydrochloride; trade name: Telintra
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
Ethanol :≥ 100 mg/mL (~188.80 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (5.19 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.75 mg/mL (5.19 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.75 mg/mL (5.19 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8880 mL | 9.4402 mL | 18.8804 mL | |
| 5 mM | 0.3776 mL | 1.8880 mL | 3.7761 mL | |
| 10 mM | 0.1888 mL | 0.9440 mL | 1.8880 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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