| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
TRi-1 (also know nas TXNRD1 inhibitor 1) is a novel, potent, specific and irreversible inhibitor of cytosolic thioredoxin reductase 1 (TXNRD1) with anticancer potential activity. It showed 5- to 10-fold higher specificity for TXNRD1 over TXNRD2.
| ln Vitro |
In FaDu cells, TRi-1 (0.679 and 6.79 μM; 6 hours) potently stimulates JNK and p38 phosphorylation while having no effect on cellular glutathione (GSH) contents [1]. TRi-1 (2 μM) H2O2 is added to grown FaDu cells in a concentration- and time-dependent manner to create TRi-1 (0.1-10 μM; 0-10 h) [1]. TRi-1 at 10 nM.
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| ln Vivo |
TRi-1 (10 mg/kg; IV; twice daily for 4 days or 5 mg/kg; IP; twice weekly for 3 weeks) damages human tumor xenografts and syngeneic mice tumors
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| Cell Assay |
Western Blot Analysis [1]
Cell Types: FaDu Cell Tested Concentrations: 0.679 and 6.79 μM Incubation Duration: 6 h Experimental Results: Effective activation of JNK and p38 phosphorylation. -100 μM; 48 h) shows cytotoxicity to cancer cells [1]. Cytotoxicity assay[1] Cell Types: Leukemia, Non-Small Cell Lung Cancer, Central Nervous System, Colon, Melanoma, Ovarian, Kidney, Prostate, and Breast Cancer Cell Tested Concentrations: 10 nM-100 μM Incubation Duration: 48 hrs (hours) Experimental Results: Potency against each cell line tested was shown, with an average growth inhibition of 50% (GI50) of 6.31 μM. |
| Animal Protocol |
Animal/Disease Models: PyMT-MMTV mice that spontaneously develop malignant breast cancer tumors [1]
Doses: 5 mg/kg Route of Administration: intraperitoneal (ip) injection, twice a week for 3 weeks Experimental Results: Impaired tumor growth, significant tumor volume Zoom out. |
| References |
[1]. Stafford WC, et al. Irreversible inhibition of cytosolic thioredoxin reductase 1 as a mechanistic basis for anticancer therapy. Sci Transl Med. 2018 Feb 14;10(428). pii: eaaf7444.
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| Molecular Formula |
C12H9CLN2O5S
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|---|---|
| Molecular Weight |
328.728260755539
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| CAS # |
246020-68-8
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| SMILES |
ClC1C=CC(=CC=1)S(C1C(=CC=C(N=1)OC)[N+](=O)[O-])(=O)=O
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| Synonyms |
TRi-1 (TXNRD1 inhibitor 1); TRi 1 (TXNRD1 inhibitor-1); TRi1 (TXNRD 1 inhibitor 1)
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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) |
DMSO : ~62.5 mg/mL (~190.13 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.33 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 20.8 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: ≥ 2.08 mg/mL (6.33 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0420 mL | 15.2101 mL | 30.4201 mL | |
| 5 mM | 0.6084 mL | 3.0420 mL | 6.0840 mL | |
| 10 mM | 0.3042 mL | 1.5210 mL | 3.0420 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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