| Chemical Properties | Back Directory | [Boiling point ]
533.2±50.0 °C(Predicted) | [density ]
1.502±0.06 g/cm3(Predicted) | [storage temp. ]
4°C, protect from light | [solubility ]
DMSO : 62.5 mg/mL (190.13 mM; Need ultrasonic) | [form ]
Solid | [pka]
-8.51±0.29(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
TRi-1 is a potent, specific and irreversible inhibitor of cytosolic thioredoxin reductase 1 (TXNRD1), with an IC50 of 12 nM. TRi-1 has little mitochondrial toxicity for anticancer therapy[1]. | [in vivo]
TRi-1 (10 mg/kg; i.v.; twice a day for 4 days or 5 mg/kg; i.p.; twice a week for 3 weeks) impaires growth and viability of human tumor xenografts and syngeneic mouse tumors[1]. | Animal Model: | SCID mice bearing established human FaDu cell xenografts[1] | | Dosage: | 10 mg/kg | | Administration: | Intravenous injection, twice a day for 4 days | | Result: | Resulted in decreased tumor growth compared to vehicle controls within four days with no signs of overt toxicity or changes in mouse weight relative to vehicle control.
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| Animal Model: | PyMT-MMTV mice that spontaneously develop malignant breast cancer tumors[1] | | Dosage: | 5 mg/kg | | Administration: | Intraperitoneal injection, twice a week for 3 weeks | | Result: | Impaired tumor growth, significantly reduced tumor volumes. |
| [storage]
4°C, protect from light | [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. DOI:10.1126/scitranslmed.aaf7444 |
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