| Identification | Back Directory | [Name]
1H-Indazol-4-amine, N-[(4-methyl-2-nitrophenyl)methyl]-6-(trifluoromethyl)- | [CAS]
2490672-92-7 | [Synonyms]
TDO-IN-1
1H-Indazol-4-amine, N-[(4-methyl-2-nitrophenyl)methyl]-6-(trifluoromethyl)- | [Molecular Formula]
C16H13F3N4O2 | [MOL File]
2490672-92-7.mol | [Molecular Weight]
350.3 |
| Chemical Properties | Back Directory | [Boiling point ]
518.1±50.0 °C(Predicted) | [density ]
1.478±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
13.28±0.40(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
TDO-IN-1 is an orally active and selective inhibitor of tryptophan 2,3-dioxygenase (TDO), shows excellent selectivity over indoleamine-2,3-dioxygenase (IDO), with an IC50 value of 0.62 μM (IDO). TDO-IN-1 reverse the local immune tolerance of tumor tissue to inhibit tumor growth in vivo[1]. | [in vivo]
TDO-IN-1 (HT-28) (25 mg/kg; p.o.; once daily; 9 d) improve the effect of tumor immunotherapy of CT26 tumor expressing TDO, substantially inhibits the proliferation of CT26 tumors in mice[1].
| Animal Model: | CT-26 allograft BALB/c mice (6-8 weeks old, female)[1] | | Dosage: | 12.5, 25, and 50 mg/kg | | Administration: | Oral gavage; once daily; 9 days | | Result: | Resulted significant reduction in tumor weight and volume in mice, with the tumor volume inhibiton rate of 76.93%.
Reduced the expression of Foxp3 and enhance the expression of CD8 and TNF-α in tumor tissue to increase the immune response of tumor-bearing mice. |
| [References]
[1] Huo C, et al. 4,6-Disubstituted-1H-Indazole-4-Amine derivatives with immune-chemotherapy effect and in vivo antitumor activity. Eur J Med Chem. 2022 Nov 5;241:114625. DOI:10.1016/j.ejmech.2022.114625 |
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