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TDO-IN-1

Catalog No. T61202   CAS 2490672-92-7

TDO-IN-1 is an orally active, potent, and selective inhibitor of tryptophan 2,3-dioxygenase (TDO), which inhibits indoleamine-2,3-dioxygenase.TDO-IN-1 has antitumor activity and is able to act by reversing local immune tolerance in tumor tissues.

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TDO-IN-1 Chemical Structure
TDO-IN-1, CAS 2490672-92-7
Pack Size Availability Price/USD Quantity
1 mg In stock $ 117.00
2 mg In stock $ 169.00
5 mg In stock $ 289.00
10 mg In stock $ 455.00
25 mg In stock $ 892.00
50 mg In stock $ 1,450.00
100 mg In stock $ 1,970.00
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Purity: 99.86%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description TDO-IN-1 is an orally active, potent, and selective inhibitor of tryptophan 2,3-dioxygenase (TDO), which inhibits indoleamine-2,3-dioxygenase.TDO-IN-1 has antitumor activity and is able to act by reversing local immune tolerance in tumor tissues.
Targets&IC50 Hepa1-6:5.08 μM, TDO:0.62 μM, Jurkat cells:7.25 μM, MOLM-13:3.43 μM, B16:37.39 μM, H22:1.34 μM, HepG2 cells:0.54 μM
In vitro TDO-IN-1 (HT-28) demonstrates a significant tumoricidal effect on different tumor lines when treated at concentrations ranging from 0 to 100 μM for 24 hours. The IC50 values for various tumor cell lines are as follows: 0.54 μM (HepG2), 5.08 μM (Hepa1-6), 1.34 μM (H22), 37.39 μM (B16), 3.43 μM (MOLM-13), and 7.25 μM (Jurkat)[1].Moreover, TDO-IN-1 (0-100 μM; 24 h) exhibits minimal cytotoxic activity against normal cells (HEK 293 cells) when the concentration is below 10 μM[1].
In vivo Administered orally at a dose of 25 mg/kg once daily for 9 days, TDO-IN-1 (HT-28) enhances the efficacy of tumor immunotherapy in CT26 tumors expressing TDO. This treatment substantially inhibits the proliferation of CT26 tumors in mice[1].
Molecular Weight 350.3
Formula C16H13F3N4O2
CAS No. 2490672-92-7

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 80 mg/mL (228.38 mM), Sonication is recommended.

TargetMolReferences and Literature

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.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library

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Keywords

TDO-IN-1 2490672-92-7 Others inhibitor inhibit

 

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