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TDO-IN-1 

Cat. No.: HY-151425
Handling Instructions

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.

For research use only. We do not sell to patients.

TDO-IN-1 Chemical Structure

TDO-IN-1 Chemical Structure

CAS No. : 2490672-92-7

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Description

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].

IC50 & Target

IC50: 0.62 μM (tryptophan 2,3-dioxygenase, TDO)[1]

In Vitro

TDO-IN-1 (HT-28) (0-100 μM; 24 h) shows significant tumoricidal effect on different tumor lines, with IC50s of 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), respectively[1].
TDO-IN-1 (0-100 μM; 24 h) exhibits few cytotoxic activity against normal cells (HEK 293 cells) below 10 μM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

350.30

Formula

C16H13F3N4O2

CAS No.
SMILES

FC(C1=CC2=C(C(NCC3=CC=C(C)C=C3[N+]([O-])=O)=C1)C=NN2)(F)F

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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TDO-IN-1
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HY-151425
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