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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.

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TDO-IN-1 Chemical Structure

TDO-IN-1 Chemical Structure

CAS No. : 2490672-92-7

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5 mg USD 350 In-stock
10 mg USD 550 In-stock
25 mg USD 1100 In-stock
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TDO-IN-1 Related Antibodies

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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].

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

TDO-IN-1 Related Antibodies
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].

MedChemExpress (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.
Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (285.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8547 mL 14.2735 mL 28.5470 mL
5 mM 0.5709 mL 2.8547 mL 5.7094 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8547 mL 14.2735 mL 28.5470 mL 71.3674 mL
5 mM 0.5709 mL 2.8547 mL 5.7094 mL 14.2735 mL
10 mM 0.2855 mL 1.4273 mL 2.8547 mL 7.1367 mL
15 mM 0.1903 mL 0.9516 mL 1.9031 mL 4.7578 mL
20 mM 0.1427 mL 0.7137 mL 1.4273 mL 3.5684 mL
25 mM 0.1142 mL 0.5709 mL 1.1419 mL 2.8547 mL
30 mM 0.0952 mL 0.4758 mL 0.9516 mL 2.3789 mL
40 mM 0.0714 mL 0.3568 mL 0.7137 mL 1.7842 mL
50 mM 0.0571 mL 0.2855 mL 0.5709 mL 1.4273 mL
60 mM 0.0476 mL 0.2379 mL 0.4758 mL 1.1895 mL
80 mM 0.0357 mL 0.1784 mL 0.3568 mL 0.8921 mL
100 mM 0.0285 mL 0.1427 mL 0.2855 mL 0.7137 mL
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TDO-IN-1 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TDO-IN-12490672-92-7Othersnitrobenzene-1H-indazoleselectivelocal immune toleranceHepG2Hepa1-6H22B16MOLM-13JurkatCT-26 allograft BALB/c miceInhibitorinhibitorinhibit

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