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680C91 is an orally active, selective tryptophan 2,3-dioxygenase (TDO) inhibitor with a Ki of 51 nM. TDO is the key enzyme of tryptophan catabolism. 680C91 can be used for the research of cancer immunotherapy and Alzheimer’s Disease.

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

680C91 Chemical Structure

680C91 Chemical Structure

CAS No. : 163239-22-3

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

680C91 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE 680C91

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  • Customer Review

Description

680C91 is an orally active, selective tryptophan 2,3-dioxygenase (TDO) inhibitor with a Ki of 51 nM. TDO is the key enzyme of tryptophan catabolism. 680C91 can be used for the research of cancer immunotherapy and Alzheimer’s Disease[1][2][3][4].

In Vitro

680C91 is a potent (Ki=51 nM) and selective TDO inhibitor with no inhibitory activity against indoleamine 2,3-dioxygenase, monoamine oxidase A and B, 5-HT uptake and 5-HT1A,1D,2A and 2C receptors at a concentration of 10 μM[2].
680C91 inhibits the catabolism of tryptophan by rat liver cells and rat liver perfused in situ[2].
Tdo2 could regulate cell proliferation and stimulate the expression of decidual marker Dtprp in the uterine stromal cells and decidual cells. Tdo2 inhibitor 680C91 also inhibits the prolifer ation activity of uterine decidual cells at 24 h[3].
Treatment of leiomyoma smooth muscle cell (LSMC) and myometrial smooth muscle cell (MSMC) spheroids with 680C91 (25 and 50 μM) significantly represses the expression of collagen type I (COL1A1) and type III (COL3A1) in a dose-dependent manner[4].

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

680C91 Related Antibodies

Cell Proliferation Assay[3]

Cell Line: Uterine stromal cells
Concentration: 0.01, 0.05, 0.1, 0.5, 1, 5, and 10 μM
Incubation Time: 24 hours
Result: The proliferation activity of stromal cells was significantly decreased at 5 and 10 μM.

Western Blot Analysis[4]

Cell Line: MSMC and LSMC
Concentration: 25 and 50 μM
Incubation Time: 48 hours
Result: Significantly reduced the expression of COL1A1 and COL3A1 in LSMC spheroids with no significant effect on expression of these proteins in MSMC spheroids.
In Vivo

680C91 (a dose of 15 mg/kg for acute treatment ) elevates tryptophan in brain[5].

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

Animal Model: Male C57Bl6/NCrl mice aged 13-18 weeks[5]
Dosage: 15 mg/kg
Administration: Administered per os
Result: Caused a significant increase in brain tryptophan.
Molecular Weight

238.26

Formula

C15H11FN2
CAS No.
Appearance

Solid

Color

Light yellow to brown

SMILES

FC1=CC2=C(C=C1)C(/C=C/C3=CC=CN=C3)=CN2
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 : 116.67 mg/mL (489.68 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 4.1971 mL 20.9855 mL 41.9710 mL
5 mM 0.8394 mL 4.1971 mL 8.3942 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.08 mg/mL (8.73 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.08 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.08 mg/mL (8.73 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.08 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.54%

SDS (476 KB)

COA (254 KB) HNMR (242 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
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 4.1971 mL 20.9855 mL 41.9710 mL 104.9274 mL
5 mM 0.8394 mL 4.1971 mL 8.3942 mL 20.9855 mL
10 mM 0.4197 mL 2.0985 mL 4.1971 mL 10.4927 mL
15 mM 0.2798 mL 1.3990 mL 2.7981 mL 6.9952 mL
20 mM 0.2099 mL 1.0493 mL 2.0985 mL 5.2464 mL
25 mM 0.1679 mL 0.8394 mL 1.6788 mL 4.1971 mL
30 mM 0.1399 mL 0.6995 mL 1.3990 mL 3.4976 mL
40 mM 0.1049 mL 0.5246 mL 1.0493 mL 2.6232 mL
50 mM 0.0839 mL 0.4197 mL 0.8394 mL 2.0985 mL
60 mM 0.0700 mL 0.3498 mL 0.6995 mL 1.7488 mL
80 mM 0.0525 mL 0.2623 mL 0.5246 mL 1.3116 mL
100 mM 0.0420 mL 0.2099 mL 0.4197 mL 1.0493 mL
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680C91 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:

680C91163239-22-3Otherstryptophan 2,3-dioxygenasetryptophan catabolismAlzheimer’s DiseaseInhibitorinhibitorinhibit

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