1. Metabolic Enzyme/Protease
  2. Indoleamine 2,3-Dioxygenase (IDO)
  3. Linrodostat

Linrodostat  (Synonyms: BMS-986205; ONO-7701)

Cat. No.: HY-101560 Purity: 99.81%
SDS COA Handling Instructions

Linrodostat (BMS-986205) is a selective and irreversible indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor with an IC50 value of 1.1 nM in IDO1-HEK293 cells. Linrodostat is well tolerated with potent pharmacodynamic activity in advanced cancers.

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

Linrodostat Chemical Structure

Linrodostat Chemical Structure

CAS No. : 1923833-60-6

Size Price Stock Quantity
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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 73 In-stock
Solution
10 mM * 1 mL in DMSO USD 73 In-stock
Solid
5 mg USD 66 In-stock
10 mg USD 99 In-stock
25 mg USD 198 In-stock
50 mg USD 330 In-stock
100 mg USD 528 In-stock
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Customer Review

Based on 4 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

Linrodostat (BMS-986205) is a selective and irreversible indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor with an IC50 value of 1.1 nM in IDO1-HEK293 cells. Linrodostat is well tolerated with potent pharmacodynamic activity in advanced cancers[1][2].

IC50 & Target[1]

IDO1

1.1 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
HeLa IC50
2.8 nM
Compound: BMS-986205
Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells using L-tryptophan as substrate incubated for 48 hrs by fluorescence assay
Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells using L-tryptophan as substrate incubated for 48 hrs by fluorescence assay
[PMID: 32832022]
In Vitro

Linrodostat (0.01-100 μM; 72 hours; SKOV-3 and Jurkat clone E6-1 cells) treatment reduces the number of viable cells compared with the non-treated control. Linrodostat also induces cell death at much lower concentrations and its IC50 is 6.3 μM[1].

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

Cell Viability Assay[1]

Cell Line: SKOV-3 and Jurkat clone E6-1 cells
Concentration: 0.01-100 μM
Incubation Time: 72 hours
Result: Reduced the number of viable cells compared with the non-treated control and induced cell death at much lower concentrations.
Clinical Trial
Molecular Weight

410.91

Formula

C24H24ClFN2O

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=CC=C(Cl)C=C1)[C@H](C)[C@@](CC2)([H])CC[C@H]2C3=CC=NC4=C3C=C(F)C=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (121.68 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 2.4336 mL 12.1681 mL 24.3362 mL
5 mM 0.4867 mL 2.4336 mL 4.8672 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
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:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

    Solubility: 2.5 mg/mL (6.08 mM); Suspended solution; Need ultrasonic

  • Protocol 2

    Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (6.08 mM); Suspended solution; Need ultrasonic

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: 99.81%

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4336 mL 12.1681 mL 24.3362 mL 60.8406 mL
5 mM 0.4867 mL 2.4336 mL 4.8672 mL 12.1681 mL
10 mM 0.2434 mL 1.2168 mL 2.4336 mL 6.0841 mL
15 mM 0.1622 mL 0.8112 mL 1.6224 mL 4.0560 mL
20 mM 0.1217 mL 0.6084 mL 1.2168 mL 3.0420 mL
25 mM 0.0973 mL 0.4867 mL 0.9734 mL 2.4336 mL
30 mM 0.0811 mL 0.4056 mL 0.8112 mL 2.0280 mL
40 mM 0.0608 mL 0.3042 mL 0.6084 mL 1.5210 mL
50 mM 0.0487 mL 0.2434 mL 0.4867 mL 1.2168 mL
60 mM 0.0406 mL 0.2028 mL 0.4056 mL 1.0140 mL
80 mM 0.0304 mL 0.1521 mL 0.3042 mL 0.7605 mL
100 mM 0.0243 mL 0.1217 mL 0.2434 mL 0.6084 mL
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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.

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Linrodostat
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