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

Name: Linrodostat
Brand: MedChemExpress
SKU: HY-101560
Rating: 5.0 (6 reviews)

製品番号: HY-101560 純度: 99.81%: Data Sheet SDS COA 取扱説明書
FAQs
Technical Support

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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

Linrodostat 構造式

CAS 番号 : 1923833-60-6

容量	価格（税別）	在庫状況	数量

>無料サンプル (0.1 - 0.2 mg)		今すぐ申し込む
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 72	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 72	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$66	在庫あり	Estimated Time of Arrival: December 31
10 mg	$99	在庫あり	Estimated Time of Arrival: December 31
25 mg	$198	在庫あり	Estimated Time of Arrival: December 31
50 mg	$330	在庫あり	Estimated Time of Arrival: December 31
100 mg	$528	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

or バルクお問い合わせ

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 6 publication(s) in Google Scholar

Other Forms of Linrodostat:

Linrodostat mesylate お問い合わせ
Linrodostat (Standard) お問い合わせ

顧客検証

Indoleamine 2,3-Dioxygenase (IDO) アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

IDO1 IDO2 IDO

生物活性
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

IC₅₀ & Target^[1]

IDO1

1.1 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	IC₅₀	2.8 1 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]
HeLa	IC₅₀	2.8 1 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]
HEK293	IC₅₀	1.1 3 Compound: 63; BMS-986205	Inhibition of IDO1 in HEK293 cells Inhibition of IDO1 in HEK293 cells	[PMID: 32055299]
HEK293	IC₅₀	1.1 3 Compound: 63; BMS-986205	Inhibition of IDO1 in HEK293 cells Inhibition of IDO1 in HEK293 cells	[PMID: 32055299]
HeLa	IC₅₀	2.8 1 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]

体外実験

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.

臨床実験

分子量

410.91

分子式

C₂₄H₂₄ClFN₂O

CAS 番号

1923833-60-6

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

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
10 mM	0.2434 mL	1.2168 mL	2.4336 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)

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

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
Protocol 3

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.06 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
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 4

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (5.06 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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.
Protocol 5

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (5.06 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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.

純度とドキュメンテーション

純度: 99.81%

Select Batch:

データシート (276 KB) SDS (396 KB)

COA (251 KB) HNMR (280 KB) LCMS (94 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Richards T, et al. Cell based functional assays for IDO1 inhibitor screening and characterization. Oncotarget. 2018 Jul 20;9(56):30814-30820. [Content Brief]

[2]. Lillian L. Siu, et al. Abstract CT116: BMS-986205, an optimized indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor, is well tolerated with potent pharmacodynamic (PD) activity, alone and in combination with nivolumab (nivo) in advanced cancers in a phase 1/2a trial. AACR; Cancer Res. 2017; 77 (13 Suppl): Abstract nr CT116.

Complete Stock Solution Preparation Table

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

Linrodostat Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

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:

Linrodostat1923833-60-6BMS-986205 ONO-7701BMS986205BMS 986205ONO7701ONO 7701ONO-7701Indoleamine 2,3-Dioxygenase (IDO)Inhibitorinhibitorinhibit

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

カスタマーレビュー

Other Forms of Linrodostat:

顧客検証

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Indoleamine 2,3-Dioxygenase (IDO) アイソフォーム固有の製品をすべて表示:

生物活性

純度とドキュメンテーション

参考文献

カスタマーレビュー

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Linrodostat Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

最近チェックした製品:

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

カスタマーレビュー

Other Forms of Linrodostat:

Linrodostat 関連抗体

顧客検証

おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

Indoleamine 2,3-Dioxygenase (IDO) アイソフォーム固有の製品をすべて表示:

生物活性

純度とドキュメンテーション

参考文献

カスタマーレビュー

Linrodostat 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Linrodostat Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

最近チェックした製品:

カスタマーレビュー

Request for HNMR Report

Request for HNMR Report