BET bromodomain-IN-5

Name: BET bromodomain-IN-5
Brand: MedChemExpress
SKU: HY-103036
Rating: 4.5 (0 reviews)

製品番号: HY-103036 純度: 99.49%: Data Sheet SDS COA 取扱説明書
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BET bromodomain-IN-5 is an orally active BET inhibitor with an IC₅₀ of 14 nM against BRD4 (1). BET bromodomain-IN-5 can inhibit the proliferation of tumor cells and induce cell cycle arrest and apoptosis. BET bromodomain-IN-5 can be used in the research of tumors.

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。

BET bromodomain-IN-5 構造式

CAS 番号 : 1505453-59-7

容量	価格（税別）	在庫状況	数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 99	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 99	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$90	在庫あり	Estimated Time of Arrival: December 31
10 mg	$150	在庫あり	Estimated Time of Arrival: December 31
25 mg	$255	在庫あり	Estimated Time of Arrival: December 31
50 mg	$357	在庫あり	Estimated Time of Arrival: December 31
100 mg	$560	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.

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Based on 0 publication(s) in Google Scholar

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製品説明

IC₅₀ & Target

BET^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
MV4-11	GI₅₀	15 1 Compound: 44	Cytotoxicity against human MV4-11 cells assessed as growth inhibition after 72 hrs by resazurin-based assay Cytotoxicity against human MV4-11 cells assessed as growth inhibition after 72 hrs by resazurin-based assay	[PMID: 26572217]
MV4-11	GI₅₀	15 1 Compound: 44	Cytotoxicity against human MV4-11 cells assessed as growth inhibition after 72 hrs by resazurin-based assay Cytotoxicity against human MV4-11 cells assessed as growth inhibition after 72 hrs by resazurin-based assay	[PMID: 26572217]
MV4-11	GI₅₀	15 1 Compound: 44	Cytotoxicity against human MV4-11 cells assessed as growth inhibition after 72 hrs by resazurin-based assay Cytotoxicity against human MV4-11 cells assessed as growth inhibition after 72 hrs by resazurin-based assay	[PMID: 26572217]

体外実験

BET bromodomain inhibitor (Compound 11) (0.001-10 μM; 4 days) can inhibit the proliferation of KMS-28PE plasmacytoma cells and AMO-1 multiple myeloma cells, and induce cell cycle arrest and apoptosis^[1].
BET bromodomain inhibitor (Compound 44) has a GI₅₀ of 15 nM against MV4-11 cells^[2].

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

分子量

445.90

分子式

C₂₄H₂₀ClN₅O₂

CAS 番号

1505453-59-7

Appearance

Solid

Color

White to off-white

SMILES

O=C(N)C[C@@H]1N=C(C2=CC=C(Cl)C=C2)C3=CC(C4=CN(C)N=C4)=CC=C3C5=C1ON=C5C

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 : ≥ 100 mg/mL (224.27 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2427 mL	11.2133 mL	22.4266 mL
5 mM	0.4485 mL	2.2427 mL	4.4853 mL
10 mM	0.2243 mL	1.1213 mL	2.2427 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: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.61 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.61 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.61 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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: 99.49%

Select Batch:

データシート (277 KB) SDS (393 KB)

COA (255 KB) HNMR (154 KB) LCMS (99 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Andrew Ryan CONERY, et al. EXPRESSION LEVELS OF BCL-xL, BCL2, BCL-w, AND BAD AND CANCER THERAPIES. WO2015153871A2. 2015-10-08.

[2]. Romero FA, et al. Disrupting Acetyl-Lysine Recognition: Progress in the Development of Bromodomain Inhibitors. J Med Chem. 2016 Feb 25;59(4):1271-98. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.2427 mL	11.2133 mL	22.4266 mL	56.0664 mL
	5 mM	0.4485 mL	2.2427 mL	4.4853 mL	11.2133 mL
	10 mM	0.2243 mL	1.1213 mL	2.2427 mL	5.6066 mL
	15 mM	0.1495 mL	0.7476 mL	1.4951 mL	3.7378 mL
	20 mM	0.1121 mL	0.5607 mL	1.1213 mL	2.8033 mL
	25 mM	0.0897 mL	0.4485 mL	0.8971 mL	2.2427 mL
	30 mM	0.0748 mL	0.3738 mL	0.7476 mL	1.8689 mL
	40 mM	0.0561 mL	0.2803 mL	0.5607 mL	1.4017 mL
	50 mM	0.0449 mL	0.2243 mL	0.4485 mL	1.1213 mL
	60 mM	0.0374 mL	0.1869 mL	0.3738 mL	0.9344 mL
	80 mM	0.0280 mL	0.1402 mL	0.2803 mL	0.7008 mL
	100 mM	0.0224 mL	0.1121 mL	0.2243 mL	0.5607 mL