DB1976 dihydrochloride

Name: DB1976 dihydrochloride
Brand: MedChemExpress
SKU: HY-135797A
Rating: 5.0 (8 reviews)

製品番号: HY-135797A 純度: 98.0%: Data Sheet COA 取扱説明書
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Technical Support

DB1976 dihydrochloride is a selenophene analog of DB270 and a potent and cell-permeable fully efficacious transcription factor PU.1 inhibitor. DB1976 dihydrochloride potently inhibits PU.1 binding (IC₅₀ of 10 nM) and strongly inhibits the PU.1/DNA complex (with high DB1976-λB affinity, K_D of 12 nM) in vitro. DB1976 dihydrochloride has apoptosis-inducing effect.

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DB1976 dihydrochloride 構造式

CAS 番号 : 2369663-93-2

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 435	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 435	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$380	在庫あり	Estimated Time of Arrival: December 31
10 mg	$600	在庫あり	Estimated Time of Arrival: December 31
50 mg	$1700	在庫あり	Estimated Time of Arrival: December 31
100 mg	$2400	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 8 publication(s) in Google Scholar

Other Forms of DB1976 dihydrochloride:

DB1976 お問い合わせ

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参考文献
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製品説明

IC₅₀ & Target

IC50: 10 nM (Transcription factor PU.1)^[1]

体外実験

DB1976 is a classic heterocyclic dication (a single heteroatom) with strong affinity and selectivity for AT-rich sequences commonly found in cognate DNA binding sites for PU.1^[2].
DB1976 inhibits PU.1-dependent transactivation of the reporter in a dose-dependent manner with an IC₅₀ value of 2.4 μM in PU.1-negative HEK293 cells^[3].
DB1976 treatment leads to a profound decrease in the growth of PU.1 URE^–/– AML cells (IC₅₀ of 105 μM), while showing little effect on normal hematopoietic cells at similar concentrations (IC₅₀ of 334 μM)^[3].
DB1976 treatment leads to a 1.6-fold increase in apoptotic cells in murine PU.1 URE^–/– AML cells, and observed similar effects in human MOLM13 cells^[3].
DB1976 treatment leads to a significant decrease in the number of viable cells (primary human AML cells) (mean decrease of 81%) and clonogenic capacity (mean decrease of 36%) compared with vehicle-treated cells. The apoptotic cell fraction increased on average by 1.5-fold with DB1976^[3].

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

分子量

520.28

分子式

C₂₀H₁₈Cl₂N₈Se

CAS 番号

2369663-93-2

Appearance

Solid

Color

Brown to black

SMILES

N=C(C1=CC=C2N=C(C3=CC=C(C4=NC5=CC=C(C(N)=N)C=C5N4)[Se]3)NC2=C1)N.[H]Cl.[H]Cl

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶剤 & 溶解度

体外:

DMSO : 50 mg/mL (96.10 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 18.33 mg/mL (35.23 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9220 mL	9.6102 mL	19.2204 mL
5 mM	0.3844 mL	1.9220 mL	3.8441 mL
10 mM	0.1922 mL	0.9610 mL	1.9220 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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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 (4.81 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.
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.

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.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

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).

純度とドキュメンテーション

純度: 98.0%

Select Batch:

COA (248 KB) HNMR (176 KB) MS (72 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Munde M, et al. Structure-dependent inhibition of the ETS-family transcription factor PU.1 by novel heterocyclic diamidines. Nucleic Acids Res. 2014 Jan;42(2):1379-90. [Content Brief]

[2]. Stephens DC, et al. Pharmacologic efficacy of PU.1 inhibition by heterocyclic dications: a mechanistic analysis. Nucleic Acids Res. 2016 May 19;44(9):4005-13. [Content Brief]

[3]. Antony-Debré I, et al. Pharmacological inhibition of the transcription factor PU.1 in leukemia. J Clin Invest. 2017 Dec 1;127(12):4297-4313. [Content Brief]

Complete Stock Solution Preparation Table

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

H₂O / DMSO	1 mM	1.9220 mL	9.6102 mL	19.2204 mL	48.0510 mL
	5 mM	0.3844 mL	1.9220 mL	3.8441 mL	9.6102 mL
	10 mM	0.1922 mL	0.9610 mL	1.9220 mL	4.8051 mL
	15 mM	0.1281 mL	0.6407 mL	1.2814 mL	3.2034 mL
	20 mM	0.0961 mL	0.4805 mL	0.9610 mL	2.4026 mL
	25 mM	0.0769 mL	0.3844 mL	0.7688 mL	1.9220 mL
	30 mM	0.0641 mL	0.3203 mL	0.6407 mL	1.6017 mL
DMSO	40 mM	0.0481 mL	0.2403 mL	0.4805 mL	1.2013 mL
	50 mM	0.0384 mL	0.1922 mL	0.3844 mL	0.9610 mL
	60 mM	0.0320 mL	0.1602 mL	0.3203 mL	0.8009 mL
	80 mM	0.0240 mL	0.1201 mL	0.2403 mL	0.6006 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.