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GSK778

Name: GSK778
Brand: TargetMol
SKU: T9703
Price: 39 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T9703Cas No. 2451862-42-1

GSK778 is a potent and selective inhibitor of BD1 bromodomain such as BRD2 BD1 (IC50s = 75 nM), BRD3 BD1 (IC50s = 41 nM), BRD4 BD1 (IC50s = 41 nM), and BRDT BD1 (IC50s = 143 nM). GSK778 inhibits proliferation, induces a cell cycle arrest and apoptosis.

GSK778

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Purity: 98.42%

Catalog No. T9703Cas No. 2451862-42-1

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$163	-	In Stock
5 mg	$328	-	In Stock
10 mg	$529	-	In Stock
25 mg	$1,060	-	In Stock
50 mg	$1,680	-	In Stock
100 mg	$2,330	-	In Stock
1 mL x 10 mM (in DMSO)	$39	-	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:98.42%

Appearance:Solid

Color:White

Resource Download

COA HNMR HPLC

Product Introduction

Bioactivity

Description	GSK778 is a potent and selective inhibitor of BD1 bromodomain such as BRD2 BD1 (IC50s = 75 nM), BRD3 BD1 (IC50s = 41 nM), BRD4 BD1 (IC50s = 41 nM), and BRDT BD1 (IC50s = 143 nM). GSK778 inhibits proliferation, induces a cell cycle arrest and apoptosis.
Targets&IC50	BRD4 BD1:41 nM, BRDT BD1:143 nM, BRD2 BD1:75 nM, BRD3 BD1:41 nM
In vitro	GSK778 phenocopies the effects of pan-BET inhibitors in cancer models. GSK778 inhibits BRD BD2 receptors such as BRD2 BD2 (IC50 = 3950 nM), BRD3 BD2 (IC50 = 1210 nM ), BRD4 BD2 (IC50 = 5843 nM), and BRDT BD2 (IC50 = 17451 nM)[1]. GSK778 (0.001-10 μM; 5 days) has a more pronounced effect on the growth and viability of MDA-453, MOLM-13, K562, MV4-11, THP-1, and MDA-MB-231 cells. GSK778 (1000 nM; 12 days) reduces the clonogenic capacity of primary human AML cells. GSK778 (0.01-10 μM; 72 hours) inhibited the production of effector cytokines including IFNγ, IL-17A and IL-22 and the proliferative activity of human primary CD4+ T cells[1].
In vivo	GSK778 (15 mg/kg/BID; s.c. for 14 days) reduces the production of anti-keyhole limpet hemocyanin (KLH) IgM and is well tolerated. GSK778 (15 mg/kg/BID; i.p. for 30 days) offers a superior survival advantage to iBET-BD2 in the aggressive MLL-AF9 AML model. The Cmax, Tmax, and AUC∞ values are 85 ng/mL, 1.48 h, and 132 ng.h/mL, respectively[1].

Chemical Properties

Molecular Weight	511.61
Formula	C₃₀H₃₃N₅O₃
Cas No.	2451862-42-1
Smiles	COCc1nc2cnc3cc(-c4c(C)noc4C)c(OC[C@H]4CCNC4)cc3c2n1[C@H](C)c1ccccc1

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 41.67 mg/mL (81.45 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.91 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.9546 mL	9.7731 mL	19.5461 mL	97.7307 mL
5 mM	0.3909 mL	1.9546 mL	3.9092 mL	19.5461 mL
10 mM	0.1955 mL	0.9773 mL	1.9546 mL	9.7731 mL
20 mM	0.0977 mL	0.4887 mL	0.9773 mL	4.8865 mL
50 mM	0.0391 mL	0.1955 mL	0.3909 mL	1.9546 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc