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GSK778 hydrochloride

Name: GSK778 hydrochloride
Brand: TargetMol
SKU: T9703L
Price: 117 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T9703LCas No. 2863657-79-6

GSK778 hydrochloride hydrochloride is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 hydrochloride hydrochloride phenocopies the effects of pan-BET inhibitors in cancer models[1].

GSK778 hydrochloride

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Purity: 98.35%

Catalog No. T9703LCas No. 2863657-79-6

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$117	In Stock	In Stock
5 mg	$262	In Stock	In Stock
10 mg	$387	In Stock	In Stock
25 mg	$592	In Stock	In Stock
50 mg	$828	In Stock	In Stock
100 mg	$1,110	-	In Stock
1 mL x 10 mM (in DMSO)	$336	In Stock	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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Purity:98.35%

Color:White to Yellow

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Product Introduction

Bioactivity

Description	GSK778 hydrochloride hydrochloride is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 hydrochloride hydrochloride phenocopies the effects of pan-BET inhibitors in cancer models[1].
Targets&IC50	BRD3 BD1:41 nM, BRDT BD1:143 nM, BRD2 BD1:75 nM, BRD4 BD1:41 nM
In vitro	GSK778 hydrochloride inhibits BRD BD2 with the IC50s of 3950 nM (BRD2 BD2), 1210 nM (BRD3 BD2), 5843 nM (BRD4 BD2), and 17451 nM (BRDT BD2), respectively[1]. GSK778 hydrochloride (0.01-10 μM; 72 hours) inhibits the proliferative activity of human primary CD4+ T cells and the production of effector cytokines including IFNγ, IL-17A and IL-22[1]. GSK778 hydrochloride (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[1]. GSK778 hydrochloride (1000 nM; 72 hours) inhibits proliferation, induces a cell cycle arrest and apoptosis in MV4-11, MOLM13, MDA-MB-231 and MB453 cells[1]. GSK778 hydrochloride (1000 nM; 12 days) reduces the clonogenic capacity of primary human AML cells[1].
In vivo	GSK778 hydrochloride (15?mg/kg/BID; i.p. for 30 days) offers a superior survival advantage to iBET-BD2 in the aggressive MLL-AF9 AML model[1]. GSK778 hydrochloride (15?mg/kg/BID; s.c. for 14 days) reduces the production of anti-keyhole limpet hemocyanin (KLH) IgM and is well tolerated[1]. GSK778 hydrochloride exhibits Cmax (85 ng/mL), Tmax (1.48 h) and AUC∞ (132 ng.h/mL) following oral administration (10?mg/kg) in mice[1].

Chemical Properties

Molecular Weight	548.08
Formula	C₃₀H₃₄ClN₅O₃
Cas No.	2863657-79-6
Smiles	C[C@@H](N1C(COC)=NC2=C1C3=CC(OC[C@@H]4CNCC4)=C(C5=C(C)ON=C5C)C=C3N=C2)C6=CC=CC=C6.[H]Cl

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: 50 mg/mL (91.23 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.8246 mL	9.1228 mL	18.2455 mL	91.2276 mL
5 mM	0.3649 mL	1.8246 mL	3.6491 mL	18.2455 mL
10 mM	0.1825 mL	0.9123 mL	1.8246 mL	9.1228 mL
20 mM	0.0912 mL	0.4561 mL	0.9123 mL	4.5614 mL
50 mM	0.0365 mL	0.1825 mL	0.3649 mL	1.8246 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