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GNE-272

Name: GNE-272
Brand: TargetMol
SKU: T15400
Rating: 4.5 (1 reviews)

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Catalog No. T15400Cas No. 1936428-93-1

GNE-272 is a selective inhibitor of CBP/EP300 (IC50: 0.02, 0.03, and 13 μM for CBP, EP300, and BRD4, respectively) and a selective in vivo probe for CBP/EP300.

GNE-272

😃Good

Catalog No. T15400Cas No. 1936428-93-1

GNE-272 is a selective inhibitor of CBP/EP300 (IC50: 0.02, 0.03, and 13 μM for CBP, EP300, and BRD4, respectively) and a selective in vivo probe for CBP/EP300.

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$107	6-8 weeks	6-8 weeks
25 mg	$728	6-8 weeks	6-8 weeks
50 mg	$946	6-8 weeks	6-8 weeks
100 mg	$1,490	6-8 weeks	6-8 weeks

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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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Product Introduction

Bioactivity

Description	GNE-272 is a selective inhibitor of CBP/EP300 (IC50: 0.02, 0.03, and 13 μM for CBP, EP300, and BRD4, respectively) and a selective in vivo probe for CBP/EP300.
Targets&IC50	EP300:0.03 μM, CBP:0.02 μM, BRD4:13 μM
In vitro	GNE-272 does not inhibit any target at >30% when tested at 10 μM in 35 kinase panel and 42 receptors off-target screening panel. GNE-272 does not inhibit (>10 μM, top concentration) several cytochrome P450s (3A4, 1A2, 2C9, 2C19, 2D6). GNE-272 is exquisitely selective for CBP/ EP300 and remarkably selective (650-fold) over BRD4. The compound has good potency in the BRET cellular assay. GNE-272 is shown to inhibit the expression of MYC10 (MV4?11 cell line) (EC50: 0.91 μM) and a good correlation between the BRET and MYC cellular assays is observed.
In vivo	GNE-272 displays a marked antiproliferative effect in hematologic cancer cell lines. Which modulates MYC expression in vivo that corresponds with antitumor activity in an AML tumor model. GNE-272 shows low clearance following a 1 mg/ kg intravenous dose in a mouse PK experiment and good oral bioavailability when dosed at 100 mg/kg, reaching an unbound Cmax of 26 μM.

Chemical Properties

Molecular Weight	424.47
Formula	C₂₂H₂₅FN₆O₂
Cas No.	1936428-93-1
Relative Density.	1.43 g/cm3 (Predicted)

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: 100 mg/mL (235.59 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (7.77 mM), Sonication is recommeded.

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	2.3559 mL	11.7794 mL	23.5588 mL	117.7940 mL
5 mM	0.4712 mL	2.3559 mL	4.7118 mL	23.5588 mL
10 mM	0.2356 mL	1.1779 mL	2.3559 mL	11.7794 mL
20 mM	0.1178 mL	0.5890 mL	1.1779 mL	5.8897 mL
50 mM	0.0471 mL	0.2356 mL	0.4712 mL	2.3559 mL
100 mM	0.0236 mL	0.1178 mL	0.2356 mL	1.1779 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 mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

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