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GNE-207

Catalog No. T15399Cas No. 2158266-58-9

GNE-207 is a selective and orally bioavailable inhibitor of the bromodomain of CBP (IC50: 1 nM). It has a selective index of >2500-fold against BRD4 (1). GNE-207 displays excellent CBP potency (EC50: 18 nM for MYC expression in MV-4-11 cells).

GNE-207

GNE-207

Catalog No. T15399Cas No. 2158266-58-9
GNE-207 is a selective and orally bioavailable inhibitor of the bromodomain of CBP (IC50: 1 nM). It has a selective index of >2500-fold against BRD4 (1). GNE-207 displays excellent CBP potency (EC50: 18 nM for MYC expression in MV-4-11 cells).
Pack SizePriceAvailabilityQuantity
25 mg$2,1208-10 weeks
50 mg$2,7808-10 weeks
100 mg$3,7008-10 weeks
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Product Introduction

Bioactivity
Description
GNE-207 is a selective and orally bioavailable inhibitor of the bromodomain of CBP (IC50: 1 nM). It has a selective index of >2500-fold against BRD4 (1). GNE-207 displays excellent CBP potency (EC50: 18 nM for MYC expression in MV-4-11 cells).
Targets&IC50
CBP:1 nM, BRD41:3.1 μM
In vivo
GNE-207 (5?mg/kg) displays moderate clearance in PK. It has an acceptable oral bioavailability.
Chemical Properties
Molecular Weight510.59
FormulaC29H30N6O3
Cas No.2158266-58-9
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 200 mg/mL (391.70 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.9585 mL9.7926 mL19.5852 mL97.9259 mL
5 mM0.3917 mL1.9585 mL3.9170 mL19.5852 mL
10 mM0.1959 mL0.9793 mL1.9585 mL9.7926 mL
20 mM0.0979 mL0.4896 mL0.9793 mL4.8963 mL
50 mM0.0392 mL0.1959 mL0.3917 mL1.9585 mL
100 mM0.0196 mL0.0979 mL0.1959 mL0.9793 mL

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TargetMol | Animal experimentsFor 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% ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | 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 DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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