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GNE-781

🥰Excellent
Catalog No. T15405Cas No. 1936422-33-1

GNE-781 is a highly potent and selective inhibitor of CBP (IC50: 0.94 nM in TR-FRET assay). GNE-781 also inhibits BRET and BRD4(1) (IC50s: 6.2 nM and 5100 nM, respectively).

GNE-781

GNE-781

🥰Excellent
Purity: 99.92%
Catalog No. T15405Cas No. 1936422-33-1
GNE-781 is a highly potent and selective inhibitor of CBP (IC50: 0.94 nM in TR-FRET assay). GNE-781 also inhibits BRET and BRD4(1) (IC50s: 6.2 nM and 5100 nM, respectively).
Pack SizePriceAvailabilityQuantity
1 mg$166In Stock
5 mg$372In Stock
10 mg$556In Stock
25 mg$896In Stock
50 mg$1,220In Stock
100 mg$1,650In Stock
1 mL x 10 mM (in DMSO)$412In Stock
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Purity:99.92%
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Product Introduction

Bioactivity
Description
GNE-781 is a highly potent and selective inhibitor of CBP (IC50: 0.94 nM in TR-FRET assay). GNE-781 also inhibits BRET and BRD4(1) (IC50s: 6.2 nM and 5100 nM, respectively).
Targets&IC50
BRET:6.2 nM, CBP:0.94 nM, BRD41:5100 nM
In vitro
GNE-781 decreases FOXP3 (forkhead box P3) transcript levels. GNE-781 is a highly advanced potent and selective bromodomain inhibitor of cyclic adenosine monophosphate response element-binding protein, binding protein. GNE-781 is exquisitely selective for CBP/P300 and is remarkably selective for CBP (5425-fold) and P300 (4250-fold), which is shown by an examination of a subset of bromodomains. GNE-781 displays an appropriate balance of cell potency, selectivity (5425-fold over BRD4(1)) [1].
In vivo
GNE-781 is a highly potent and selective inhibitor of CBP that is efficacious in a MOLM-16 AML xenograft model. GNE-781 shows antitumor activity in an AML tumor model and is also shown to reduce Foxp3 transcript levels in a dose-dependent manner and it also shows moderate to low clearance in vivo in all species evaluated, with acceptable oral bioavailability. The effect of GNE-781 is determined in an in vivo PK/PD experiment using a MOLM-16 (adult AML cell line) xenograft mouse model. GNE-781(3 and 30 mg/kg; Single doses) are given in MOLM-16 tumor-bearing animals, and samples are collected at time points covering 2-24 h. Upon tumor establishment, Administration with GNE-781(3-30 mg/kg; twice daily ). Single-agent efficacy is observed at all doses, as evidenced by inhibition of MOLM-16 tumor growth. Tumor growth inhibition (%TGI) is 73%, 71%, and 89% at 3, 10, and 30 mg/kg, respectively. All doses of GNE-781 are well tolerated over the 21-day dosing window, with a maximal body weight loss of 3.7%. Tumor RNA is generated and used to assess MYC transcript by quantitative RT-PCR relative to vehicle-treated animals. At doses as low as 3 mg/kg at 2 and 8 h, suppression of MYC is observed, with maximal suppression observed at 10 and 30 mg/kg at 2 h (87% and 88% inhibition, respectively). To evaluate the in vivo efficacy of GNE-781, MOLM-16 AML xenografts are established in SCID beige mice[1].
Chemical Properties
Molecular Weight525.59
FormulaC27H33F2N7O2
Cas No.1936422-33-1
SmilesCNC(=O)N1CCc2c(C1)c(nn2C1CCOCC1)N1CCCc2cc(-c3cnn(C)c3)c(cc12)C(F)F
Relative Density.1.45 g/cm3 (Predicted)
Storage & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 95 mg/mL (180.75 mM), Sonication is recommended.
Ethanol: 95 mg/mL (180.75 mM)
Solution Preparation Table
DMSO/Ethanol
1mg5mg10mg50mg
1 mM1.9026 mL9.5131 mL19.0262 mL95.1312 mL
5 mM0.3805 mL1.9026 mL3.8052 mL19.0262 mL
10 mM0.1903 mL0.9513 mL1.9026 mL9.5131 mL
20 mM0.0951 mL0.4757 mL0.9513 mL4.7566 mL
50 mM0.0381 mL0.1903 mL0.3805 mL1.9026 mL
100 mM0.0190 mL0.0951 mL0.1903 mL0.9513 mL

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