Size | Price | Stock | Qty |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
GNE-781 (GNE781) is a novel, highly potent and selective inhibitor of CBP (Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein) with immunomodulatory and anticancer effects. It inhibits CBP with an IC50 of 0.94 nM in TR-FRET assay. GNE-781 also inhibits BRET and BRD4(1) with IC50s of 6.2 nM and 5100 nM, respectively. GNE-781 showed TR-FRET IC50 = 0.94 nM, BRET IC50 = 6.2 nM, BRD4(1) IC50 = 5,100 nΜ) that maintained good in vivo PK properties in multiple species. GNE-781 displays anti-tumor activity in an AML tumor model and was also shown to decrease Foxp3 transcript levels in a dose dependent manner.
Targets |
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ln Vitro |
GNE-781 is a highly developed, strong, and specific bromodomain inhibitor of the CBP (cyclic adenosine monophosphate response element-binding protein). The transcript levels of FOXP3 (forkhead box P3) are decreased by GNE-781. Analysis of a subset of bromodomains revealed that GNE-781 has significant selectivity for both CBP (5425-fold) and P300 (4250-fold), and is very selective for CBP/P300. GNE-781 exhibits cellular potency and selectivity in the ideal ratio—5425 times higher than BRD4 (1)—[1].
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ln Vivo |
In mice bearing MOLM-16 AML xenografts, GNE-781 (3-30 mg/kg; po; twice daily for 21 days) suppresses tumor growth inhibition (%TGI) at doses of 3, 10, and 30 mg/kg 73%, 71%, and 89%, respectively [1]. Foxp3 transcript levels are lowered in a dose-dependent manner by GNE-781. At doses as low as 3 mg/kg, GNE-781 (3-30 mg/kg) inhibits MYC at 2 and 8 hours; at 10 and 30 mg/kg, the greatest inhibition (87% and 88% inhibition) is reached at 2 hours [1].
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Animal Protocol |
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References |
[1]. Romero FA, et al. GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP). J Med Chem. 2017 Nov 22;60(22):9162-9183
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Molecular Formula |
C27H33F2N7O2
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Molecular Weight |
525.593432188034
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CAS # |
1936422-33-1
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SMILES |
O=C(N1CCC(N(C2CCOCC2)N=C3N4CCCC5=C4C=C(C(F)F)C(C6=CN(C)N=C6)=C5)=C3C1)NC
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InChi Key |
CQCWHSDMJBAGDC-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C27H33F2N7O2/c1-30-27(37)34-9-5-23-22(16-34)26(32-36(23)19-6-10-38-11-7-19)35-8-3-4-17-12-20(18-14-31-33(2)15-18)21(25(28)29)13-24(17)35/h12-15,19,25H,3-11,16H2,1-2H3,(H,30,37)
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Chemical Name |
3-[7-(difluoromethyl)-6-(1-methylpyrazol-4-yl)-3,4-dihydro-2H-quinolin-1-yl]-N-methyl-1-tetrahydropyran-4-yl-6,7-dihydro-4H-pyrazolo[4,3-c]pyridine-5-carboxamide
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Synonyms |
GNE781; GNE 781; GNE-781.
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~100 mg/mL (~190.26 mM)
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.9026 mL | 9.5131 mL | 19.0262 mL | |
5 mM | 0.3805 mL | 1.9026 mL | 3.8052 mL | |
10 mM | 0.1903 mL | 0.9513 mL | 1.9026 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.