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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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G646818-1mg | 1mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $550.90 | |
G646818-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $980.90 | |
G646818-10mg | 10mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $1,500.90 |
Specifications & Purity | ≥97% |
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Biochemical and Physiological Mechanisms | GNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP , with an IC 50 of 1 nM, exhibits a selectively index ofu202f>2500-fold against BRD4 (1). GNE-207 shows excellent CBP potency, with an EC 50 of 18 nM for MYC expres |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Product Description | GNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP , with an IC 50 of 1 nM, exhibits a selectively index of >2500-fold against BRD4 (1). GNE-207 shows excellent CBP potency, with an EC 50 of 18 nM for MYC expression in MV-4-11 cells In Vitro GNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP, with an IC 50 of 1 nM, a selectively index of >2500-fold against BRD4 (1) (IC 50 , 3.1 μM). GNE-207 shows excellent CBP potency, with an EC 50 of 18 nM for MYC expression in MV-4-11 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo GNE-207 (5 mg/kg) shows moderate clearance in PK, with acceptable oral bioavailability . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:BRD4(1) 3.1 μM (IC 50 ) CBP 1 nM (IC 50 ) |
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IUPAC Name | 5-[8-[5-acetyl-1-(oxan-4-yl)-6,7-dihydro-4H-pyrazolo[4,3-c]pyridin-3-yl]isoquinolin-3-yl]-N-methylpyridine-2-carboxamide |
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INCHI | InChI=1S/C29H30N6O3/c1-18(36)34-11-8-27-24(17-34)28(33-35(27)21-9-12-38-13-10-21)22-5-3-4-19-14-26(32-16-23(19)22)20-6-7-25(31-15-20)29(37)30-2/h3-7,14-16,21H,8-13,17H2,1-2H3,(H,30,37) |
InChi Key | MUJXZEDIWKGKQD-UHFFFAOYSA-N |
Canonical SMILES | CC(=O)N1CCC2=C(C1)C(=NN2C3CCOCC3)C4=CC=CC5=CC(=NC=C54)C6=CN=C(C=C6)C(=O)NC |
Isomeric SMILES | CC(=O)N1CCC2=C(C1)C(=NN2C3CCOCC3)C4=CC=CC5=CC(=NC=C54)C6=CN=C(C=C6)C(=O)NC |
PubChem CID | 132186469 |
Molecular Weight | 510.59 |
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Solubility | DMSO : 200 mg/mL (391.70 mM; Need ultrasonic) |
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