Description
GNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP, with an IC50 of 1 nM, exhibits a selectively index of >2500-fold against BRD4 (1). GNE-207 shows excellent CBP potency, with an EC50 of 18 nM for MYC expression in MV-4-11 cells.
Product information
CAS Number: 2158266-58-9
Molecular Weight: 510.59
Formula: C29H30N6O3
Chemical Name: 5-{8-[5-acetyl-1-(oxan-4-yl)-1H,4H,5H,6H,7H-pyrazolo[4,3-c]pyridin-3-yl]isoquinolin-3-yl}-N-methylpyridine-2-carboxamide
Smiles: CC(=O)N1CC2=C(CC1)N(N=C2C1=CC=CC2C=C(N=CC=21)C1=CN=C(C=C1)C(=O)NC)C1CCOCC1
InChiKey: MUJXZEDIWKGKQD-UHFFFAOYSA-N
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)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 200 mg/mL (391.70 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
GNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP, with an IC50 of 1 nM, a selectively index of >2500-fold against BRD4 (1) (IC50, 3.1 μM). GNE-207 shows excellent CBP potency, with an EC50 of 18 nM for MYC expression in MV-4-11 cells.
In Vivo:
GNE-207 (5 mg/kg) shows moderate clearance in PK, with acceptable oral bioavailability.
Products are for research use only. Not for human use.
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