| Identification | Back Directory | [Name]
GNE-207 | [CAS]
2158266-58-9 | [Synonyms]
GNE-207
2-Pyridinecarboxamide, 5-[8-[5-acetyl-4,5,6,7-tetrahydro-1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazolo[4,3-c]pyridin-3-yl]-3-isoquinolinyl]-N-methyl- | [Molecular Formula]
C29H30N6O3 | [MDL Number]
MFCD31807616 | [MOL File]
2158266-58-9.mol | [Molecular Weight]
510.59 |
| Chemical Properties | Back Directory | [Boiling point ]
812.8±65.0 °C(Predicted) | [density ]
1.38±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 200 mg/mL (391.70 mM) | [form ]
Solid | [pka]
13.75±0.46(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
GNE-207 is a novel, potent, and orally bioavailable inhibitor of the bromodomain of CBP. GNE-207 has excellent CBP potency (CBP IC50?=?1?nM, MYC EC50?=?18?nM), and it exhibits a good pharmacokinetic profile. | [Uses]
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[1]. | [in vivo]
GNE-207 (5 mg/kg) shows moderate clearance in PK, with acceptable oral bioavailability[1]. | [IC 50]
BRD4(1): 3.1 μM (IC50); CBP: 1 nM (IC50) | [References]
[1] Lai KW, et al. Design and synthesis of a biaryl series as inhibitors for the bromodomains of CBP/P300. ioorg Med Chem Lett. 2018 Jan 1;28(1):15-23. DOI:10.1016/j.bmcl.2017.11.025 |
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| Company Name: |
cjbscvictory
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| Tel: |
13348960310 |
| Website: |
https://www.weikeqi-biotech.com/ |
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