| Identification | Back Directory | [Name]
INDEX NAME NOT YET ASSIGNED | [CAS]
2474876-09-8 | [Synonyms]
GSK046 (iBET-BD2)
GSK046 (Synonyms: iBET-BD2)
Benzamide, 4-(acetylamino)-3-fluoro-N-(trans-4-hydroxycyclohexyl)-5-[(1S)-1-phenylethoxy]- | [Molecular Formula]
C23H27FN2O4 | [MOL File]
2474876-09-8.mol | [Molecular Weight]
414.47 |
| Chemical Properties | Back Directory | [Boiling point ]
562.6±50.0 °C(Predicted) | [density ]
1.26±0.1 g/cm3(Predicted) | [storage temp. ]
-20°C | [solubility ]
DMSO: soluble | [form ]
A crystalline solid | [pka]
12.90±0.70(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
GSK046 (iBET-BD2) is a potent, selective and orally active BD2 bromodomain inhibitor of the BET proteins, with IC50s of 264 nM (BRD2 BD2), 98 nM (BRD3 BD2), 49 nM (BRD4 BD2) and 214 nM (BRDT BD2), respectively. GSK046 has immunomodulatory activity[1]. | [in vivo]
GSK046 (40?mg/kg/QD; s.c. for 14 days) has immunomodulatory activity[1].
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GSK046 exhibits Cmax (C57BL6 1589, C57B16 2993 ng/mL) and terminal elimination half-lives (C57BL6 1.8, C57B16 1.9 h) following oral administration (C57BL6 10, C57B16 40 mg/kg)[1].
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GSK046 exhibits Cmax (mouse 1589, rat 202 ng/mL) and terminal elimination half-lives (mouse 1.8, rat 1.4 h) following oral administration (mouse 10, rat 10 mg/kg)[1]. | Animal Model: | Male C57BL/6 mice (8/10-weeks-old) are injected with keyhole limpet hemocyanin (KLH)[1] | | Dosage: | 40?mg/kg/QD | | Administration: | S.c. injections for 14 days | | Result: | Reduced the production of anti-keyhole limpet hemocyanin (KLH) IgM and was well tolerated. |
| Animal Model: | Female C57BL/6 mice[1] | | Dosage: | 10?mg/kg (Pharmacokinetic Analysis) | | Administration: | Oral administration | | Result: | Cmax (1859 ng/mL), T1/2 (1.8 h). |
| Animal Model: | Male C57BL/6 mice[1] | | Dosage: | 40?mg/kg (Pharmacokinetic Analysis) | | Administration: | Oral administration | | Result: | Cmax (2993 ng/mL), T1/2 (1.9 h). |
| Animal Model: | Female Lewis rat[1] | | Dosage: | 10?mg/kg (Pharmacokinetic Analysis) | | Administration: | Oral administration | | Result: | Cmax (202 ng/mL), T1/2 (1.4 h). |
| [IC 50]
BRD2 BD2: 264 nM (IC50); BRD3 BD2: 98 nM (IC50); BRD4 BD2: 49 nM (IC50); BRDT BD2: 214 nM (IC50) | [storage]
-20°C | [References]
[1] Omer G, et, al. Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation. Science. 2020 Apr 24; 368(6489): 387-394. DOI:10.1126/science.aaz8455 |
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| Company Name: |
cjbscvictory
|
| Tel: |
13348960310 13348960310 |
| Website: |
https://www.weikeqi-biotech.com/ |
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