Benzamide, 4-?(acetylamino)?-?3-?fluoro-?N-?(trans-?4-?hydroxycyclohexyl)?-?5-?[(1S)?-?1-?phenylethoxy]?-

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Benzamide, 4-?(acetylamino)?-?3-?fluoro-?N-?(trans-?4-?hydroxycyclohexyl)?-?5-?[(1S)?-?1-?phenylethoxy]?- manufacturers

  • GSK046
  • GSK046 pictures
  • $55.00
  • 2026-08-30
  • CAS:2474876-09-8
  • Purity: 99.97%
  • Supply Ability: 10g
Benzamide, 4-?(acetylamino)?-?3-?fluoro-?N-?(trans-?4-?hydroxycyclohexyl)?-?5-?[(1S)?-?1-?phenylethoxy]?- Basic information
Product Name:Benzamide, 4-?(acetylamino)?-?3-?fluoro-?N-?(trans-?4-?hydroxycyclohexyl)?-?5-?[(1S)?-?1-?phenylethoxy]?-
Synonyms:GSK046 (Synonyms: iBET-BD2);Benzamide, 4-(acetylamino)-3-fluoro-N-(trans-4-hydroxycyclohexyl)-5-[(1S)-1-phenylethoxy]-;GSK046 (iBET-BD2);GSK046,Epigenetic Reader Domain,BRDT,BRD2,inhibit,immuno-inflammation,GSK 046,GSK-046,BRD4,Inhibitor,BD2,BRD3;GSK046 GSK-046;4-(acetylamino)-3-fluoro-N-(trans-4-hydroxycyclohexyl)-5-[(1S)-1-phenylethoxy]benzamide;4-Acetamido-3-fluoro-N-(trans-4-hydroxycyclohexyl)-5-((S)-1-phenylethoxy)benzamide;GSK046, 10 mM in DMSO
CAS:2474876-09-8
MF:C23H27FN2O4
MW:414.47
EINECS:
Product Categories:
Mol File:2474876-09-8.mol
Benzamide, 4-?(acetylamino)?-?3-?fluoro-?N-?(trans-?4-?hydroxycyclohexyl)?-?5-?[(1S)?-?1-?phenylethoxy]?- Structure
Benzamide, 4-?(acetylamino)?-?3-?fluoro-?N-?(trans-?4-?hydroxycyclohexyl)?-?5-?[(1S)?-?1-?phenylethoxy]?- Chemical Properties
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
pka12.90±0.70(Predicted)
color White to off-white
InChIKeyFRBRZGLUFOZRGD-JVPBZIDWSA-N
SMILESO=C(N[C@H]1CC[C@H](O)CC1)C2=CC(F)=C(NC(C)=O)C(O[C@H](C3=CC=CC=C3)C)=C2
Safety Information
WGK Germany WGK 3
Storage Class11 - Combustible Solids
MSDS Information
Benzamide, 4-?(acetylamino)?-?3-?fluoro-?N-?(trans-?4-?hydroxycyclohexyl)?-?5-?[(1S)?-?1-?phenylethoxy]?- Usage And Synthesis
UsesGSK046 (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 (40mg/kg/QD; s.c. for 14 days) has immunomodulatory activity[1].
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].
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:40mg/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:10mg/kg (Pharmacokinetic Analysis)
Administration:Oral administration
Result:Cmax (1859 ng/mL), T1/2 (1.8 h).
Animal Model:Male C57BL/6 mice[1]
Dosage:40mg/kg (Pharmacokinetic Analysis)
Administration:Oral administration
Result:Cmax (2993 ng/mL), T1/2 (1.9 h).
Animal Model:Female Lewis rat[1]
Dosage:10mg/kg (Pharmacokinetic Analysis)
Administration:Oral administration
Result:Cmax (202 ng/mL), T1/2 (1.4 h).
IC 50BRD2 BD2: 264 nM (IC50); BRD3 BD2: 98 nM (IC50); BRD4 BD2: 49 nM (IC50); BRDT BD2: 214 nM (IC50)
storageStore at -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
Benzamide, 4-?(acetylamino)?-?3-?fluoro-?N-?(trans-?4-?hydroxycyclohexyl)?-?5-?[(1S)?-?1-?phenylethoxy]?- Preparation Products And Raw materials
Tag:Benzamide, 4-?(acetylamino)?-?3-?fluoro-?N-?(trans-?4-?hydroxycyclohexyl)?-?5-?[(1S)?-?1-?phenylethoxy]?-(2474876-09-8) Related Product Information
Benzamide, 4-?(acetylamino)?-?3-?fluoro-?N-?(trans-?4-?hydroxycyclohexyl)?-?5-?[(1S)?-?1-?phenylethoxy]?- NA NA GNE-781 ZL0420 PF-CBP-1.HCl