| Identification | Back Directory | [Name]
GDC-0853 | [CAS]
1434048-34-6 | [Synonyms]
GDC0853
CS-2241
EOS-61209
FENEBRUTINIB
GDC-0853 (RG7845)
GDC-0853;GDC 0853
GDC-0853/Fenebrutinib
FENEBRUTINIB (GDC-0853)
(S)-2-(3'-(hydroxymethyl)-1-methyl-5-((5-(2-methyl-4-(oxetan-3-yl)piperazin-1-yl)pyridin-2-yl)amino)-6-oxo-1,6-dihydro-[3,4'-bipyridin]-2'-yl)-7,7-dimethyl-3,4,7,8-tetrahydro-2H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1(6H)-one
2H-Cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1(6H)-one, 2-[1,6-dihydro-3'-(hydroxymethyl)-1-methyl-5-[[5-[(2S)-2-methyl-4-(3-oxetanyl)-1-piperazinyl]-2-pyridinyl]amino]-6-oxo[3,4'-bipyridin]-2'-yl]-3,4,7,8-tetrahydro-7,7-dimethyl- | [Molecular Formula]
C37H44N8O4 | [MDL Number]
MFCD30489729 | [MOL File]
1434048-34-6.mol | [Molecular Weight]
664.8 |
| Chemical Properties | Back Directory | [Boiling point ]
936.3±65.0 °C(Predicted) | [density ]
1.42±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMF:20.0(Max Conc. mg/mL);30.08(Max Conc. mM)
DMSO:17.0(Max Conc. mg/mL);25.57(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:2):0.33(Max Conc. mg/mL);0.5(Max Conc. mM)
Ethanol:5.0(Max Conc. mg/mL);7.52(Max Conc. mM) | [form ]
A crystalline solid | [pka]
13.15±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
GDC-0853 is an orally bioavailable, selective, and reversible Bruton’s tyrosine kinase (BTK) inhibitor with IC50s ranging from 2-9 nM for basophil activation, B cell receptor activation, and constitutive p-BTK activity in whole blood lysates.1,2 In rats, treatment for longer than 7 days leads to pancreatic toxicity but it does not occur in mice or dogs, even at higher doses.3 Formulations containing GDC-0853 were well-tolerated in Phase I clinical trials and are in additional clinical trials for rheumatoid arthritis, lupus erythematosus, lymphoma, and leukemia. | [Uses]
Fenebrutinib is a selective and reversible oral small-molecular BTK inhibitor for the treatment of rheumatoid arthritis and systemic lupus erythematosus. | [storage]
Store at -20°C |
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