- Fenebrutinib
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- $36.00 / 1mg
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2025-11-10
- CAS:1434048-34-6
- Min. Order:
- Purity: 98.94%
- Supply Ability: 10g
- GDC-0853
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- $6.68 / 1KG
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2020-01-09
- CAS: 1434048-34-6
- Min. Order: 1KG
- Purity: 97%-99%
- Supply Ability: 1kg-1000kg
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| | GDC-0853 Basic information |
| Product Name: | GDC-0853 | | Synonyms: | (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;GDC0853;EOS-61209;GDC-0853 (RG7845);GDC-0853;GDC 0853;FENEBRUTINIB (GDC-0853);FENEBRUTINIB;CS-2241 | | CAS: | 1434048-34-6 | | MF: | C37H44N8O4 | | MW: | 664.8 | | EINECS: | | | Product Categories: | | | Mol File: | 1434048-34-6.mol |  |
| | GDC-0853 Chemical Properties |
| 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 | | InChIKey | WNEODWDFDXWOLU-QHCPKHFHSA-N | | SMILES | C12=CC3CC(C)(C)CC=3N1CCN(C1=NC=CC(C3C=C(NC4=NC=C(N5CCN(C6COC6)C[C@@H]5C)C=C4)C(=O)N(C)C=3)=C1CO)C2=O |
| | GDC-0853 Usage And Synthesis |
| 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. 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. 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. | | in vivo | Fenebrutinib (GDC-0853) dose-dependently reduces ankle thickness following once (0.06, 0.25, 1, 4, and 16 mg/kg QD; orally) or twice (0.125, 0.5, and 2 mg/kg BID; orally) daily in female Lewis rats with developing collagen-induced arthritis[2].
Fenebrutinib (0.2 mg/kg IV and 1.0 mg/kg PO; for rats) and (0.2 mg/kg IV and 0.5 mg/kg PO for dogs) demonstrates the half-lives (t1/2s) of 2.2 and 3.8 h In rats, and dogs, respectively[2]. | Animal Model: | Female Lewis rats with developing collagen-induced arthritis (CIA)[2] | | Dosage: | 0.06, 0.25, 1, 4, and 16 mg/kg once daily (QD); 0.125, 0.5, and 2 mg/kg twice daily (BID) | | Administration: | Dosed orally; for 16 days | | Result: | Dose-dependently reduced ankle thickness following QD and BID dosing regimens. |
| | References | [1] JAMES J. CRAWFORD*. Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton’s Tyrosine Kinase Inhibitor in Early Clinical Development[J]. Journal of Medicinal Chemistry, 2018, 61 6: 2227-2245. DOI: 10.1021/acs.jmedchem.7b01712 |
| | GDC-0853 Preparation Products And Raw materials |
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