1. Protein Tyrosine Kinase/RTK
  2. Btk
  3. Fenebrutinib

Fenebrutinib (Synonyms: GDC-0853)

Cat. No.: HY-19834 Purity: 99.83%
Handling Instructions

Fenebrutinib (GDC-0853) is a potent, selective, orally available, and noncovalent bruton's tyrosine kinase (Btk) inhibitor with Kis of 0.91 nM, 1.6, 1.3, 12.6, and 3.4 nM for WT Btk, and the C481S, C481R, T474I, T474M mutants. Fenebrutinib has the potential for rheumatoid arthritis and systemic lupus erythematosus research.

For research use only. We do not sell to patients.

Fenebrutinib Chemical Structure

Fenebrutinib Chemical Structure

CAS No. : 1434048-34-6

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Description

Fenebrutinib (GDC-0853) is a potent, selective, orally available, and noncovalent bruton's tyrosine kinase (Btk) inhibitor with Kis of 0.91 nM, 1.6, 1.3, 12.6, and 3.4 nM for WT Btk, and the C481S, C481R, T474I, T474M mutants. Fenebrutinib has the potential for rheumatoid arthritis and systemic lupus erythematosus research[1].

IC50 & Target

Ki: 0.91 nM (Btk WT), 1.6 nM (Btk C481S), 1.3 nM (Btk C481R), 12.6 nM (Btk T474I), and 3.4 nM (Btk T474M)[1]

In Vitro

Fenebrutinib (GDC-0853) inhibits CD69 expression on CD19+ B cells in human whole blood with an IC50 of 8.4±5.6 nM. Fenebrutinib inhibits CD63 expression on basophils with an IC50 of 30.7±4.1 nM[2].
Fenebrutinib suppresses anti-IgM induced Btk Y223 autophosphorylation in human whole blood (IC50=11 nM)[2].

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.
Clinical Trial
Molecular Weight

664.80

Formula

C₃₇H₄₄N₈O₄

CAS No.

1434048-34-6

SMILES

O=C1C(NC(C=C2)=NC=C2N3CCN(C4COC4)C[[email protected]@H]3C)=CC(C5=CC=NC(N6C(C7=CC(CC(C)(C)C8)=C8N7CC6)=O)=C5CO)=CN1C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 23 mg/mL (34.60 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5042 mL 7.5211 mL 15.0421 mL
5 mM 0.3008 mL 1.5042 mL 3.0084 mL
10 mM 0.1504 mL 0.7521 mL 1.5042 mL
*Please refer to the solubility information to select the appropriate solvent.
References

Purity: 99.83%

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Keywords:

FenebrutinibGDC-0853GDC0853GDC 0853BtkBruton tyrosine kinaseInhibitorinhibitorinhibit

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