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[CAS NO. 1434048-34-6] Fenebrutinib
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-19834 |
| Brand: | MCE |
| CAS: | 1434048-34-6 |
Overview
| MDL | - |
|---|---|
| Molecular Weight | 664.80 |
| Molecular Formula | C37H44N8O4 |
| SMILES | O=C1C(NC(C=C2)=NC=C2N3CCN(C4COC4)C[C@@H]3C)=CC(C5=CC=NC(N6C(C7=CC(CC(C)(C)C8)=C8N7CC6)=O)=C5CO)=CN1C |
3 Publications Citing Use of MCE
Summary
Fenebrutinib (GDC-0853) is a potent, selective, orally available, and noncovalent bruton's tyrosine kinase ( Btk ) inhibitor with K i s 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 IC
50
of 8.4±5.6 nM. Fenebrutinib inhibits CD63 expression on basophils with an IC
50
of 30.7±4.1 nM
[2]
.
Fenebrutinib suppresses anti-IgM induced Btk Y223 autophosphorylation in human whole blood (IC
50
=11 nM)
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 (t
1/2
s) of 2.2 and 3.8 h In rats, and dogs, respectively
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| 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
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT03188783 | Hoffmann-La Roche |
Healthy Volunteer
|
January 24, 2017 | Phase 1 |
| NCT03290703 | Genentech, Inc. |
Healthy Volunteers
|
April 18, 2017 | Phase 1 |
| NCT02908100 | Genentech, Inc. |
Systemic Lupus Erythematosus
|
January 19, 2017 | Phase 2 |
| NCT04544449 | Hoffmann-La Roche |
Multiple Sclerosis, Primary Progressive
|
October 26, 2020 | Phase 3 |
| NCT05119569 | Hoffmann-La Roche |
Relapsing Multiple Sclerosis
|
March 1, 2022 | Phase 2 |
| NCT03137069 | Genentech, Inc. |
Urticaria
|
May 26, 2017 | Phase 2 |
| NCT03174041 | Genentech, Inc. |
Healthy Participants
|
April 18, 2017 | Phase 1 |
| NCT01991184 | Genentech, Inc. |
Lymphocytic Leukemia, Chronic, Diffuse Large B-Cell Lymphoma
|
December 16, 2013 | Phase 1 |
| NCT04586010 | Hoffmann-La Roche |
Relapsing Multiple Sclerosis
|
March 17, 2021 | Phase 3 |
| NCT03596632 | Hoffmann-La Roche |
Healthy Participants
|
July 27, 2018 | Phase 1 |
| NCT02833350 | Genentech, Inc. |
Rheumatoid Arthritis
|
September 9, 2016 | Phase 2 |
| NCT03693625 | Genentech, Inc. |
Urticaria
|
September 27, 2018 | Phase 2 |
| NCT04586023 | Hoffmann-La Roche |
Relapsing Multiple Sclerosis
|
March 24, 2021 | Phase 3 |
| NCT03407482 | Genentech, Inc. |
Lupus Erythematosus, Systemic
|
January 9, 2018 | Phase 2 |
| NCT02983227 | Genentech, Inc. |
Rheumatoid Arthritis
|
November 30, 2016 | Phase 2 |
| NCT02699710 | Genentech, Inc. |
Healthy Volunteer
|
September 3, 2015 | Phase 1 |
Appearance
Solid
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
DMSO : ≥ 23 mg/mL ( 34.60 mM )
* "≥" means soluble, but saturation unknown.
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 |
References
- [1] Erickson RI , et al. Bruton's Tyrosine Kinase Small Molecule Inhibitors Induce a Distinct Pancreatic Toxicity in Rats. J Pharmacol Exp Ther. 2017 Jan;360(1):226-238.
- [2] Crawford JJ, et al. Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development. J Med Chem. 2018 Mar 22;61(6):2227-2245.
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