[CAS NO. 1434048-34-6] Fenebrutinib

Name: Fenebrutinib
Brand: Arctom Scientific
SKU: HY-19834

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PRODUCTS SPECIFICATIONS [1434048-34-6]

Distributor

Catalog

HY-19834

Brand

MCE

CAS

1434048-34-6

DESCRIPTION [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

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

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

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.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 1 mg/mL (1.50 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 1 mg/mL (1.50 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 1 mg/mL (1.50 mM); Clear solution

* All of the co-solvents are available by MCE.