Fenebrutinib (Synonyms: GDC-0853)

Name: Fenebrutinib
Brand: MedChemExpress
SKU: HY-19834
Rating: 5.0 (11 reviews)

Cat. No.: HY-19834 Purity: 99.89%: Data Sheet
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Fenebrutinib (GDC-0853) is a potent, selective, orally available, and noncovalent bruton's tyrosine kinase (Btk) inhibitor with K_is 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.

CAS No. : 1434048-34-6

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
2 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 11 publication(s) in Google Scholar

11 Publications Citing Use of MCE Fenebrutinib

Cell Proliferation/Viability Assay

Bio/Physico-chemical Assay

: Fenebrutinib purchased from MedChemExpress. Usage Cited in: ACS Pharmacol Transl Sci. 2025 Mar 12;8(4):917-931. [Abstract]; 11-point dose response curves (or lack thereof) for Fenebrutinib (GDC-0853) (0.0001-100 nM) to wild-type BTK and a BTK mutant (BTK C481S).

: Fenebrutinib purchased from MedChemExpress. Usage Cited in: Leukemia. 2021 May;35(5):1317-1329. [Abstract]; Fenebrutinib (1 μM) blocked phosphorylation of BTK (Y223 and Y551) in both C481S and C481T variants.

: Fenebrutinib purchased from MedChemExpress. Usage Cited in: Leukemia. 2021 May;35(5):1317-1329. [Abstract]; Fenebrutinib (1-3 μM) in COS-7 cells transfected with the resistant variants T474M/C481T, T474I/C481S, and T474M/C481S.

: Fenebrutinib purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2021 Dec 22;23(1):76.; Fenebrutinib (50 nM) significantly inhibited SPA in donors with normal and high SPA values (59-432 AU*min).

: Fenebrutinib purchased from MedChemExpress. Usage Cited in: JCI Insight. 2019 Jun 20;4(12). pii: 127566. [Abstract]; Cell proliferation assays of TMD8 lymphoma cells expressing the indicated BTK wild-type or mutant alleles were treated with Fenebrutinib (GDC-0853) (0.1-10,000 nM; 72 h).

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Description

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]

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	> 30 μM Compound: 29; GDC-0853	Inhibition of human ERG expressed in HEK293 cells incubated for 3 to 5 mins by automated parallel patch clamp assay Inhibition of human ERG expressed in HEK293 cells incubated for 3 to 5 mins by automated parallel patch clamp assay	[PMID: 29457982]
Hepatocyte	IC₅₀	> 300 μM Compound: 29; GDC-0853	Cytotoxicity against human primary hepatocytes assessed as reduction in cell viability Cytotoxicity against human primary hepatocytes assessed as reduction in cell viability	[PMID: 29457982]
TMD8	IC₅₀	12.6 nM Compound: GDC-0853	Cytotoxicity against human TMD8 cells incubated for 48 hrs by celltitre glo 2.0 assay Cytotoxicity against human TMD8 cells incubated for 48 hrs by celltitre glo 2.0 assay	[PMID: 37195170]

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].

MedChemExpress (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_1/2s) of 2.2 and 3.8 h In rats, and dogs, respectively^[2].

MedChemExpress (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

Molecular Weight

664.80

Formula

C₃₇H₄₄N₈O₄

CAS No.

1434048-34-6

Appearance

Solid

Color

White to off-white

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

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 : 20 mg/mL (30.08 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2 mg/mL (3.01 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2 mg/mL (3.01 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 1 mg/mL (1.50 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.89%

Select Batch:

Data Sheet (274 KB) SDS (581 KB)

COA (247 KB) HNMR (325 KB) RP-HPLC (252 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

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. [Content Brief]

[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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.5042 mL	7.5211 mL	15.0421 mL	37.6053 mL
	5 mM	0.3008 mL	1.5042 mL	3.0084 mL	7.5211 mL
	10 mM	0.1504 mL	0.7521 mL	1.5042 mL	3.7605 mL
	15 mM	0.1003 mL	0.5014 mL	1.0028 mL	2.5070 mL
	20 mM	0.0752 mL	0.3761 mL	0.7521 mL	1.8803 mL
	25 mM	0.0602 mL	0.3008 mL	0.6017 mL	1.5042 mL
	30 mM	0.0501 mL	0.2507 mL	0.5014 mL	1.2535 mL

Fenebrutinib Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Fenebrutinib1434048-34-6GDC-0853GDC0853GDC 0853BtkBruton tyrosine kinaseInhibitorinhibitorinhibit

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Fenebrutinib (Synonyms: GDC-0853)

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Fenebrutinib Related Antibodies

11 Publications Citing Use of MCE Fenebrutinib

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Fenebrutinib Related Antibodies

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Complete Stock Solution Preparation Table

Fenebrutinib Related Classifications

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