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GDC-0853 (Fenebrutinib)

Cat. No. M8941
GDC-0853 (Fenebrutinib) Structure

Fenebrutinib; RG7845

Size Price Availability Quantity
2mg USD 65  USD65 In stock
5mg USD 102  USD102 In stock
10mg USD 180  USD180 In stock
25mg USD 405  USD405 In stock
50mg USD 720  USD720 In stock
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Quality Control & Documentation
Biological Activity

GDC-0853 (Fenebrutinib) is a potent, selective and non-covalent bruton tyrosine kinase (Btk) inhibitor with a Ki value of 0.91 nM against BRK. GDC-0853 inhibits the activity of BTK and prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. This prevents both B-cell activation and BTK-mediated activation of downstream survival pathways, which leads to the inhibition of the growth of malignant B-cells that overexpress BTK.

Chemical Information
Molecular Weight 664.8
Formula C37H44N8O4
CAS Number 1434048-34-6
Solubility (25°C) DMSO ≥ 20 mg/mL
Storage 2-8°C, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.


[1] H Yesid Estupin, et al. Comparative Analysis of BTK Inhibitors and Mechanisms Underlying Adverse Effects

[2] Ayse Bag-Ozbek, et al. Emerging B-Cell Therapies in Systemic Lupus Erythematosus

[3] Kirti J Johal, et al. Current and emerging treatments for chronic spontaneous urticaria

[4] Pavel Kolkhir, et al. New treatments for chronic urticaria

[5] James J Crawford, et al. Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development

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Keywords: GDC-0853 (Fenebrutinib), Fenebrutinib; RG7845 supplier, BTK, inhibitors, activators

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