Free shipping on all orders over $ 500

GDC-0853 (Fenebrutinib)

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

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
Free Delivery on orders over USD 500 Bulk Inquiry?

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.

References

[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

Related BTK Products
BCPyr

BCPyr is a new candidate BTK degradation agent (DC50 = 800 nM).

BMS-986143

BMS-986143 is a potent, reversible inhibitor of tyrosine kinase (BTK), which has been successfully targeted by a number of irreversible tumor compounds.

BIIB091

The reversible BTK kinase inhibitor BIIB091 is a highly selective phase I clinical candidate compound for multiple sclerosis.

TAK-020

TAK-020 is a highly selective oral covalent BTK inhibitor with a promising safety and tolerability profile for both hematologic malignancies and autoimmune diseases.

BTK inhibitor 1 (Compound 27)

BTK inhibitor 1 (compound 27) is an inhibitor of BTK with an IC50 of 0.11 nM for Btk and inhibits B cell activation in hWB with an IC50 of 2 nM.

  Catalog
Abmole Inhibitor Catalog




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

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.