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.
| Molecular Weight | 664.8 |
| Formula | C37H44N8O4 |
| CAS Number | 1434048-34-6 |
| Solubility (25°C) | DMSO ≥ 20 mg/mL |
| Storage | 2-8°C, sealed |
| 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.
[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
| Related BTK Products |
|---|
| TL-925
TL-925 is a potentially first-in-class Bruton's tyrosine kinase (BTK) inhibitor that targets mast cell-mediated ocular inflammation and hypersensitivity and can be used in studies related to dry eye. |
| JAK3/BTK-IN-6
JAK3/BTK-IN-6 is a potent BTK and JAK3 dual inhibitor, with IC50 values of 0.6 and 0.4 nM, respectively. |
| NX-2127
NX-2127 is an orally active, potent BTK inhibitor that induces degradation of mutant BTKC481S in cells, as well as inhibits the proliferation of BTKC481S mutant TMD8 cells. In addition, NX-2127 stimulates T cell activation and increases IL-2 production in primary human T cells. |
| DBt-10
DBt-10 is a potent BTK degrader. |
| BTK-IN-27
BTK-IN-27 is a BTK inhibitor (IC50: 0.2 nM). |
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