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Spebrutinib (AVL-292) is an orally available and highly selective covalent inhibitor of Bruton's tyrosine kinase (Btk) that is currently undergoing Phase 1b clinical development for CLL and B-NHL. AVL-292 selectively and covalently bonds to Btk to inactivate and silence its activity. Spebrutinib (AVL-292) inhibited osteoclast function and reduced osteoclast-stimulated proliferation of MM cells. Spebrutinib (AVL-292) was well tolerated from 125-400 mg po QD and early efficacy analysis in CLL and B-NHL shows 10/11 efficacy evaluable pts with SD. The ongoing phase Ib clinical trial of AVL-292 is being conducted in patients with B-cell malignancies, including B-cell NHL, CLL, and WM.
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Source | Allergy (2017). Figure 1. AVL-292 |
| Method | flow cytometry | |
| Cell Lines | HMC-1 cells, and KU812 cells | |
| Concentrations | 0.01-10 μmol/L | |
| Incubation Time | 4 hours | |
| Results | We found that dasatinib, ibrutinib, AVL-292, and CNX-774 counteract anti-IgE-induced expression of pBTK in BA |
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Source | Allergy (2017). Figure 5. AVL-292 |
| Method | proliferation assay | |
| Cell Lines | HMC-1 cells and KU812 cells | |
| Concentrations | 0.001-10 μmol/L | |
| Incubation Time | 48 h | |
| Results | As determined by 3H-thymidine uptake, ibrutinib, AVL-292, and P505-15 showed no significant effects on proliferation of HMC-1.1, HMC-1.2, and KU812 cells unless high concentrations (≥1 μmol/L) were applied |
| Cell Experiment | |
|---|---|
| Cell lines | naïve human B cells |
| Preparation method | Immunoblot Analysis. Cells were incubated in serum-free RPMI media for 1–1.5 hours. Isolated human B cells were incubated with CC-292 at a final concentration of 0.001, 0.01, 0.1 and 1 μM. Ramos cells were incubated with 0.1 nM–3 μM CC-292. Cells were then incubated in the presence of compound for 1 hour at 37°C. Following incubation, cells were centrifuged and resuspended in 100 μl of serum-free RPMI and BCR was stimulated with addition of 5 μg/ml α-human IgM. Samples were centrifuged, washed in phosphate-buffered saline (PBS), and lysed in 100 μl of Cell Extraction Buffer plus 1:10 (v/v) PhosSTOP Phosphatase Inhibitor and 1:10 (v/v) Complete Protease Inhibitor. Antibodies used for immunoblot analysis include P-PLCγ2, PLCγ2, Syk, P-Syk, Btk, P-Btk, and Tubulin. Membranes were scanned on a Li-Cor Odyssey scanner using infrared fluorescence detection. |
| Concentrations | 0.001, 0.01, 0.1 and 1 μM |
| Incubation time | 1h |
| Animal Experiment | |
|---|---|
| Animal models | Collagen-Induced Arthritis Model |
| Formulation | not mentioned |
| Dosages | 10,30,50 mg/kg |
| Administration | oral |
| Molecular Weight | 423.44 |
| Formula | C22H22FN5O3 |
| CAS Number | 1202757-89-8 |
| Solubility (25°C) | DMSO 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Danilo De Novellis, et al. The TKI Era in Chronic Leukemias
[2] Emanuela Grassilli, et al. p65BTK Is a Novel Biomarker and Therapeutic Target in Solid Tumors
| Related BTK Products |
|---|
| PCI-32765
PCI-32765 (Ibrutinib) is a potent, selective and orally bioavailable irreversible inhibitor of BTK with IC50 value of 0.46 nM. |
| CNX-774
CNX-774 is an irreversible, orally active, and highly selective BTK inhibitor with IC50 of <1 nM. |
| GDC-0834
GDC-0834 is a novel potent and selective BTK inhibitor with IC50 of 5.9 nM. |
| CGI1746
CGI1746 is a potent and highly selective small-molecule inhibitor of the Btk with IC50 of 1.9 nM. |
| RN486
RN486 is a Bruton's tyrosine kinase (Btk) inhibitor with an IC50 Value of 4.0 nM. |
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