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AVL 292
- CC 292 - Spebrutinib
Axon 2226
CAS:
1202757-89-8
Purity:
98%
- Soluble in DMSO
- MF: C22H22FN5O3
- MW: 423.44
Description
AVL 292 (Spebrutinib) is a potent, selective, orally bioavailable and covalent Brutons tyrosine kinase (BTK) inhibitor. It is more specific for BTK than ibrutinib (Axon 1858) in the cited comparison and reduces CLL cell migration toward CXCL12 and CXCL13.
BTK is a central mediator of B cell receptor signaling and is a therapeutic target in B cell malignancies and autoimmune disease. AVL 292 is relevant for studying covalent BTK inhibition, CLL survival and BCR-associated chemokine signaling.
Key Features
- Covalent BTK inhibitor
- Selective and orally bioavailable kinase inhibitor scaffold
- Reduces CLL migration toward CXCL12 and CXCL13
- Suppresses BCR activation markers in CLL co-culture systems
Applications
- BTK kinase assays
- B cell receptor signaling research
- CLL migration and survival studies
- Covalent kinase inhibitor profiling
More Information
| Parent CAS No. | 1202757-89-8 |
|---|---|
| Chemical Name | N-(3-(5-Fluoro-2-(4-(2-methoxyethoxy)phenylamino)pyrimidin-4-ylamino)phenyl)acrylamide |
| SMILES | C(NC1=CC=CC(NC2C(F)=CN=C(NC3=CC=C(OCCOC)C=C3)N=2)=C1)(=O)C=C |
| MFCD | N.A. |
| InChi | InChI=1S/C22H22FN5O3/c1-3-20(29)25-16-5-4-6-17(13-16)26-21-19(23)14-24-22(28-21)27-15-7-9-18(10-8-15)31-12-11-30-2/h3-10,13-14H,1,11-12H2,2H3,(H,25,29)(H2,24,26,27,28) |
| InChiKey | KXBDTLQSDKGAEB-UHFFFAOYSA-N |
| CID | 59174488 |
| Short Description | BTK inhibitor |
AVL 292 (Spebrutinib)
covalent BTK inhibitor
AVL 292
Spebrutinib
CC 292
AVL292
CC292
covalent BTK
Inhibitor
BTK kinase assays
B cell receptor signaling research
CLL migration and survival studies
Covalent kinase inhibitor profiling
kinase signaling
receptor selectivity
signal transduction
receptor pharmacology
drug discovery
enzyme pharmacology
Axon Medchem
Axon 2226
Supplier
Vendor
References
- E.K. Evans et al. Inhibition of Btk with CC-292 provides early pharmacodynamic assessment of activity in mice and humans. J. Pharmacol. Exp. Ther. 2013, 346, 219-228.
- H. Eda et al. A novel Bruton′s tyrosine kinase inhibitor CC-292 in combination with the proteasome inhibitor carfilzomib impacts multiple myeloma bone microenviroment with resultant anti-myeloma activity. Blood 2013, 122, 682.
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