WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 204480
Description: Spebrutinib, also known as AVL-292 or CC-292, is an orally bioavailable, selective inhibitor of BrutonÂ’s agammaglobulinemia tyrosine kinase (BTK), with potential antineoplastic activity. Upon administration, AVL-292 targets and covalently binds to BTK, thereby preventing its activity. By irreversibly inhibiting BTK, administration of this agent may lead to an inhibition of B cell receptor (BCR) signaling and may inhibit cell proliferation of B-cell malignancies.
MedKoo Cat#: 204480
Chemical Formula: C22H22FN5O3
Exact Mass: 423.17067
Molecular Weight: 423.44
Elemental Analysis: C, 62.40; H, 5.24; F, 4.49; N, 16.54; O, 11.34
Synonym: CC292; CC-292; CC 292; AVL292; AVL-292; AVL 292; Spebrutinib.
IUPAC/Chemical Name: N-(3-((5-fluoro-2-((4-(2-methoxyethoxy)phenyl)amino)pyrimidin-4-yl)amino)phenyl)acrylamide
InChi Key: KXBDTLQSDKGAEB-UHFFFAOYSA-N
InChi Code: 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)
SMILES Code: C=CC(NC1=CC=CC(NC2=NC(NC3=CC=C(OCCOC)C=C3)=NC=C2F)=C1)=O
AVL-292 has demonstrated efficacy in animal models of rheumatoid arthritis and multiple sclerosis, diseases in which B cells play an important role. Btk plays a critical role in the development and activation of B cells, and its inhibition will be of therapeutic significance in the treatment of both of B cell-related hematological cancers (e.g. non-Hodgkin lymphoma (NHL) and B cell chronic lymphocytic leukemia (B-CLL), and autoimmune diseases (e.g. rheumatoid arthritis). (source: http://www.avilatx.com/pipeline/bruton%27s-tyrosine-kinase-inhibitor-program.html).
1: Burger JA. Bruton's tyrosine kinase (BTK) inhibitors in clinical trials. Curr Hematol Malig Rep. 2014 Mar;9(1):44-9. doi: 10.1007/s11899-013-0188-8. PubMed PMID: 24357428.