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.
Product information
CAS Number: 1202757-89-8
Molecular Weight: 423.44
Formula: C22H22FN5O3
Synonym:
CC-292
Spebrutinib
Chemical Name: N-{3-[(5-fluoro-2-{[4-(2-methoxyethoxy)phenyl]amino}pyrimidin-4-yl)amino]phenyl}prop-2-enamide
Smiles: COCCOC1C=CC(=CC=1)NC1=NC(NC2=CC(=CC=C2)NC(=O)C=C)=C(F)C=N1
InChiKey: KXBDTLQSDKGAEB-UHFFFAOYSA-N
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)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
AVL-292 exhibits dose-dependent inhibition of Btk with EC50 of 8 nM and downstream BCR signaling components in Ramos cells. AVL-292, by inhibiting BTK activities, further inhibits B cell proliferation with EC50 of 3 nM.
In Vivo:
In a collagen-induced arthritis mouse model, AVL-292 (3- 30 mg/kg, p.o.) dose-dependently inhibits the clinical signs of inflammatory disease, including reduction in joint and paw swelling and visible redness of the affected paws.
References:
- Evans EK, et al. J Pharmacol Exp Ther. 2013, 346(2), 219-228.
- Evans E, et al. ASH Annual Meeting, 2011 San Diego, CA.
Products are for research use only. Not for human use.
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