Catalog No.S7173 Synonyms: CC-292,LMK-435
Molecular Weight(MW): 423.44
CC-292 (AVL-292) is a covalent, orally active, and highly selective BTK inhibitor with IC50 of <0.5 nM, displaying at least 1400-fold selectivity over the other kinases assayed. Phase 1.
Purity & Quality Control
Choose Selective BTK Inhibitors
|Description||CC-292 (AVL-292) is a covalent, orally active, and highly selective BTK inhibitor with IC50 of <0.5 nM, displaying at least 1400-fold selectivity over the other kinases assayed. Phase 1.|
|Features||Orally bioavailable BTK-selective inhibitor that has been tested in Phase I clinical trials for treatment of relapsed or refractory B-NHL, CLL and WM.|
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. |
Procedures for BTK OMNIA Assay:The Omnia continuous read assay is performed essentially as described by the vendor. The assay conditions are: 40 μM ATP (1X KMATP), 10 μM Y5-Sox, and 10 nM BTK enzyme. Briefly, a substrate mix containing 1.13X ATP and the Y5 Sox substrate is first prepared in 1X Omnia Kinase Reaction Buffer (KRB) consisting of 20 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EGTA, 5 mMβ-glycerophosphate, 5% glycerol, and 0.2 mM DTT. For IC50 measurements, 5 μL of enzyme are incubated with serially diluted (3-fold) compounds prepared in 50% DMSO in a Corning (#3574) 384-well, white, non-binding surface microtiter plate at 25°C for 30 min. Kinase reactions are started with the addition of 45 μL of the ATP/Y5 substrate mix and monitored at λex360/λem485 in a Synergy 4 plate reader for 60 minutes. Progress curves from each well are examined for linear reaction kinetics and fit statistics. Initial velocity from each reaction is determined from the slope of a plot of relative fluorescence units versus time and then plotted against inhibitor concentration to estimate IC50 using the Response, Variable Slope model in GraphPad Prism from GraphPad Software.
|In vitro||DMSO||85 mg/mL (200.73 mM)|
* 1 mg/ml means slightly soluble or insoluble.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02433457||Completed||Healthy Volunteers||Celgene Corporation|Celgene||May 2014||Phase 1|
|NCT02031419||Recruiting||Lymphoma, Large B-Cell, Diffuse||Celgene Corporation||December 2013||Phase 1|
|NCT01975610||Completed||Rheumatoid Arthritis||Celgene Corporation||October 2013||Phase 2|
|NCT01766583||Active, not recruiting||Relapsed/Refractory B-cell Lymphoma||The Lymphoma Academic Research Organisation|Celgene Corporation||February 2013||Phase 1|
|NCT01732861||Active, not recruiting||Leukemia Lymphocytic Chronic B-Cell||Celgene Corporation||December 2012||Phase 1|
|NCT01744626||Completed||Leukemia Lymphocytic Chronic B-Cell||Celgene Corporation||December 2012||Phase 1|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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