CC-292 (AVL-292)

Catalog No.S7173 Synonyms: CC-292,LMK-435

CC-292 (AVL-292) Chemical Structure

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.

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1 Customer Review

  • J Biomol Screen, 2015, 20(7):876-886.. CC-292 (AVL-292) purchased from Selleck.

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

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.
Targets
BTK [1] YES [2] c-Src [2] BRK [2] Lyn [2]
<0.5 nM 723 nM 1.729 μM 2.43 μM 4.401 μM
In vitro

AVL-292 exhibits dose-dependent inhibition of Btk with EC50 of 8 nM and downstream BCR signaling components in Ramos cells. [1] AVL-292, by inhibiting BTK activities, further inhibits B cell proliferation with EC50 of 3 nM. [2]

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. [2]

Protocol

Kinase Assay:[2]
+ Expand

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 mMβ-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.
Cell Research:[2]
+ Expand
  • Cell lines: Human B cells
  • Concentrations: ~1000 nM
  • Incubation Time: 72 hours
  • Method: A suspension of resting purified naïve human B cells isolated by negative selection in RPMI is prepared at 0.4–0.5 × 106 cells/ml. Cells are mixed together with α-human IgM (final concentration of 5 μg/ml in each well) and vehicle (dimethyl sulfoxide) or AVL-292 (final concentrations of 0.01, 0.1, 1.0, 10.0, 100.0, or 1000 nM per well) and seeded in a 96-well plate. Cells are incubated for 56 hours in a humidified incubator maintained at 37°C and 5% CO2. 3H-Thymidine is added (final concentration of 1 μCi in each well) and cells are incubated overnight, harvested, and measured for 3H incorporation. Experiments are performed in triplicate.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 85 mg/mL (200.73 mM)
Water <1 mg/mL
Ethanol <1 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 423.44
Formula

C22H22FN5O3

CAS No. 1202757-89-8
Storage powder
in solvent
Synonyms CC-292,LMK-435

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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

Tech Support

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.

Handling Instructions

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BTK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID