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Spebrutinib

Catalog No. T2603 CAS 1202757-89-8

Synonyms: CC-292, LMK-435, AVL-292

Spebrutinib (LMK-435) is an orally bioavailable, selective inhibitor of Bruton's agammaglobulinemia tyrosine kinase (BTK), with potential antineoplastic activity.

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Spebrutinib, CAS 1202757-89-8

Pack Size	Availability	Price/USD
2 mg	In stock	$ 35.00
5 mg	In stock	$ 53.00
10 mg	In stock	$ 77.00
25 mg	In stock	$ 100.00
50 mg	In stock	$ 126.00
100 mg	In stock	$ 207.00
1 mL * 10 mM (in DMSO)	In stock	$ 57.00

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Purity: 100%

Purity: 97.14%

Biological Description

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Description	Spebrutinib (LMK-435) is an orally bioavailable, selective inhibitor of Bruton's agammaglobulinemia tyrosine kinase (BTK), with potential antineoplastic activity.
Targets&IC50	BTK:<0.5 nM
In vitro	Oral administration of 3-30 mg/kg AVL-292 suppresses clinical symptoms of inflammation in a mouse model of collagen-induced arthritis, including the reduction of joint and paw swelling as well as visible redness in the affected paws.
In vivo	AVL-292 inhibits the activity of BTK, subsequently suppressing B-cell proliferation with an EC50 of 3 nM. Additionally, AVL-292 exerts an inhibitory effect on BTK expressed in Ramos cells, with an EC50 of 8 nM, demonstrating dose-dependency, and inhibits the downstream BCR pathway.
Kinase Assay	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	A suspension of resting purified na?ve 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)

Synonyms	CC-292, LMK-435, AVL-292
Molecular Weight	423.44
Formula	C22H22FN5O3
CAS No.	1202757-89-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 79 mg/mL (186.6 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Evans E, et al. ASH Annual Meeting, 2011 San Diego, CA. 2. Evans EK, et al. J Pharmacol Exp Ther. 2013, 346(2), 219-228.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Highly Selective Inhibitor Library Drug Repurposing Compound Library Inhibitor Library Tyrosine Kinase Inhibitor Library Immunology/Inflammation Compound Library Anti-Cancer Compound Library Angiogenesis related Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Spebrutinib 1202757-89-8 Angiogenesis Tyrosine Kinase/Adaptors BTK Src inhibit Bruton tyrosine kinase CC 292 CC-292 Btk LMK-435 AVL 292 CC292 Inhibitor LMK 435 AVL292 AVL-292 LMK435 inhibitor

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