Spebrutinib

SKU: orb1305275

Description

Spebrutinib (LMK-435) is an oral, selective, and irreversible inhibitor of Bruton's tyrosine kinase (BTK). It is utilized in preclinical research for studying B-cell malignancies and autoimmune diseases, demonstrating activity in both cellular assays and animal models.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1202757-89-8
• MW: 423.44
• Purity: 97.14% (May vary between batches)
• Formula: C₂₂H₂₂FN₅O₃
• SMILES: COCCOc1ccc(Nc2ncc(F)c(Nc3cccc(NC(=O)C=C)c3)n2)cc1
• Target: Src|||BTK
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.72 mM);DMSO:79 mg/mL (186.57 mM)

Bioactivity

• Target IC50:
  BTK:<0.5 nM
• 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.
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• 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.
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• 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)
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Yes, Spebrutinib, AVL 292, AVL292, AVL-292, Bruton tyrosine kinase, Btk, BTK, CC292, CC-292, CC 292, BRK, c-Src, inhibit, LMK 435, LMK435, LMK-435, Lyn, Inhibitor

Compound Identifiers

PubChem CID

59174488