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Home > Chemicals > Inhibitors, Activators, Antagonists, and Agonists > A-Z Inhibitors, Activators, Antagonists, and Agonists > AVL-292 (SPEBRUTINIB)

AVL-292 (SPEBRUTINIB)

Spebrutinib, CC-292

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Description

Background Information:

B-cell antigen receptor (BCR) signaling is required for tumor expansion and proliferation. Bruton's Tyrosine Kinase (BTK) is an essential element of the BCR signaling pathway, playing an important role in B lymphocyte development, activation, signaling, proliferation and survival. Inhibiting BTK blocks BCR signaling and is of therapeutic significance in the treatment of both of B cell-related hematological cancers (e.g. non-Hodgkin lymphoma (NHL) and B cell chronic lymphocytic leukemia (B-CLL), and autoimmune diseases (e.g. rheumatoid arthritis). AVL-292 is a potent, selective and orally bioavailable irreversible inhibitor of BTK with IC50 value at low nM, currently in clinical trials.

Reference:

1. Robak T, et al, Tyrosine kinase inhibitors as potential drugs for B-cell lymphoid malignancies and autoimmune disorders. Expert Opin Investig Drugs. 2012 Jul;21(7):921-47.

APIM050012: AVL-292 (SPEBRUTINIB)

CAS No.: 1202757-89-8.
Molecular Formula: C22H22FN5O3.
Molecular Weight: 423.
Purity: >98.5% by HPLC.
QC: HPLC-MS, 1HNMR, and Quantitative Elemental Analysis.
Solubility: Soluble in DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.

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