Cat. No. Name Size Price Add Cart
KI2617AVL-29210 mg$390
AVL-29225 mg$650
AVL-29250 mg$1170
AVL-292100 mg$1690
AVL-292200 mg$2470

Chemical Characteristic

Product NameAVL-292
SynonymsCC-292
CAS No.1202757-89-8
Molecular Weight 423.44
FormulaC22H22FN5O3
Chemical NameN-[3-[[5-fluoro-2-[4-(2-methoxyethoxy)anilino]pyrimidin-4-yl]amino]phenyl]prop-2-enamide
SmilesC(=O)(C=C)Nc1cc(ccc1)Nc1nc(ncc1F)Nc1ccc(cc1)OCCOC
Chemical Structure

Biological activities

AVL-292 is a selective and covalent inhibitor of Bruton's tyrosine kinase (Btk). AVL-292 also binds to Cys-481 at the domain of Btk kinase.[1] The IC50 of AVL-292 against Btk is < 0.5 nM. AVL-292 inhibits Btk kinase activity in Ramos cells with an EC50 of 8 nM.[2] AVL-292 treatment inhibits B cell receptor (BCR) signaling and the proliferation of B-cell malignancies.[3] AVL-292 is also reported to show a promising effect in animal models with rheumatoid arthritis.[1] AVL-292 also will be used in the treatment of B cell-related hematological cancers, including non-Hodgkin lymphoma (NHL) and B cell chronic lymphocytic leukemia (B-CLL) in animal models and human trials.[4]

References

[1] Vargas L, et al. Inhibitors of BTK and ITK: State of the New Drugs for Cancer, Autoimmunity and Inflammatory Diseases. Scand J Immunol. 2013, 78(2): 130-139.
[2] E Evans, et al. Clinical Development of AVL-292: A Potent, Selective Covalent Btk Inhibitor for the Treatment of B Cell Malignancies. ASH Annual Meeting. 2011.
[3] Buggy JJ, et al. Bruton tyrosine kinase (BTK) and its role in B-cell malignancy. Int Rev Immunol. 2012 , 31(2): 119-132.
[4] Robak T, et al. Tyrosine kinase inhibitors as potential drugs for B-cell lymphoid malignancies and autoimmune disorders. Expert Opin Investig Drugs. 2012, 21(7): 921-947.

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