BTK inhibitor, orally active, irreversible and selective
CAS：1202759-32-7
分子式：C26H22FN7O3
分子量：499.5
纯度：98%
存储：Store at -20°C

Background:

CNX-774 is an orally active and selective inhibitor of BTK with IC50 value of<1 nM.

Bruton’s tyrosine kinase (BTK) is an important enzyme in the B-cell antigen receptor (BCR) signaling pathway and also plays an important role in mast cell activation and B cell maturation.

CNX-774 is an orally active, irreversible and selective BTK inhibitor with IC50 value of<1 nM. CNX-774 formed covalent bond with the Cys481 residue within the ATP binding site of BTK. In cellular assays, CNX-774 inhibited BTK with IC50 values of 1-10 nM [1].

Reference:
[1].  Akinleye A, Chen Y, Mukhi N, et al. Ibrutinib and novel BTK inhibitors in clinical development. J Hematol Oncol, 2013, 6: 59.