For research use only. Not for therapeutic Use.
CNX-774 is an orally active, irreversible and selective BTK inhibitor, with an IC50 of < 1 nM. CNX-774 specifically targets Cysteine 481 of Btk for covalent modification[1][2].
CNX-774 strongly inhibits Btk activity in Ramos cells with an IC50 of 1-10 nM. CNX-774 demonstrates strong time- and dose-dependent occupancy of Btk in Ramos cells[1].
CNX-774 is stable and non-reactive in fresh human and rat whole blood and does not covalently bond to any of the mid-level abundance human plasma proteins[1].
CNX-774 demonstrates potent inhibitory activity towards the intended target, Btk, while achieving remarkable specificity in a variety of assays designed to assess off-target reactivity towards abundant cellular thiols and blood proteins[1].
| Catalog Number | I013929 |
| CAS Number | 1202759-32-7 |
| Synonyms | 4-[4-[[5-fluoro-4-[3-(prop-2-enoylamino)anilino]pyrimidin-2-yl]amino]phenoxy]-N-methylpyridine-2-carboxamide |
| Molecular Formula | C26H22FN7O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C26H22FN7O3/c1-3-23(35)31-17-5-4-6-18(13-17)32-24-21(27)15-30-26(34-24)33-16-7-9-19(10-8-16)37-20-11-12-29-22(14-20)25(36)28-2/h3-15H,1H2,2H3,(H,28,36)(H,31,35)(H2,30,32,33,34) |
| InChIKey | VVLHQJDAUIPZFH-UHFFFAOYSA-N |
| SMILES | CNC(=O)C1=NC=CC(=C1)OC2=CC=C(C=C2)NC3=NC=C(C(=N3)NC4=CC(=CC=C4)NC(=O)C=C)F |
| Reference | [1]. Matthew Labenski, et al. In Vitro Reactivity Assessment of Covalent Drugs Targeting Bruton’s Tyrosine Kinase. [2]. Akintunde Akinleye, et al. Ibrutinib and novel BTK inhibitors in clinical development. J Hematol Oncol. 2013 Aug 19;6:59. |
