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CNX-774 Catalog No.GC13439

BTK inhibitor, orally active, irreversible and selective

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Sample solution is provided at 25 µL, 10mM.

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Chemical Properties

Cas No. 1202759-32-7 SDF
Chemical Name 4-[4-[[5-fluoro-4-[3-(prop-2-enoylamino)anilino]pyrimidin-2-yl]amino]phenoxy]-N-methylpyridine-2-carboxamide
Canonical 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
Formula C26H22FN7O3 M.Wt 499.5
Solubility Soluble in DMSO Storage Store at -20° C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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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].

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