GNF-6 (Compound 14) inhibits the gatekeeper threonine residue mutation of BCR-ABL-T315I with IC50s of 0.25 µM, 0.09 µM and 0.590 µM for c-ABL-T334I, BCR-ABL and BCR-ABL-T315I variants, respectively. GNF-6, an ATP competitive inhibitor, disrupts the assembly of the hydrophobic spine (a network of hydrophobic interactions), thereby locking the kinase in an inactive 'DFG-out conformation[1].
Molecular Weight:
456.42
CAS Number:
[839708-29-1]
Formula:
C22H19F3N6O2
Target:
Bcr-Abl
Application Notes:
Reference compound
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