GNF-6 (Compound 14), an ATP competitive inhibitor, inhibits the gatekeeper threonine residue mutation of BCR-ABL-T315I with IC50 values of 0.25 µM for c-ABL-T334I, 0.09 µM for BCR-ABL, and 0.590 µM for BCR-ABL-T315I variants. It disrupts the assembly of the hydrophobic spine (a network of hydrophobic interactions), locking the kinase in an inactive DFG-out conformation [1].
Molecular Weight:
456.42
CAS Number:
[839708-29-1]
Formula:
C22H19F3N6O2
Target:
Bcr-Abl
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