839708-29-1
Chemical Structure
GNF-6
- CAS No.: 839708-29-1
- Formula:C22H19F3N6O2
- Molecular Weight:456.42
InChIKey: ZWVLMQTXUWMUII-UHFFFAOYSA-N
SMILES: O=C(C1=CC=CC(C(F)(F)F)=C1)NC2=CC=C(C)C(N3C(N(C)C4=NC(N)=NC=C4C3)=O)=C2
Biological Activity: 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].
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GNF-6 | 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. | |||||||||||||||||||||
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Keywords
