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[1].
Product Specifications
CAS Number
839708-29-1
UNSPSC
12352005
Target
Bcr-Abl
Type
Reference compound
Related Pathways
Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/gnf-6.html
Solubility
10 mM in DMSO
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
Molecular Formula
C22H19F3N6O2
Molecular Weight
456.42
References & Citations
[1]David F. Woodward, et al. Non-acidic cyclopentane heptanoic acid, 2-cycloalkyl or arylalkyl derivatives as therapeutic agents. WO1994006433A1.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Frequently Asked Questions
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