GNF 5

• Supplier: Tocris Bioscience
• Catalog: 4399
• Prices: $225.00, $925.00
• Sizes: 10 mg, 50 mg
• Function Type: Inhibitor
• Cas Number: 778277-15-9
• Chemical Name: N-(2-Hydroxyethyl)-3-[6-[[4-(trifluoromethoxy)phenyl]amino]-4-pyrimidinyl]benzamide
• Formula: C20H17F3N4O3
• Molecular Weight: 418.37
• Purity: >98 %
• Description: Selective, non-ATP competitive allosteric inhibitor of Bcr-Abl (IC 50 = 220 nM for wild-type Abl). Binds the myristate-binding site of Abl. Acts in combination with nilotinib to inhibit T315I Bcr-Abl in vitro and in vivo . Analog of GNF 2 (Cat. No. 4399).

Product References

Expanding the diversity of allosteric bcr-abl inhibitors. - Expanding the diversity of allosteric bcr-abl inhibitors.

Deng X, Okram B, Ding Q, Zhang J, Choi Y, Adrian FJ, Wojciechowski A, Zhang G, Che J, Bursulaya B, Cowan-Jacob SW, Rummel G, Sim T, Gray NS. J Med Chem. 2010 Oct 14;53(19):6934-46.

Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors. - Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors.

Zhang J, Adrian FJ, Jahnke W, Cowan-Jacob SW, Li AG, Iacob RE, Sim T, Powers J, Dierks C, Sun F, Guo GR, Ding Q, Okram B, Choi Y, Wojciechowski A, Deng X, Liu G, Fendrich G, Strauss A, Vajpai N, Grzesiek S, Tuntland T, Liu Y, Bursulaya B, Azam M, Manley PW, Engen JR, Daley GQ, Warmuth M, Gray NS. Nature. 2010 Jan 28;463(7280):501-6.

Allosteric interactions between the myristate- and ATP-site of the Abl kinase. - Allosteric interactions between the myristate- and ATP-site of the Abl kinase.

Iacob RE, Zhang J, Gray NS, Engen JR. PLoS One. 2011 Jan 10;6(1):e15929.