GNF-5

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Chemical Information

Product name：GNF-5	Purity：98% min
CAS NO：778277-15-9	Solubility：DMSO : ≥ 49 mg/mL (117.12 mM)
Molecular Formula：C₂₀H₁₇F₃N₄O₃	Package：Package according to customer requirements
Molecular Weight：418.369	Storage：Store at -20℃

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Remarks

GNF-5 is a selective allosteric inhibitor of Bcr-Abl (IC50 = 220 nM for wild-type Abl). GNF-5 has improved pharmacokinetic properties, when used in combination with the ATP-competitive inhibitors imatinib or nilotinib, suppressed the emergence of resistance mutations in vitro, displayed additive inhibitory activity in biochemical and cellular assays against T315I mutant human Bcr-Abl and displayed in vivo efficacy against this recalcitrant mutant in a murine bone-marrow transplantation model.

References

[1]. Zhang J, et al. Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors. Nature. 2010 Jan 28;463(7280):501-6.

[2]. Meirson T, et al. Targeting invadopodia-mediated breast cancer metastasis by using ABL kinase inhibitors. Oncotarget. 2018 Apr 24;9(31):22158-22183.