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GNF-5

Cat. No. M2603
GNF-5 Structure
Size Price Availability Quantity
10mg USD 60 In stock
50mg USD 170 In stock
100mg USD 240 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

GNF-5 is a cell-permeable GNF-2 N-hydroxyethyl carboxamide analog.It exhibits in vivo efficacy in suppressing the proliferation of Bcr-abl-expressing Ba/F3 in murine xenograft models of leukemia.GNF-5 shows potent antiproliferative activity with EC50 of 430 nM and 580 nM against wt-Bcr-Abl and E255K mutant Bcr-Abl transformed cells, respectively. GNF-5 is ineffective toward the myristate-binding site mutant E505K and the ATP-binding site 'gatekeeper' mutant T315I.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 418.37
Formula C20H17F3N4O3
CAS Number 778277-15-9
Purity >99%
Solubility DMSO
Storage at -20°C
References

Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors.
Zhang J,et al. Nature. 2010 Jan 28;463(7280). PMID: 20072125.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: GNF-5 supplier, Src-bcr-Abl, inhibitors

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