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GNF-5

Cat. No. M2603
GNF-5 Structure
Size Price Availability Quantity
10mM*1mL in DMSO USD 65  USD65 In stock
10mg USD 60  USD60 In stock
50mg USD 170  USD170 In stock
100mg USD 240  USD240 In stock
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Quality Control & Documentation
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.

Chemical Information
Molecular Weight 418.37
Formula C20H17F3N4O3
CAS Number 778277-15-9
Solubility (25°C) DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Zhang J,et al. Nature. Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors.

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