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Chemical Structure| 778277-15-9 Chemical Structure| 778277-15-9

Structure of GNF-5
CAS No.: 778277-15-9

Chemical Structure| 778277-15-9

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GNF-5 is a selective non-ATP competitive inhibitor of Bcr-Abl with IC50 of 220 nM, it's an analogue of GNF-2 with improved pharmacokinetic properties.

4.5 *For Research Use Only! Not for Human Use. We Do Not Sell to Patients.

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Product Details of GNF-5

CAS No. :778277-15-9
Formula : C20H17F3N4O3
M.W : 418.37
SMILES Code : O=C(NCCO)C1=CC=CC(C2=NC=NC(NC3=CC=C(OC(F)(F)F)C=C3)=C2)=C1
English Name :N-(2-Hydroxyethyl)-3-(6-((4-(trifluoromethoxy)phenyl)amino)pyrimidin-4-yl)benzamide
MDL No. :MFCD16877246
InChI Key :IIQUYGWWHIHOCF-UHFFFAOYSA-N
Pubchem ID :44129660

Safety of GNF-5

Related Pathways of GNF-5

RTK

Isoform Comparison

Biological Activity

Target
  • Bcr-Abl

    Bcr-Abl, IC50:220 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Human airway smooth muscle (HASM) cells 5 µM 1 hour or 24 hours To evaluate the inhibitory effect of GNF-5 on c-Abl, it was found that GNF-5 reduced the number of cells undergoing cytokinesis, increased the quantity of cells in metaphase/anaphase, and increased the number of multinucleate cells Am J Respir Cell Mol Biol. 2014 Jun;50(6):1076-83.
Mouse tracheal rings 10 µM 10 minutes To evaluate the inhibitory effect of GNF-5 on acetylcholine-induced contraction of tracheal rings, results showed that GNF-5 significantly attenuated the contraction of tracheal rings. Respir Res. 2013 Oct 11;14(1):105.
Human ASM cells 10 µM 10 minutes To assess the cooperative effects of β-agonists and c-Abl inhibitors on ASM contraction, results showed that GNF-5 and β-agonist ISO combined significantly enhanced ASM relaxation. FASEB J. 2021 Jul;35(7):e21674.
Ba/F3 cells 2 µM Combinations of GNF-5 and nilotinib inhibited T315I Bcr-Abl-dependent cell growth, showing moderate synergy. Nature. 2010 Jan 28;463(7280):501-6.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c mice OVA-induced asthma model Intranasal administration 10 mg/kg 1 hour before and 5 hours after each OVA challenge, lasting for three weeks To evaluate the inhibitory effect of GNF-5 on airway resistance and airway smooth muscle hyperplasia in the OVA-induced asthma model, results showed that GNF-5 significantly inhibited the increase in airway resistance and smooth muscle growth. Respir Res. 2013 Oct 11;14(1):105.
Mice Murine precision cut lung slices model In vitro treatment 10 μM 20 minutes To assess the cooperative effects of GNF-5 and β-agonist ISO on ASM contraction, results showed that GNF-5 and ISO combined significantly enhanced ASM relaxation. FASEB J. 2021 Jul;35(7):e21674.
Mice T315I Bcr-Abl bone marrow transplantation model Oral 75 mg/kg Twice daily for 15 days The combination of GNF-5 with nilotinib showed significant efficacy in the T315I Bcr-Abl bone marrow transplantation model, normalizing blood cell counts and spleen size, and significantly extending the survival of mice. Nature. 2010 Jan 28;463(7280):501-6.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.39mL

0.48mL

0.24mL

11.95mL

2.39mL

1.20mL

23.90mL

4.78mL

2.39mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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