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Chemical Structure| 778270-11-4 Chemical Structure| 778270-11-4

Structure of GNF-2
CAS No.: 778270-11-4

Chemical Structure| 778270-11-4

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GNF-2 is a highly selective non-ATP competitive inhibitor of oncogenic Bcr-Abl activity (IC50 = 0.14 μM).

Synonyms: Bcr-Abl Inhibitor

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Product Details of GNF-2

CAS No. :778270-11-4
Formula : C18H13F3N4O2
M.W : 374.32
SMILES Code : O=C(N)C1=CC=CC(C2=NC=NC(NC3=CC=C(OC(F)(F)F)C=C3)=C2)=C1
Synonyms :
Bcr-Abl Inhibitor
MDL No. :MFCD09265253
InChI Key :WEVYNIUIFUYDGI-UHFFFAOYSA-N
Pubchem ID :5311510

Safety of GNF-2

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of GNF-2

RTK

Isoform Comparison

Biological Activity

Target
  • Bcr-Abl

    Bcr-Abl (K562 cell line), IC50:273 nM

    Bcr-Abl (SUP-B15 cell line), IC50:268 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Ba/F3 cells 10 µM To evaluate the inhibitory effect of GNF-2 on Bcr-Abl mutants. Results showed that GNF-2 was completely ineffective against certain mutants (e.g., E505K, P465S, and C464Y). PMC2901986
Ba/F3 cells 1 µM 21 days To evaluate the effect of GNF-2 and imatinib combination on the frequency of resistant mutations. Results showed that the combination significantly reduced the emergence of resistant clones. PMC2901986
K562 cells 10 μM To assess whether ZXH-2-107 exerts antiviral activity through targeted degradation of ABL-family kinases. Results showed that ZXH-2-107 did not induce ABL degradation in K562 cells. PMC11516100
Huh7.5 cells 5 and 10 μM 24 h To evaluate the degradation effect of GNF-2-based degraders on dengue E protein. Results showed that ZXH-2-107 significantly reduced E protein levels at 10 μM, and this degradation was CRBN-dependent. PMC11516100
Vero cells 25 μM 45 min Fluorescence microscopy confirmed the co-localization of GNF2-Cy5 with the dengue virus E protein, demonstrating the interaction of GNF-2 with viral particles. PMC4865888
BHK21 cells 15 μM 1 h Time-of-addition experiments showed that GNF-2 exhibits antiviral activity during the early stages of viral infection. PMC4865888
Huh-7 cells 15 μM 24 h Evaluated the inhibitory effect of GNF-2 on dengue virus replication, showing that GNF-2 has stronger antiviral activity than imatinib. PMC4865888
Recombinant Arg (amino acids 110–581) 100 nM 30 min GNF-2 inhibits Arg tyrosine kinase activity with an IC50 of approximately 0.67 μM, slightly less potent than its inhibition of c-Abl. PMC2781447
Recombinant Abl (amino acids 65–534) 100 nM 30 min GNF-2 inhibits the kinase activity of non-myristoylated c-Abl by binding to the myristate-binding pocket in the C-lobe of the kinase domain, with an IC50 of approximately 0.24 μM. PMC2781447
32D cells 1 μM Screen for compounds specifically inhibiting Bcr-Abl transformed cells, identifying GNF-1 (4a) with an EC50 of 1 μM PMC2951064
Ba/F3.p210 cells 140 nM 48 h Evaluate the antiproliferative activity of GNF-2 against Bcr-Abl transformed cells, showing an EC50 of 140 nM PMC2951064

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.67mL

0.53mL

0.27mL

13.36mL

2.67mL

1.34mL

26.72mL

5.34mL

2.67mL

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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