1. Protein Tyrosine Kinase/RTK
    Anti-infection
  2. Bcr-Abl
    SARS-CoV
  3. GNF-2

GNF-2 

Cat. No.: HY-11007 Purity: 99.10%
Handling Instructions

GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC50 of 138 nM .

For research use only. We do not sell to patients.

GNF-2 Chemical Structure

GNF-2 Chemical Structure

CAS No. : 778270-11-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 77 In-stock
Estimated Time of Arrival: December 31
5 mg USD 70 In-stock
Estimated Time of Arrival: December 31
10 mg USD 120 In-stock
Estimated Time of Arrival: December 31
50 mg USD 450 In-stock
Estimated Time of Arrival: December 31
100 mg USD 750 In-stock
Estimated Time of Arrival: December 31
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Based on 2 publication(s) in Google Scholar

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Description

GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC50 of 138 nM [1].

IC50 & Target[1]

Bcr-Abl

 

In Vitro

GNF-2 selectively inhibits Bcr-abl-dependent cell proliferation. GNF-2 (0.005-10 μM; 48 hours) specifically inhibits the proliferation of the Bcr-abl-expressing cells with an IC50 of 138 nM and not show any cytotoxic effects on the nontransformed cells at concentrations of up to 10 μM. GNF-2 (0.005-10 μM; 48 hours) causes a dose-dependent growth inhibition of the Bcr-abl-positive cell lines with IC50 values of 273 nM (K562) and 268 nM (SUP-B15). GNF-2 (0.005-10 μM; 48 hours) inhibits E255V and Y253H mutant Bcr-abl cell growth (IC50 values of 268 and 194 nM, respectively)[1].
GNF-2 (1-10 μM; 48 hours) induces apoptosis of Bcr-abl-transformed cells[1].
GNF-2 (0.1-10 μM; 90 minutes) inhibits the cellular tyrosine phosphorylation of Bcr-abl in a dose-dependent manner with an IC50 of 267 nM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: Ba/F3.p210, Ba/F3.p210E255V and Ba/F3.p185Y253H cells
Concentration: 0.005, 0.01, 0.1, 1, 10 μM
Incubation Time: 48 hours
Result: Inhibited Bcr-abl-transformed cells proliferation.

Apoptosis Analysis[1]

Cell Line: Ba/F3.p210 and Ba/F3.p210E255V cells
Concentration: 1, 10 μM
Incubation Time: 48 hours
Result: Increased number of Ba/F3.p210 cells undergoing apoptosis at 1 μM for 48 h.
Ba/F3.p210E255V underwent apoptotic death after 48 h incubation in the presence of 1 μM or higher concentration.

Western Blot Analysis[1]

Cell Line: Ba/F3.p210 and Ba/F3.p210E255V cells
Concentration: 0.1, 1, 10 μM
Incubation Time: 90 minutes
Result: Decreased the autophosphorylation levels at a concentration of 1 μM and were barely detectable at 10 μM, whereas the level of total Bcr-abl remained unchanged.
Induced a significant decrease in the levels of p-Stat5 (at Y694) at 1 μM in Ba/F3.p210 and Ba/F3.p210E255V cells.
In Vivo

GNF-2 (10 mg/kg; i.p. for 8 days) protects LPS (5 mg/kg) induced bone erosion in mice. GNF-2 protects the LPS induced bone loss and abrogates the LPS-induced decreases of bone volume/tissue volume (BV/TV) of LPS-treated mice[2].
GNF-2 prevents the LPS-induced increases of N.Oc/B.Pm, the percentage of Oc.S/BS, and the percentage of ES/BS[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Eight-week-old C57/BL6 mice were administered i.p. injections of LPS (5 mg/kg)[2]
Dosage: 10 mg/kg
Administration: I.p. injections for 8 days; 1 day before and every day after the LPS injection
Result: Prevented inflammatory bone destruction in vivo.
Molecular Weight

374.32

Formula

C₁₈H₁₃F₃N₄O₂

CAS No.

778270-11-4

SMILES

O=C(C1=CC=CC(C2=CC(NC3=CC=C(OC(F)(F)F)C=C3)=NC=N2)=C1)N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (267.15 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6715 mL 13.3576 mL 26.7151 mL
5 mM 0.5343 mL 2.6715 mL 5.3430 mL
10 mM 0.2672 mL 1.3358 mL 2.6715 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.68 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.68 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.68 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

GNF-2GNF2GNF 2Bcr-AblSARS-CoVSARS coronavirusallostericnon-ATP competitive inhibitorBa/F3.p210Ba/F3.p210E255VBa/F3.p185Y253Hbone erosionInhibitorinhibitorinhibit

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GNF-2
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