1. Neuronal Signaling
    Protein Tyrosine Kinase/RTK
  2. Trk Receptor
  3. GNF-5837

GNF-5837 

Cat. No.: HY-13491 Purity: 99.19%
Handling Instructions

GNF-5837 is a potent, selective, and orally bioavailable pan-tropomyosin receptor kinase (TRK) inhibitor which display antiproliferative effects in cellular Ba/F3 assays ( IC50 values of 7 nM, 9 nM and 11 nM for cells containing the fusion proteins Tel-TrkC, Tel-TrkB and Tel-TrkA, respectively) .

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

GNF-5837 Chemical Structure

GNF-5837 Chemical Structure

CAS No. : 1033769-28-6

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 59 In-stock
Estimated Time of Arrival: December 31
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10 mg USD 90 In-stock
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25 mg USD 150 In-stock
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50 mg USD 240 In-stock
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100 mg USD 400 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

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Description

GNF-5837 is a potent, selective, and orally bioavailable pan-tropomyosin receptor kinase (TRK) inhibitor which display antiproliferative effects in cellular Ba/F3 assays ( IC50 values of 7 nM, 9 nM and 11 nM for cells containing the fusion proteins Tel-TrkC, Tel-TrkB and Tel-TrkA, respectively) [1].

IC50 & Target[1]

TrkB

9 nM (IC50)

TrkC

7 nM (IC50)

TrkA

11 nM (IC50)

In Vitro

GNF-5837 (0.1-500 nM; 72-144 hours; GOT1 cells) treatment decreases cell viability in a time- and dose-dependent manner in GOT1 cells[2].
GNF-5837 (5-500 nM; 24 hours; GOT1 cells) causes downregulation of PI3K-Akt-mTOR signaling, Ras-Raf-MEK-ERK signaling[2].
GNF-5837 (5-500 nM; 72 hours; GOT1 cells) treatment induces G1 cell cycle arrest[2].
GNF-5837 (500 nM; 144 hours; GOT1 cells) treatment increases apoptotic cell death[2].

Cell Viability Assay[2]

Cell Line: GOT1 cells
Concentration: 0.1 nM , 0.5 nM , 1 nM , 5 nM , 10 nM , 50 nM , 100 nM and 500 nM
Incubation Time: 72 hours, 96 hours and 144 hours
Result: Cell viability assay determined a clear decrease of GOT1 cell viability in a time- and dose- dependent manner.

Western Blot Analysis[2]

Cell Line: GOT1 cells
Concentration: 5 nM, 50 nM and 500 nM
Incubation Time: 24 hours
Result: Significant levels of TrkA expression, faint TrkC expression and no TrkB expression.

Cell Cycle Analysis[2]

Cell Line: GOT1 cells
Concentration: 5 nM, 500 nM
Incubation Time: 72 hours
Result: Induced G1 cell cycle arrest.

Apoptosis Analysis[2]

Cell Line: GOT1 cells
Concentration: 500 nM
Incubation Time: 144 hours
Result: Induced apoptosis.
In Vivo

GNF-5837 (25-100 mg/kg; oral administration; once daily; for 10 days; mice) treatment inhibits tumor growth in a mouse xenograft model derived from RIE cells expressing both TRKA and NGF[1].

Animal Model: Mouse xenograft model[1]
Dosage: 25 mg/kg, 50 mg/kg, 100 mg/kg
Administration: Oral administration; once daily; for 10 days
Result: 72 and 100% tumor regression was observed at 50 and 100 mg/kg, respectively. At 25 mg/kg, only partial tumor growth inhibition was achieved.
Molecular Weight

535.49

Formula

C₂₈H₂₁F₄N₅O₂

CAS No.

1033769-28-6

SMILES

O=C(NC1=CC(C(F)(F)F)=CC=C1F)NC2=CC=C(C)C(NC3=CC(NC/4=O)=C(C=C3)C4=C\C5=CC=CN5)=C2

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 : ≥ 32 mg/mL (59.76 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8674 mL 9.3372 mL 18.6745 mL
5 mM 0.3735 mL 1.8674 mL 3.7349 mL
10 mM 0.1867 mL 0.9337 mL 1.8674 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 (4.67 mM); Clear solution

  • 2.

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

    Solubility: 2.5 mg/mL (4.67 mM); Suspended solution; Need ultrasonic

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

Purity: 99.19%

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Keywords:

GNF-5837GNF5837GNF 5837Trk ReceptorTropomyosin related kinase receptorInhibitorinhibitorinhibit

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GNF-5837
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