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

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) .

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GNF-5837 Chemical Structure

GNF-5837 Chemical Structure

CAS No. : 1033769-28-6

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10 mM * 1 mL in DMSO
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Based on 3 publication(s) in Google Scholar

GNF-5837 Related Antibodies

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TrkA TrkB TrkC Trk

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  • Purity & Documentation

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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].

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

GNF-5837 Related Antibodies

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].

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

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.
Appearance

Solid

Color

Orange to red

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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 32 mg/mL (59.76 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.65%

SDS (393 KB)

COA (247 KB) RP-HPLC (244 KB) MS (68 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8674 mL 9.3372 mL 18.6745 mL 46.6862 mL
5 mM 0.3735 mL 1.8674 mL 3.7349 mL 9.3372 mL
10 mM 0.1867 mL 0.9337 mL 1.8674 mL 4.6686 mL
15 mM 0.1245 mL 0.6225 mL 1.2450 mL 3.1124 mL
20 mM 0.0934 mL 0.4669 mL 0.9337 mL 2.3343 mL
25 mM 0.0747 mL 0.3735 mL 0.7470 mL 1.8674 mL
30 mM 0.0622 mL 0.3112 mL 0.6225 mL 1.5562 mL
40 mM 0.0467 mL 0.2334 mL 0.4669 mL 1.1672 mL
50 mM 0.0373 mL 0.1867 mL 0.3735 mL 0.9337 mL
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GNF-5837 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GNF-58371033769-28-6GNF5837GNF 5837Trk ReceptorTropomyosin related kinase receptorInhibitorinhibitorinhibit

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