Art. -Nr.: HY-13491

GNF-5837

4 Cited Publications

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Based on 4 publication(s) in Google Scholar

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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Reinheit: 99.44%
CAS. Nr.: 1033769-28-6
Formel: C₂₈H₂₁F₄N₅O₂
Molecular Weight:535.49

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

GNF-5837 Chemical Structure

CAS. Nr.: 1033769-28-6

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

TrkB

9 nM (IC₅₀)

TrkC

7 nM (IC₅₀)

TrkA

11 nM (IC₅₀)

Alle Trk Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A10	IC₅₀	0.5 μM Compound: 22, GNF-5837	Inhibition of PDGFR in rat A10 cells Inhibition of PDGFR in rat A10 cells	[PMID: 24900443]
BaF3	IC₅₀	0.007 μM Compound: 22, GNF-5837	Antiproliferative activity against mouse BA/F3 cells expressing Tel-TRKC Antiproliferative activity against mouse BA/F3 cells expressing Tel-TRKC	[PMID: 24900443]
BaF3	IC₅₀	0.009 μM Compound: 22, GNF-5837	Antiproliferative activity against mouse BA/F3 cells expressing Tel-TRKB Antiproliferative activity against mouse BA/F3 cells expressing Tel-TRKB	[PMID: 24900443]
BaF3	IC₅₀	0.011 μM Compound: 22, GNF-5837	Antiproliferative activity against mouse BA/F3 cells expressing Tel-TRKA Antiproliferative activity against mouse BA/F3 cells expressing Tel-TRKA	[PMID: 24900443]
BaF3	IC₅₀	0.042 μM Compound: 22, GNF-5837	Antiproliferative activity against mouse BA/F3 cells expressing TRKA and NGF Antiproliferative activity against mouse BA/F3 cells expressing TRKA and NGF	[PMID: 24900443]
BaF3	IC₅₀	0.87 μM Compound: 22, GNF-5837	Inhibition of Tel-fused PDGFRbeta in mouse BA/F3 cells Inhibition of Tel-fused PDGFRbeta in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	0.91 μM Compound: 22, GNF-5837	Inhibition of Tel-fused KIT in mouse BA/F3 cells Inhibition of Tel-fused KIT in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	2.9 μM Compound: 22, GNF-5837	Inhibition of Tel-fused JNK2 in mouse BA/F3 cells Inhibition of Tel-fused JNK2 in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	3 μM Compound: 22, GNF-5837	Antiproliferative activity against mouse BA/F3 cells expressing Tel-KDR Antiproliferative activity against mouse BA/F3 cells expressing Tel-KDR	[PMID: 24900443]
BaF3	IC₅₀	3.4 μM Compound: 22, GNF-5837	Inhibition of Tel-fused ALK in mouse BA/F3 cells Inhibition of Tel-fused ALK in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	3.6 μM Compound: 22, GNF-5837	Inhibition of Tel-fused FGR in mouse BA/F3 cells Inhibition of Tel-fused FGR in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	4 μM Compound: 22, GNF-5837	Inhibition of Tel-fused FMS in mouse BA/F3 cells Inhibition of Tel-fused FMS in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	4.4 μM Compound: 22, GNF-5837	Inhibition of Tel-fused FLT1 in mouse BA/F3 cells Inhibition of Tel-fused FLT1 in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	4.7 μM Compound: 22, GNF-5837	Inhibition of Tel-fused RON in mouse BA/F3 cells Inhibition of Tel-fused RON in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	4.7 μM Compound: 22, GNF-5837	Inhibition of Tel-fused ZAP70 in mouse BA/F3 cells Inhibition of Tel-fused ZAP70 in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	5.1 μM Compound: 22, GNF-5837	Inhibition of Tel-fused FLT3 in mouse BA/F3 cells Inhibition of Tel-fused FLT3 in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	5.3 μM Compound: 22, GNF-5837	Inhibition of Tel-fused RET in mouse BA/F3 cells Inhibition of Tel-fused RET in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	5.6 μM Compound: 22, GNF-5837	Antiproliferative activity against wild type mouse BA/F3 cells in presence of IL3 Antiproliferative activity against wild type mouse BA/F3 cells in presence of IL3	[PMID: 24900443]
BaF3	IC₅₀	5.7 μM Compound: 22, GNF-5837	Inhibition of Tel-fused TIE1 in mouse BA/F3 cells Inhibition of Tel-fused TIE1 in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	5.8 μM Compound: 22, GNF-5837	Inhibition of Tel-fused EPHB2 in mouse BA/F3 cells Inhibition of Tel-fused EPHB2 in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	5.8 μM Compound: 22, GNF-5837	Inhibition of Tel-fused MET in mouse BA/F3 cells Inhibition of Tel-fused MET in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	5.9 μM Compound: 22, GNF-5837	Inhibition of Tel-fused EPHA3 in mouse BA/F3 cells Inhibition of Tel-fused EPHA3 in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	6 μM Compound: 22, GNF-5837	Inhibition of Tel-fused ROS in mouse BA/F3 cells Inhibition of Tel-fused ROS in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	6.7 μM Compound: 22, GNF-5837	Inhibition of Tel-fused BMX in mouse BA/F3 cells Inhibition of Tel-fused BMX in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	6.8 μM Compound: 22, GNF-5837	Inhibition of NMP-ALK in mouse BA/F3 cells Inhibition of NMP-ALK in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	7 μM Compound: 22, GNF-5837	Inhibition of Tel-fused FGFR4 in mouse BA/F3 cells Inhibition of Tel-fused FGFR4 in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	7.3 μM Compound: 22, GNF-5837	Inhibition of Tel-fused LYN in mouse BA/F3 cells Inhibition of Tel-fused LYN in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	7.3 μM Compound: 22, GNF-5837	Inhibition of Tel-fused SRC in mouse BA/F3 cells Inhibition of Tel-fused SRC in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	7.6 μM Compound: 22, GNF-5837	Inhibition of Tel-fused IGF1R in mouse BA/F3 cells Inhibition of Tel-fused IGF1R in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	8 μM Compound: 22, GNF-5837	Inhibition of Tel-fused INSR in mouse BA/F3 cells Inhibition of Tel-fused INSR in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	8.2 μM Compound: 22, GNF-5837	Inhibition of Bcr-ABL in mouse BA/F3 cells Inhibition of Bcr-ABL in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	9.3 μM Compound: 22, GNF-5837	Inhibition of Tel-fused FGFR3 in mouse BA/F3 cells Inhibition of Tel-fused FGFR3 in mouse BA/F3 cells	[PMID: 24900443]

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.

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.

Chemical Information

CAS. Nr. 1033769-28-6
Appearance Solid
Molecular Weight 535.49
Formel C₂₈H₂₁F₄N₅O₂
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (4)

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Journal Impact Factor

Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
J Hazard Mater

Mechanistic exploration on neurodevelopmental toxicity induced by upregulation of alkbh5 targeted by triclosan exposure to larval zebrafish. [Abstract]

2023 Sep 5:457:131831. PMID: 37320907
Int J Immunopathol Pharmacol

GNF-5837 alleviates intervertebral disc ageing by upregulating glutathione peroxidase 7. [Abstract]

2025 Jan-Dec:39:3946320251343365. PMID: 40474606
BMC Complement Altern Med

Effects of Chinese medicinal herbs on expression of brain-derived Neurotrophic factor (BDNF) and its interaction with human breast cancer MDA-MB-231 cells and endothelial HUVECs. [Abstract]

2017 Aug 12;17(1):401. PMID: 28800782

Lösungsmittel & Löslichkeit

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Albaugh, P. et al. Discovery of GNF-5837, a Selective TRK Inhibitor with Efficacy in Rodent Cancer Tumor Models. ACS MEDICINAL CHEMISTRY LETTERS, 2012; 3 (2): 140 [Content Brief]

[2]. Aristizabal Prada ET, et al. Tropomyosin receptor kinase: a novel target in screened neuroendocrine tumors. Endocr Relat Cancer. 2018 May;25(5):547-560. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

GNF-5837

4 Cited Publications

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GNF-5837

Orally Active Compound Library

Chemical Probe Library

Targeted Diversity Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Kinase Inhibitor Library

Neuronal Signaling Compound Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Covalent Screening Library

Publications Citing Use of MedChemExpress (MCE) GNF-5837

Alle Trk Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GNF-5837

Orally Active Compound Library

Chemical Probe Library

Targeted Diversity Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Kinase Inhibitor Library

Neuronal Signaling Compound Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Covalent Screening Library

Publications Citing Use of MedChemExpress (MCE) GNF-5837

Alle Trk Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GNF-5837 Related Classifications

HY-13491 Related Classifications