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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) [1].

Product Specifications

CAS Number

[1033769-28-6]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Trk Receptor

Type

Reference compound

Related Pathways

Neuronal Signaling; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/GNF-5837.html

Concentration

10mM

Purity

99.44

Solubility

DMSO : ≥ 32 mg/mL

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

Molecular Formula

C28H21F4N5O2

Molecular Weight

535.49

Precautions

H302, H315, H319, H335

References & Citations

[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|[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.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

TrkA; TrkB; TrkC

Available Sizes

Curated Selection

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