GNF-5837

SKU: orb1301076

Description

GNF-5837 is a potent, orally active pan-TRK inhibitor targeting TrkA and TrkB with IC50 values of 8 nM and 12 nM, respectively. It is a valuable research tool for investigating TRK kinase signaling in cancer and neurological disease models, both in vitro and in vivo.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1033769-28-6
• MW: 535.49
• Purity: 99.29% (May vary between batches)
• Formula: C₂₈H₂₁F₄N₅O₂
• SMILES: Cc1ccc(NC(=O)Nc2cc(ccc2F)C(F)(F)F)cc1Nc1ccc2\C(=C\c3ccc[nH]3)C(=O)Nc2c1
• Target: Trk receptor,c-Kit,PDGFR
• Solubility: DMSO:40 mg/mL (74.7 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.73 mM);Ethanol:5.4 mg/mL (10.08 mM)

Bioactivity

• Target IC50:
  TrkC:7 nM|TrkB:12 nM|TrkA:8 nM
• In Vivo:
  In both male Balb/c mice and Sprague–Dawley rats, GNF-5837 has the low drug clearance, and moderate biovailability. In mice bearing Rie xenografts expressing TrkA and NGF, GNF-5837 (100 mg/kg/d p.o.) significantly inhibits tumor growth.
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• In Vitro:
  In Ba/F3 cells overexpressing the constitutively active Tel-TRKC fusion, GNF-5837 shows potent anti-Trk activity and potent antiproliferation activity with IC50 of 0.042 μM.
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• Cell Research:
  Compounds are tested for their ability to inhibit the proliferation of wt Ba/F3 cells and Ba/F3 cells transformed with constitutively expressed luciferase reporter and BCR-ABL or Tel-KDR or other Tel fusion kinases. Parental Ba/F3 cells are maintained in media containing recombinant mouse IL3 and the kinase transformed Ba/F3 cells are maintained in media without IL-3. 7.5 nL of compounds are spotted to each well of 1536-well assay plates by Liquid handling System Echo 555 (Labcyte). 700 cells are then plated into each well of the assay plates in 7 μL culture media per well and compounds are tested at 0.17 nM to 10 uM in 3-fold serial dilutions. The cells were then incubated for 48 hours at 37 °C. 3 μL of Bright-Glo® is added to each well and the plates are read using ViewLux. (Only for Reference)
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

cKit, Inhibitor, GNF5837, GNF-5837, GNF 5837, Kit, inhibit, PDGFRβ, Tropomyosin related kinase receptor, Trk receptor, Trk Receptor, TrkA, TrkC, TrkB, Trkreceptor

Compound Identifiers

PubChem CID

59397065