[CAS NO. 1033769-28-6]  GNF-5837

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PRODUCTS SPECIFICATIONS [1033769-28-6]

Distributor
Catalog
SLK-S7519
Brand
Selleck
CAS
1033769-28-6

DESCRIPTION [1033769-28-6]

Overview

MDLMFCD24386809
Molecular Weight535.49
Molecular FormulaC28H21F4N5O2
SMILESO=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

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Description

GNF-5837 is a selective, and orally bioavailable pan- inhibitor for TrkA, and TrkB with of 8 nM, and 12 nM, respectively.

Targets

TrkC [1]
(cellular Ba/F3 assays)
TrkA [1]
(Cell-free assay)
TrkB [1]
(Cell-free assay)
7 nM8 nM12 nM

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.

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.