Trk Inhibitor III, GNF-5837 ((Z)-1-(3-((3-((1H-Pyrrol-2-yl)methylene)-2-oxoindolin-6-yl)amino)-4-methylphenyl)-3-(2-fluoro-5-(trifluoromethyl)phenyl)urea), CAS [[1033769-28-6]]

Product Overview

• Article Name: Trk Inhibitor III, GNF-5837 ((Z)-1-(3-((3-((1H-Pyrrol-2-yl)methylene)-2-oxoindolin-6-yl)amino)-4-methylphenyl)-3-(2-fluoro-5-(trifluoromethyl)phenyl)urea), CAS [[1033769-28-6]]
• Biozol Catalog Number: USB-217847
• Supplier Catalog Number: 217847
• Alternative Catalog Number: USB-217847-10
• Manufacturer: US Biological
• Category: Biochemikalien

Product Description

An orally bioavailable oxindole compound that and acts as a potent, reversible and type II DFG-out inhibitor of pan-Trk activity (IC50=8 and 12nM for TrkA and TrkB). Shown to target Trk (tropomyosin receptor kinase) ATP binding cleft and an immediately adjacent hydrophobic pocket. Preferentially arrests the proliferation of Ba/F3 cells fused with Tel-TrkA, Tel-TrkB and Tel-TrkC (IC50=11, 9 and 7nM, respectively) and in Ba/F3 and RIE cells expressing both TrkA and NGF (IC50=42 and 17nM, respectively) over Mo7e-c-Kit and Rat-A10-PDGFR (IC50=1 and 0.5uM) and Ba/F3-Tel-R and wt-Ba/F3 cells (IC50=3.0 and 5.6uM). Displays ~100-fold greater selectivity among a panel of 59 closely related kinases and in 33 cellular kinase assays. Weakly active against relevant cytochrome P450 isozymes and hERG channel, and exhibit adequate microsomal stability, pharmacokinetic profile and efficacy in mice and rats. Suppresses tumor growth in a mouse RIE-TrkAmNGF xenograft model (50mg/kg, p.o.) Synonyms: (Z)-1-(3-((3-((1H-Pyrrol-2-yl)methylene)-2-oxoindolin-6-yl)amino)-4-methylphenyl)-3-(2-fluoro-5-(trifluoromethyl)phenyl)urea. CAS Number: 1033769-28-6 Formula: C28H21F4N5O2 Molecular Weight: 535.5 Solubility: DMSO (50mg/ml) Storage and Stability: Lyophilized powder may be stored at -20C. Stable for 12 months at -20C. Reconstitute with sterile buffer or dH2O. Aliquot to avoid repeated freezing and thawing. Store at -20C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.

Product Properties

• Molecular Weight: 535.5
• Purity: 98% (HPLC)
• Form: Supplied as an orange powder.
• CAS Number: [1033769-28-6]