GNF-5837 ≥95%

Supplier: ADIPOGEN CORP MS

Synonyms: 1-(3-((3-((1H-Pyrrol-2-yl)methylene)-2-oxoindolin-6-yl)amino)-4-methylphenyl)-3-(2-fluoro-5-(trifluoromethyl)phenyl)urea

SYN-1183-M001 SYN-1183-M005 SYN-1183-M010 SYN-1183-M050
102992-626EA 119.08 USD
102992-626 102992-628 102992-630 102992-632
GNF-5837 ≥95%
GNF-5837

Inhibitor of pan-Trk activity (IC(50) = 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 (IC(50) = 11, 9 and 7nM, respectively) and in Ba/F3 and RIE cells expressing both TrkA and NGF (IC(50) = 42 and 17nM, respectively) over Mo7e-c-Kit and Rat-A10-PDGFR (IC(50) = 1 and 0.5µM) and Ba/F3-Tel-KDR and wt-Ba/F3 cells (IC(50) = 3.0 and 5.6µM). 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.).

Formula: C₂₈H₂₁F₄N₅O₂
MW: 535.5 g/mol
Storage Temperature: Freezer
MDL Number: MFCD24386809
CAS Number: 1033769-28-6

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Specification Test Results

Purity 95%
Appearance/Color Solid.
Solubility Soluble in DMSO.

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