GNF-5837

Product description: 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.).

Alternate Names/Synonyms: GNF5837

Product Type: Chemical

Molecular Formula: C28H21F4N5O2

Molecular Weight: 535.5

CAS: 1033769-28-6

Purity: >95%

InChiKey: YYDUWLSETXNJJT-MTJSOVHGSA-N

Appearance Solid.

Solubility: Soluble in DMSO.

Short Term Storage: +4°C

Long Term Storage: -20°C

Shipping: AMBIENT

Use & Stability: Stable for at least 2 years after receipt when stored at -20°C.

Lien vers la Fiche Technique