648451

Trk Inhibitor III, GNF-5837

The Trk Inhibitor III, GNF-5837 controls the biological activity of Trk. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Sinônimo(s): 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
• Fórmula empírica (Notação de Hill): C₂₈H₂₁F₄N₅O₂
• Número CAS: 1033769-28-6
• Peso molecular: 535.49
• Número MDL: MFCD24386809
• Código UNSPSC: 12352200
• NACRES: NA.77

Propriedades

• Nível de qualidade: 100
• Ensaio: ≥98% (HPLC)
• Formulário: powder
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: orange
• solubilidade: DMSO: 50 mg/mL
• Condições de expedição: ambient
• temperatura de armazenamento: 2-8°C
• cadeia de caracteres SMILES: O=C(NC1=C(C=CC(C(F)(F)F)=C1)F)NC2=CC(NC3=CC(NC/4=O)=C(C=C3)C4=C\C5=CC=CN5)=C(C)C=C2
• InChI: 1S/C28H21F4N5O2/c1-15-4-6-19(35-27(39)37-25-11-16(28(30,31)32)5-9-22(25)29)13-23(15)34-18-7-8-20-21(12-17-3-2-10-33-17)26(38)36-24(20)14-18/h2-14,33-34H,1H3,(H,36,38)(H2,35,37,39)/b21-12-
• chave InChI: YYDUWLSETXNJJT-MTJSOVHGSA-N

Descrição

Descrição geral

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 12 nM 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 7 nM, respectively) and in Ba/F3 and RIE cells expressing both TrkA and NGF (IC₅₀ = 42 and 17 nM, respectively) over Mo7e-c-Kit and Rat-A10-PDGFR (IC₅₀ = 1 and 0.5 µM) and Ba/F3-Tel-KDR and wt-Ba/F3 cells (IC₅₀ = 3.0 and 5.6 µM). 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 (50 mg/kg, p.o.).

Embalagem

Packaged under inert gas

Advertência

Toxicity: Standard Handling (A)

Reconstituição

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Outras notas

Albaugh, P., et al. 2012. ACS Med. Chem. Lett.3, In press.

Informações legais

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable