371806

GTP-14564

A cell-permeable, reversible, and ATP-competitive tricyclic benzofurano-indazolo compound that acts as a potent and specific inhibitor of class III receptor tyrosine kinases.

• Sinónimos: GTP-14564, 1-Phenyl-3-H-8-oxa-2,3-diaza-cyclopenta[a]inden, 3-Phenyl-1H-benzofuro[3,2-c]pyrazole
• Fórmula empírica (notación de Hill): C₁₅H₁₀N₂O
• Número de CAS: 34823-86-4
• Peso molecular: 234.25
• Código UNSPSC: 12352200

Propiedades

• Nivel de calidad: 100
• Análisis: ≥98% (HPLC)
• formulario: solid
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze; protect from light
• color: pale yellow
• solubilidad: DMSO: 5 mg/mL
• Condiciones de envío: ambient
• temp. de almacenamiento: 2-8°C
• InChI: 1S/C15H10N2O/c1-2-6-10(7-3-1)13-15-14(17-16-13)11-8-4-5-9-12(11)18-15/h1-9H,(H,16,17)
• Clave InChI: DZQLVVLATXPWBK-UHFFFAOYSA-N

Descripción

Descripción general

A cell-permeable, reversible, ATP-competitive, and tricyclic, benzofurano-indazolo compound that acts as a potent and specific inhibitor of class III receptor tyrosine kinases (IC₅₀ = 300 nM for c-fms, c-kit, wt-FLT3, and internal tandem duplication (ITD)-FLT3; 1 µM for PDGFRβ). Does not affect the activities of KDR, EGFR, HER2, Abl, Src, PKA, Akt, PKC, MEK, or ERK1/2 (IC₅₀ >10 µM). Inhibits FLT-3 ligand-dependent growth of Ba/F3 cells expressing wild type FLT-3. Reported to be useful in differentiating signal transduction pathways activated by wt-FLT3 and ITD-FLT3 in Ba/F3 cells.

A cell-permeable, reversible, and ATP-competitive tricyclic benzofurano-indazolo compound that acts as a potent and specific inhibitor of class III receptor tyrosine kinases (IC₅₀ = 0.3 µM for c-fms, c-kit, wt-FLT3 and ITD-FLT3; 1.0 µM for PDGFRβ). Does not affect the activities of KDR, EGFR, HER2, Abl, Src, PKA, AKT, PKC, MEK, or ERK1/2 (IC₅₀ ≥ 10 µM). Has been used successfully to differentiate between the signalling pathways activated by wt-FLT3 and ITD-FLT3 in Ba/F3 cells.

Acciones bioquímicas o fisiológicas

Cell permeable: yes

Primary Target
Class III receptor tyrosine kinases

Product competes with ATP.

Reversible: yes

Target IC₅₀: 0.3 µM for c-fms, c-kit, wt-FLT3 and ITD-FLT3; 1.0 µM for PDGFRβ

Envase

Packaged under inert gas

Advertencia

Toxicity: Carcinogenic / Teratogenic (D)

Otras notas

Murata, K., et al. 2003. J. Biol. Chem.278, 32892.

Información legal

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

Información de seguridad

• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 1