445835-M

Mer RTK Inhibitor, UNC569

Mer RTK Inhibitor, UNC569, 1350547-65-7 is a potent, reversible and ATP-competitive inhibitor of Mer receptor tyrosine kinase (IC50 = 2.9 nM; Ki = 4.3 nM).

• Sinónimos: Mer RTK Inhibitor, UNC569, MERTK Inhibitor I, RP38 Inhibitor I, TAM Family RTK Inhibitor I, UNC-569, 1-(( trans-4-Aminocyclohexyl)methyl)-N-butyl-3-(4-fluorophenyl)-1H-pyrazolo[3,4-d]pyrimidin-6-amine, MERTK Inhibitor I, RP38 Inhibitor I, TAM Family RTK Inhibitor I, UNC-569, 1-((trans-4-Aminocyclohexyl)methyl)-N-butyl-3-(4-fluorophenyl)-1H-pyrazolo[3,4-d]pyrimidin-6-amine
• Fórmula empírica (notación de Hill): C₂₂H₂₉FN₆
• Peso molecular: 396.50
• Código UNSPSC: 12352200

Propiedades

• Nivel de calidad: 100
• Análisis: ≥95% (HPLC)
• formulario: powder
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze; protect from light
• color: beige
• solubilidad: DMSO: 100 mg/mL; water: 2.5 mg/mL (with gentle warming)
• temp. de almacenamiento: 2-8°C

Descripción

Descripción general

An orally bioavailable pyrazolopyrimidine compound that acts as a potent, reversible and ATP-competitive inhibitor of Mer receptor tyrosine kinase (IC₅₀ = 2.9 nM; K_i = 4.3 nM) with ~10-fold greater selectivity over other TAM family kinases (IC₅₀ = 37 and 48 nM for Axl and Tyro3, respectively). Also shown to affect the activities of Flt3, MAPKAPK2, RET and Ret-Y791F at 30 nM by 82%, 92%, 59% and 56% in a 72 kinase panel, and block Mer auto-phosphorylation in human Pre-B leukemia 697 cells with an IC₅₀ of 141 nM. Exhibits desirable pharmacokinetic profile and efficacy in mice.

Advertencia

Toxicity: Standard Handling (A)

Forma física

Supplied as a trifluoroacetate salt.

Reconstitución

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

Otras notas

Liu, J., et al. 2012. ACS Med. Chem. Lett.3, 129.

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
• Punto de inflamabilidad (°F): Not applicable
• Punto de inflamabilidad (°C): Not applicable