10mM in DMSO para flujos de trabajo cromatográficos y analíticos sensibles que requieren una interferencia mínima de la línea base.
Store at -80°C Envío Dry ice packs + Cold packs. Consulte el COA específico del lote para conocer las especificaciones exactas.
SDS, COA, ficha técnica y hoja de especificaciones disponibles para descargar. COA específico del lote accesible mediante búsqueda por número de lote.
Citado en 0 publicaciones revisadas por pares sobre cromatografía, síntesis orgánica y reacciones de acoplamiento cruzado.
AMG 511 is a potent and orally available pan inhibitor of class I PI3K s, with K i s of 4 nM, 6 nM, 2 nM and 1 nM for PI3Kα , β, δ and γ, respectively. AMG 511 significantly suppresses PI3K signaling that is indicated by p-Akt (Ser473) decrease. AMG 511 exhibits anti-tumor activity in mouse glioblastoma xenograft model
In Vitro
AMG 511 shows the inhibition of AKT (Ser473) phosphorylation in U87 malignant glioma (MG) cells with an IC 50 of 4 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
AMG 511 potently blocks the targeted PI3K pathway in a mouse liver pharmacodynamic model (3-30 mg/kg; p.o.) and inhibits tumor growth in a U87 MG glioblastoma xenograft model (3-30 mg/kg; p.o.; daily; for 12 days) . AMG 511 shows excellent in vivo efficacy and pharmacokinetic profile . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female CD1 NU/NU mice, with U87 MG glioblastoma xenograft model Dosage: 1 mg/kg, 3 mg/kg, 10 mg/kg Administration: Oral administration, daily, for 12 days Result: Inhibited tumor growth. Animal Model: Male Sprague-Dawley rats Dosage: 1 mg/kg Administration: Oral administration (Pharmacokinetic Analysis) Result: Had a superior pharmacokinetic profile with low clearance (0.4 L/h/kg, 12% of liver blood flow), good oral bioavailability (F = 60%), and a commensurate high oral exposure (AUC = 5.0 μM·h).
IC50& Target:PI3Kα 4 nM (Ki) PI3Kβ 6 nM (Ki) PI3Kδ 2 nM (Ki) PI3Kγ 1 nM (Ki)
Documento completo sobre peligros, manipulación, almacenamiento y cumplimiento normativo.
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