AMG 511 - 10mM in DMSO , CAS No.1253573-53-3

CAS: 1253573-53-3 Cat. No.: A656499 Fórmula: C₂₂H₂₈FN₉O₃S Peso molecular: 503.55 PubChem CID: 56947516

GRAU & PUREZA 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Visão geral

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)

Especificações

Especificações e pureza

10mM in DMSO

Mecanismos bioquímicos e fisiológicos

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 e

Condições de armazenamento de armazenamento

Store at -80°C

Enviado em

Dry ice packs + Cold packs

Este produto requer transporte de cadeia fria. Serviços terrestres e outros serviços econômicos não estão disponíveis.

Tipo de ação

INHIBITOR

Nomes e identificadores

SMILES isoméricas

CC1=NC(=NC(=N1)N)C2=C(N=CC(=C2)[C@@H](C)N3CCN(CC3)S(=O)(=O)C)NC4=CC(=C(N=C4)OC)F

PubChem CID

56947516

Peso molecular

503.55

Alvos associados (humanos)

PIK3CG Tclin Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform (1 Activities)

Discover Target: PIK3CG

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PIK3CA Tclin Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (1 Activities)

Discover Target: PIK3CA

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)