ALM301 - 10mM in DMSO , CAS No.1313439-71-2

CAS: 1313439-71-2 Cat. No.: A655455 Fórmula: C₂₅H₂₅N₃O₃ Peso molecular: 415.48 PubChem CID: 68299673

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

ALM301 is an orally active highly specific AKT inhibitor with IC 50 values of 0.13 µM, 0.09 µM and 2.75 µM for AKT1 , AKT2 and AKT3 , respectively. ALM301 inhibits AKT phosphorylation and modulates downstream signalling in vitro . ALM301 can inhibit cancer cell proliferation and tumor growth

In Vitro

ALM301 (0.001-10 µM; 72 h) inhibits the proliferation of cancer cells, and PI3KCA-mutant MCF-7 cells is the most sensitive; increases sub-G0 population in a dose-dependent manner. ALM301 (1 µM; 1 h) inhibits AKT phosphorylation in MCF-7 and sustains up to 48 h, with an EC 50 value of 0.47 µM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: MCF-7, T47D, NCI-H460, HCT116 and other cancer cells Concentration: 0.001-10 µM Incubation Time: 72 h Result: Inhibited the proliferation of cancer cells, and PI3KCA-mutant MCF-7 cells was the most sensitive with an IC 50 of 2.25 µM. Western Blot AnalysisCell Line: MCF-7 Concentration: 0.001-10 µM Incubation Time: 1, 4, 24 and 48 h Result: Inhibited pAKT and pGSK3β at various concentrations and timepoints up to 48 h.

In Vivo

ALM301 (10, 30 and 100 mg/kg; p.o.; single dosage) inhibits pAKT S473 in tumors and suppresses tumor growth . ALM301 (3 or 10 mg/kg; p.o.; q.d. for 49 days) shows better tumor inhibition ability when combined with Tamoxifen . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: BALB/c mice (bearing A549 xenografts) Dosage: 10, 30 and 100 mg/kg Administration: p.o.; single dosage Result: Increased total plasma concentrations dose-dependently that resulted in almost total abrogation of measurable pAKT S473 in tumors at all timepoints over 24 h. Exhibited the tumour growth inhibition (TGI) of 23, 31 and 41% at 10, 30 and 100 mg/kg, respectively. Animal Model: BALB/c mice (bearing PIK3CA-mutant MCF-7 xenografts) Dosage: 3 or 10 mg/kg Administration: p.o.; q.d. for 49 days Result: Showed significant tumour regressions of 57% and 50% at 3 and 10 mg/kg, respectively, when combined with Tamoxifen (5 mg/kg; q.d.).

IC50& Target:AKT1 0.13 μM (IC 50 ) Akt2 0.09 μM (IC 50 ) Akt3 2.75 μM (IC 50 )

Specifications

Especificaciones y pureza

10mM in DMSO

Mecanismos bioquímicos y fisiológicos

ALM301 is an orally active highly specific AKT inhibitor with IC 50 values of 0.13 µM, 0.09 µM and 2.75 µM for AKT1 , AKT2 and AKT3 , respectively. ALM301 inhibits AKT phosphorylation and modulates downstream signalling in vitro . ALM301 can inhibit cance

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Tipo de acción

INHIBITOR

Nombres e identificadores

• Isómeros SMILES: CCN1C(=O)COC2=C1C=C(C(=N2)C3=CC=C(C=C3)C4(CC(C4)O)N)C5=CC=CC=C5
• PubChem CID: 68299673
• Peso molecular: 415.48

Preguntas frecuentes

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 1313439-71-2, the molecular formula is C25H25N3O3, and the molecular weight is 415.48 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.