Akt1/Akt2-IN-1 - ≥99% , CAS No.893422-47-4

CAS: 893422-47-4 Cat. No.: A649162 Peso molecular: 539.63

GRADE & PURITY ≥99%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Descripción general

Akt1/Akt2-IN-1 (Compound 17) is an allosteric inhibitor of Akt1 ( IC 50 =3.5 nM) and Akt2 (IC 50 =42 nM), with potent and balanced activity

In Vitro

Consistent with the allosteric mode of inhibition, Akt1/Akt2-IN-1 (Compound 17) is dependent on the PH-domain for Akt inhibition, is selective for Akt1/2 over Akt3 (IC 50 =1900 nM), and is highly selective over other members of the AGC family of kinases (>50 μM vs PKA, PKC, SGK). Akt1/Akt2-IN-1 has moderate activity in an hERG binding assay (IC 50 =5610 nM) and is a substrate for human P-glycoprotein. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Akt1/Akt2-IN-1 (Compound 17) is well tolerated in at exposures that provide high levels of Akt1 and 2 inhibition in vivo. Akt1/Akt2-IN-1 has also been shown to inhibit the growth of A2780 tumors in vivo when used as monotherapy. Akt1/Akt2-IN-1 has potent inhibitory activity against Akt1 and 2 in vivo in a mouse lung and efficacy in a tumor xenograft model. Akt1/Akt2-IN-1 shows good pharmacokinetics in rat with a low clearance of 4.6 mL/min/kg and a half-life of 3.8 h. Due to the improved cell potency, physical properties, and rodent pharmacokinetics of Akt1/Akt2-IN-1, tolerability and Akt inhibition are assessed in mice. Using an acute dosing schedule (IP dosing of 50 mg/kg at times 0, 3, and 8 h), administration of Akt1/Akt2-IN-1 is well tolerated in mice and shows high levels of Akt inhibition in mouse lung . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Form:Solid

IC50& Target:Akt1 3.5 nM (IC 50 ) Akt2 42 nM (IC 50 )

Specifications

Especificaciones y pureza

≥99%

Mecanismos bioquímicos y fisiológicos

Akt1/Akt2-IN-1 (Compound 17) is an allosteric inhibitor of Akt1 ( IC 50 =3.5 nM) and Akt2 (IC 50 =42 nM), with potent and balanced activity.

Condiciones de almacenamiento de almacenamiento

Store at -20°C

Enviado en

Ice chest + Ice pads

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

Tipo de acción

INHIBITOR

Pureza

≥99%

Nombres e identificadores

• Peso molecular: 539.63

Propiedades químicas y físicas

• Solubilidad: DMSO : ≥ 35 mg/mL (64.86 mM)