Afuresertib (GSK2110183) - 99%, high purity , Serine/threonine-protein kinase AKT inhibitor, CAS No.1047644-62-1, Serine/threonine-protein kinase AKT inhibitor

Item Number

A413769

• Synonyms: CS-3384 | N-[(2S)-1-amino-3-(3-fluorophenyl)propan-2-yl]-5-chloro-4-(4-chloro-2-methylpyrazol-3-yl)thiophene-2-carboxamide | NSC829868 | NSC-829868 | GTPL7890 | Q27281976 | AC-35761 | ASB183 | ASB-183 | Afuresertib | 2-Thiophenecarboxamide, N-[(1S)-2-amin
• Specifications & Purity: Moligand™, ≥99%
• Biochemical and Physiological Mechanisms: Afuresertib (GSK2110183) is a potent, orally bioavailable Akt inhibitor with K_i of 0.08 nM, 2 nM, and 2.6 nM for Akt1, Akt2, and Akt3, respectively. Phase 2.
• Storage Temp: Protected from light,Store at -20°C,Argon charged
• Shipped In: Ice chest + Ice pads
• Grade: Moligand™
• Action Type: INHIBITOR
• Mechanism of action: Serine/threonine-protein kinase AKT inhibitor

Product Description

Information

Afuresertib (GSK2110183) is a potent, orally bioavailableAktinhibitor withKiof 0.08 nM, 2 nM, and 2.6 nM for Akt1, Akt2, and Akt3, respectively. Phase 2.

Targets

Akt1 (Cell-free assay); Akt2 (Cell-free assay); Akt3 (Cell-free assay) 0.08 nM(Ki); 2 nM(Ki); 2.6 nM(Ki)

In vitro

Afuresertib inhibits the kinase activity of the E17K AKT1 mutant protein with EC50 of 0.2 nM. Afuresertib shows a concentration-dependent effect on multiple AKT substrate phosphorylation levels, including GSK3b, PRAS40, FOXO and Caspase 9. Overall 65% of the hematological cell lines are sensitive to afuresertib (EC50 < 1 μM). Among tested solid tumor cell lines, 21% have EC50 < 1 μM in response to afuresertib.

In vivo

Mice bearing BT474 breast tumor xenografts are dosed with afuresertib (p.o.) at 10, 30 or 100 mg/kg daily which results in 8, 37 and 61% TGI, respectively. Mice bearing SKOV3 ovarian tumor xenografts are treated with 10, 30 and 100 mg/kg afuresertib which results in 23, 37 and 97% TGI, respectively.

Cell Research(from reference)

Cell lines：Hematological cell lines and solid tumor cell lines 

Concentrations：30 μM 

Incubation Time：72 h