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 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
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Afuresertib (GSK2110183)
CAS number：1047644-62-1 molecular formula：C18H17Cl2FN4OS
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| Chinese alias | 阿福瑞塞替尼 (GSK2110183) | ||
| English alias | 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-amino-1-[(3-fl | ||
| CAS number | 1047644-62-1 | molecular formula | C18H17Cl2FN4OS |
| molecular weight | 427.32 g/mol | Exact mass | - |
| PSA | 101.000 Ų | logp | 3.884 |
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