2016年7月14日星期四

GSK2110183|GSK-2110183|pan AKT inhibitor

GSK2110183|GSK-2110183|pan AKT inhibitor

GSK2110183 is an orally bioavailable, selective, ATP-competitive and potent pan-Akt inhibitor with IC50s of 0.08/2/2.6 nM for Akt1/Akt2/Akt3 respectively.

Product name: GSK2110183|Purity>98%| CAS: 1047634-63-8|Molecule Formular: C18H16Cl2F2N4OS|MW: 445.31|Other Namess: GSK-2110183,GSK 2110183

GSK2110183 showed concentration-dependent effect on multiple AKT substrate phosphorylation levels, including GSK3β, PRAS40, FOXO and Caspase 9 in BT474 (breast; ERBB2+, PIK3CA K111N) and LNCaP (prostate; PTEN null). Mice bearing BT474 breast tumor xenografts were dosed orally with either vehicle or GSK2110183 at 10, 30 or 100 mg/kg daily for 21 days which resulted in 8, 37 and 61% TGI, respectively. Similarly, mice treated with GSK2110183 at 10, 30 and 100 mg/kg resulted in 23, 37 and 97% TGI, respectively, of SKOV3 xenografts.

For research only, not for human use.

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