GSK2110183 hydrochloride

• CAT Number: I005868
• Molecular Formula: C18H17Cl3F2N4OS
• Molecular Weight: 481.77
• Purity: ≥95%
• Target: Akt
• Solubility: DMSO: ≥ 36 mg/mL
• Storage: Store at -20°C
• IC50: 0.08/2/2.6 nM(Akt1/Akt2/Akt3)

GSK2110183 Hcl 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. 


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.
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Reference

[1]. Dumble M, et al. Discovery of novel AKT inhibitors with enhanced anti-tumor effects in combination with the MEK inhibitor. PLoS One. 2014 Jun 30;9(6):e100880.