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  • The efficacy and selectivity of tumor cell killing by Akt inhibitors are substantially increased by chloroquine.

The efficacy and selectivity of tumor cell killing by Akt inhibitors are substantially increased by chloroquine.

Bioorganic & medicinal chemistry (2008-08-12)
Changkun Hu, V Raja Solomon, Gerardo Ulibarri, Hoyun Lee
要旨

This study was to evaluate the enhancement value of chloroquine (CQ) in cancer cell killing when used in combination with Akt inhibitors. The results showed that the combination of CQ and Akt inhibitors is much more effective than either one alone. Importantly, the CQ-mediated chemosensitization of cell killing effects by Akt inhibitors is cancer specific. In particular, when combined with 10 microM CQ, 1,3-dihydro-1-(1-((4-(6-phenyl-1H-imidazo[4,5-g]quinoxalin-7-yl)phenyl)methyl)-4-piperidinyl)-2H-benzimidazol-2-one (an Akt1 and 2 inhibitor; compound 8) killed cancer cells 10-120 times more effectively than normal cells. Thus, CQ is a very effective and cancer-specific chemosensitizer when used in combination with Akt inhibitors.

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製品内容

Sigma-Aldrich
クロロキン 二リン酸塩, powder or crystals, 98.5-101.0% (EP)