AZD5363 is a potent Akt inhibitor for Akt1, Akt2 and Akt3 with IC50 of 3 nM, 8 nM and 8 nM, respectively.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 60 mg/mL|
|Source||Cancer Biol Ther (2018). Figure 3. AZD5363|
|Cell Lines||HEK293T cells|
|Incubation Time||24 h|
|Results||Proliferation of homozygous H2189Y mutant cells was significantly inhibited by the mTOR inhibitor everolimus (P =0.018), the PI3K inhibitor LY294002 (P D 0.016), and the AKT inhibitors AZD5363 (P = 0.009) and MK-2206 (P = 0.003). The PI3K inhibitor Wortmannin had no significant effect on proliferation in these five cell lines|
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|AKT inhibitor VIII
Akt Inhibitor VIII is a cell-permeable quinoxaline compound that has been shown to potently, selectively, allosterically, and reversibly inhibit Akt1, Akt2, and Akt3 activity (IC50 = 58 nM, 210 nM, and 2.12 μM; respectively).
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