A-674563 is a potent selective Akt1 (Protein Kinase B) inhibitor. A-674563 also shows inhibitory activity against PKA and CDK2 with IC50 values of 16nM and 46nM respectively. A-674563 has a significant effect on depolarization of purkinje fiber in an in vitro assay, and severe CV toxicity (e.g. hypotension) in vivo. A-674563 induced Akt blockade results in decreased STS cell downstream target phosphorylation and tumor cell growth inhibiton. A-674563 (0-30 µM) reduces the phosphorylation of GSK3α/β, TSC2, mTOR, and ribosomal protein S6 in a dose-dependent fashion in MiaPaCa-2 cells in vitro. Furthermore, A-674563 inhibits hERG ion channels in vitro and causes acute hypotension in vivo. A674563-treated (20 mg/kg/bid, p.o.) mice exhibits slower tumor growth and more than 50% decrease in the tumor volume at the termination of the study compared with that in control group.
|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 70 mg/mL
Water 70 mg/mL
Synthesis and evaluation of indazole based analog sensitive Akt inhibitors.
Okuzumi T, et al. Mol Biosyst. 2010 Aug;6(8):1389-402. PMID: 20582381.
Potent and selective inhibitors of Akt kinases slow the progress of tumors in vivo.
Luo Y, et al. Mol Cancer Ther. 2005 Jun;4(6):977-86. PMID: 15956255.
|Related Akt Products|
GSK2141795 is a potent and selective pan-Akt inhibitor with IC50 values of 180 nM for Akt1, 328 nM for Akt2, and 38 nM for Akt3 respectively (Clinical phase 1).
GDC-0068(RG 7440) 2Hcl is a highly selective pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 5 nM/18 nM/8 nM, 620-fold selectivity over PKA.
Afuresertib (GSK2110183) is a potent, orally bioavailable Akt inhibitor with Ki of 0.08 nM, 2 nM, and 2.6 nM for Akt1, Akt2, and Akt3, respectively. Phase 2.
SC79 is an inhibitor of Akt-PH domain translocation and a specific Akt activator used to enhance Akt activity in various conditions.
|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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