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Description: SC66 is a novel, potent and allosteric inhibitor of AKT with potential anticancer activity, it reduces cell viability in a dose- and time-dependent manner, inhibits colony formation and induces apoptosis in hepatocellular carcinoma (HCC) cells. SC66 exhibits a dual-inhibitory function toward AKT activity with IC50 values of 0.77, 2.85 and 0.47 μg/ml in HepG2, Huh7 and Hep3B cells, respectively. SC66 reduces cell viability in a dose- and time-dependent manner, it also inhibits colony formation and induces apoptosis in hepatocellular carcinoma (HCC) cells. SC66 treatment led to a reduction in total and phospho-AKT levels. SC66 induced the production of reactive oxygen species (ROS) and DNA damage. SC66 significantly potentiated the effects of both conventional chemotherapeutic and targeted agents, doxorubicin and everolimus, respectively. In vivo, SC66 inhibited tumor growth of Hep3B cells in xenograft models, with a similar mechanism observed in the in vitro model. SC66 had antitumor effects on HCC cells.
References: Oncotarget. 2015 Jan 30;6(3):1707-22.
Product Catalog 2023
Guide to Product Handling
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
In Vitro
In vitro activity: SC66 is a novel, potent and allosteric inhibitor of AKT, it displays a dual-inhibitory function toward AKT activity with IC50 values of 0.77, 2.85 and 0.47 μg/ml in HepG2, Huh7 and Hep3B cells, respectively. SC66 reduces cell viability in a dose- and time-dependent manner, it also inhibits colony formation and induces apoptosis in hepatocellular carcinoma (HCC) cells. SC66 treatment led to a reduction in total and phospho-AKT levels. SC66 induced the production of reactive oxygen species (ROS) and DNA damage. SC66 significantly potentiated the effects of both conventional chemotherapeutic and targeted agents, doxorubicin and everolimus, respectively. In vivo, SC66 inhibited tumor growth of Hep3B cells in xenograft models, with a similar mechanism observed in the in vitro model. SC66 had antitumor effects on HCC cells.
Cell Assay: Cells are seeded into each well (5 ×103/well) of 96-well microtiter plates and then incubated overnight. At time 0, the medium is replaced with fresh complete medium and different doses of SC66 are added. Cells are cultured for 24, 48 and 72 hours. At the end of treatment, MTS assays are performed using the CellTiter Aqueous OneSolution kit. Cell viability is expressed as a percentage of the absorbance measured in the control cells. Values are expressed as means±SD of three separate experiments, each performed in triplicate
In Vivo
Male nude athymic mice (Fox1 nu/nu) aged 4 weeks were obtained from Harlan and allowed to acclimatize for 1 week. Suspensions of 10 × 106 Hep3B cells in 0.2 ml of PBS were inoculated into the right flank of the animal. When tumors became palpable (around 150 mm3), the mice were randomly divided into three groups of 6 animals each, with the various tumor volumes equally distributed among the three groups. Two groups of mice were treated twice a week with 15 and 25 mg/Kg SC66 suspended in DMSO, further diluted in a solution of 25% ethanol and administered via i.p. injection. The control group received the vehicle alone. Tumor volumes were determined twice a week using calipers. Primary tumor volumes were calculated with the formula: v = length × (width)2/2. Mice were euthanized by cervical dislocation when the tumor burden exceeded 10% of animal body weight, or when tumor ulcerated or other conditions of morbidity were ascertained, in conformity with institutional guidelines which are in compliance with national (D.L., 116 G.U., Suppl.40; 18 February 1992) and international laws and policies (ECC Council Directive 86/609, OJ L358.1, 12 December 1987). This study was authorized by the Italian Ministry of Health (D.M. n. 39/2014-B).
Animal model
Male nude athymic mice
Formulation & Dosage
References
Oncotarget. 2015 Jan 30;6(3):1707-22.
Purity ≥98%
SC66 is cytotoxic to HCC cell lines. Oncotarget. 2015 Jan 30;6(3):1707-22.
SC66 induces apoptosis in HCC cell lines. Oncotarget. 2015 Jan 30;6(3):1707-22.
Effects of SC66 on the phosphorylation status of critical components of the cellular signaling pathway. Oncotarget. 2015 Jan 30;6(3):1707-22.
SC66 induces anoikis. Oncotarget. 2015 Jan 30;6(3):1707-22.
SC66 induces ROS production. Oncotarget. 2015 Jan 30;6(3):1707-22.
The antioxidant NAC reverts SC66-induced anoikis, cell growth and AKT signaling inhibition. Oncotarget. 2015 Jan 30;6(3):1707-22.
SC66 significantly reduced cell viability in combination with doxorubicin and everolimus in Hep3B cells. Oncotarget. 2015 Jan 30;6(3):1707-22.
The effect of SC66 on xenograft models of Hep3B cells. Oncotarget. 2015 Jan 30;6(3):1707-22.