SC66 - Akt 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESC66Cat. No.: HY-19832CAS No.: 871361-88-5分式: CHNO分量: 276.33作靶點(diǎn): Akt; Apoptosis作通路: PI3K/Akt/mTOR; Apoptosis儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 34 mg/mL (123.04 mM)* means solub

2、le, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 3.6189 mL 18.0943 mL 36.1886 mL5 mM 0.7238 mL 3.6189 mL 7.2377 mL10 mM 0.3619 mL 1.8094 mL 3.6189 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 SC66種 Akt 抑制劑，降低細(xì)胞活，這種作存在劑量和時(shí)間依賴性，且抑制肝癌 (HCC) 細(xì)胞的集落形成和誘

3、導(dǎo)凋亡。IC50 & Target Akt體外研究SC66 inhibits cell viability and colony forming capacity of HCC cells with IC50s of 0.77，0.47，0.92，0.751/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEand 2.85 g/mL at 72 hours for HepG2, Hep3B, PLC/PRF/5，HA22T/VGH and Huh7 cells. HepG2,HA22T/VGH and PLC/PRF/5 cells have si

4、milar IC50s of approximately 0.85 and 0.75 g/mL at 48 and 72hours, respectively. To determine whether the decrease in cell viability is related to apoptosis induction,TUNEL assays are performed in Hep3B and Huh7 cells treated with 1, 2 and 4 g/mL of SC66 for 24 hours.In Hep3B cells the number of TUN

5、EL-positive cells increased with increasing concentrations of SC66,whereas in Huh7 cells very few light brown-colored cells are observed only after treatment with 4 g/mLSC66 1.體內(nèi)研究 To demonstrate the effectiveness in vivo of SC66 on HCC, a mouse xenograft tumor model of Hep3B cells isused. When tumo

6、rs became palpable, at a size of about 150 mm3, mice are randomized into three groups of6 animals each. The treated group receive SC66 at 15 and 25 mg/kg twice a week via i.p. injection, while theuntreated group receive the vehicle alone. Treatment with 25 mg/Kg SC66 significantly reduces tumorvolum

7、e to 37% on day 17 when compared with tumors of the untreated group 1.PROTOCOLCell Assay 1 Cells (5 103/well) are distributed into each well of 96-well microtiter plates and then incubated overnight. Attime 0, the medium is replaced with fresh complete medium and different doses of SC66 are added. C

8、ells arecultured for 24, 48 and 72 hours. At the end of treatment, MTS assays are performed using the CellTiterAqueous OneSolution kit. Cell viability is expressed as a percentage of the absorbance measured in thecontrol cells. Values are expressed as meansSD of three separate experiments, each perf

9、ormed in triplicate1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice 1Administration 1 Male nude athymic mice (Fox1 nu/nu) aged 4 weeks are used. Suspensions of 1107 Hep3B cells in 0.2 mLof PBS are inoculated into the right flank of the anim

10、al. When tumors became palpable (around 150 mm3),the mice are randomly divided into three groups of 6 animals each, with the various tumor volumes equallydistributed among the three groups. Two groups of mice are treated twice a week with 15 and 25 mg/kgSC66 suspended in DMSO, further diluted in a s

11、olution of 25% ethanol and administered via i.p. injection.The control group receive the vehicle alone. Tumor volumes are determined twice a week using calipers.Primary tumor volumes are calculated.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Cusimano A, et al. Cytotoxic activity of the novel small molecule AKT inhibitor SC66 in hepatocellular carcinoma cells. Oncotarget. 2015Jan 30;6(3):1707-22.McePdfHeightCaution: Product