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| 25mg |
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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. With IC50 values of 0.77, 2.85, and 0.47 μg/ml in HepG2, Huh7, and Hep3B cells, respectively, SC66 demonstrates a dual inhibitory function toward AKT activity. In hepatocellular carcinoma (HCC) cells, SC66 inhibits colony formation, decreases cell viability in a dose- and time-dependent manner, and triggers apoptosis. SC66 treatment led to a reduction in total and phospho-AKT levels. Reactive oxygen species (ROS) and DNA damage were both induced by SC66. Both the effects of doxorubicin, a traditional chemotherapeutic, and those of everolimus, a targeted agent, were markedly enhanced by SC66. Hep3B cell tumor growth was inhibited by SC66 in vivo in xenograft models; an analogous mechanism was seen in the in vitro model. HCC cells responded favorably to SC66's antitumor properties.
| Targets |
Akt
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|---|---|
| ln Vitro |
SC66 inhibits colony formation, causes apoptosis in HCC cells, and decreases cell viability in a dose- and time-dependent manner. Total and phospho-AKT levels are decreased after SC66 treatment. This is accompanied by modifications in the cytoskeleton's structure, a decrease in the expression levels of E-cadherin, β-catenin, and phospho-FAK, as well as an upregulation of Snail protein. DNA damage and reactive oxygen species (ROS) production are additional effects of SC66. The AKT/mTOR signaling in HCC cell lines is impacted by SC66[1].
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| ln Vivo |
In the mouse xenograft tumor model of Hep3B cells, SC66 treatment significantly reduces tumor volume to 37% on day 17 of treatment when compared with tumors in the untreated group. In the tumors of animals given SC66 treatment, there is a correlation between the inhibition of cell growth and a decrease in phospho-AKT levels[1].
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| Cell Assay |
Caspase activity assays: Cells (2 × 104/well) are treated with 2 and 4 μg/ml SC66 and after 1, 3 and 6 hours the levels of caspase3/7 activities in the cells are measured by the Caspase-Glo® 3/7 Assay. Relative luminescence units (RLU) are used to express results. Values are the mean SD of two separate experiments that were carried out in duplicate.
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| Animal Protocol |
Mice: We use 4-week-old male nude athymic mice (Fox1 nu/nu). Inoculations of 1×107 Hep3B cells in 0.2 mL of PBS are injected into the animal's right flank. The mice are randomly divided into three groups of six animals each, with the various tumor volumes evenly distributed among the three groups, at the point at which the tumors become palpable (around 150 mm3). Two groups of mice are given i.p. injections of SC66 (15 and 25 mg/kg) suspended in DMSO, further diluted in a solution of 25% ethanol, twice weekly. The only vehicle is given to the control group. Using calipers, tumor volumes are calculated twice per week. Volumes of the primary tumor are calculated.
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| References |
| Molecular Formula |
C18H16N2O
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|---|---|---|
| Molecular Weight |
276.33
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| Exact Mass |
276.126
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| Elemental Analysis |
C, 78.24; H, 5.84; N, 10.14; O, 5.79
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| CAS # |
871361-88-5
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| Related CAS # |
871361-88-5
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| PubChem CID |
6018993
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
514.5±50.0 °C at 760 mmHg
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| Flash Point |
260.0±36.5 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.683
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| LogP |
3.03
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
21
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| Complexity |
389
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(/C1C=CN=CC=1)=C1/CCC/C(=C\C2C=CN=CC=2)/C/1=O
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| InChi Key |
CYVVJSKZRBZHAV-UNZYHPAISA-N
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| InChi Code |
InChI=1S/C18H16N2O/c21-18-16(12-14-4-8-19-9-5-14)2-1-3-17(18)13-15-6-10-20-11-7-15/h4-13H,1-3H2/b16-12+,17-13+
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| Chemical Name |
(2E,6E)-2,6-bis(pyridin-4-ylmethylidene)cyclohexan-1-one
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.05 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (9.05 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (9.05 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6189 mL | 18.0943 mL | 36.1886 mL | |
| 5 mM | 0.7238 mL | 3.6189 mL | 7.2377 mL | |
| 10 mM | 0.3619 mL | 1.8094 mL | 3.6189 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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. |
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