Actein
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Actein, a triterpene glycoside, shows an inhibitory effect on cancer cells, which is isolated from the rhizomes of Cimicifuga foetida. Actein suppresses cell proliferation, induces autophagy and apoptosis through promoting ROS/JNK activation, and blunting AKT pathway in bladder cancer. Actein has little toxicity in vivo.
For research use only. We do not sell to patients.
- Purity: 99.58%
- CAS No.: 18642-44-9
- Formula: C37H56O11
- Molecular Weight:676.83
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCC1806 | IC50 |
>20 μM
Compound: 1
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Antiproliferative activity against human HCC1806 cells assessed as inhibition of cell growth incubated for 36 hrs by SRB assay
Antiproliferative activity against human HCC1806 cells assessed as inhibition of cell growth incubated for 36 hrs by SRB assay
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[PMID: 37121522] |
| HeLa | IC50 |
>10 μM
Compound: 11
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Cytotoxicity against human HeLa cells after 48 hrs by MTT assay
Cytotoxicity against human HeLa cells after 48 hrs by MTT assay
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[PMID: 25136911] |
| HL-60 | IC50 |
>10 μM
Compound: 11
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Cytotoxicity against human HL60 cells after 48 hrs by MTT assay
Cytotoxicity against human HL60 cells after 48 hrs by MTT assay
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[PMID: 25136911] |
| MCF7 | IC50 |
>10 μM
Compound: 11
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Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay
Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay
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[PMID: 25136911] |
| MCF7 | IC50 |
14 μM
Compound: 1
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Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 96 hrs by coulter counter analysis
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 96 hrs by coulter counter analysis
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[PMID: 37121522] |
| MDA-MB-231 | IC50 |
>20 μM
Compound: 1
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Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 36 hrs by SRB assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 36 hrs by SRB assay
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[PMID: 37121522] |
| MDA-MB-231 | IC50 |
60 μM
Compound: 1
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Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth
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[PMID: 37121522] |
| MDA-MB-231 | IC50 |
74 μM
Compound: 1
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Antiproliferative activity against human MDA-MB-231 cells overexpressing ERnegative and Her2 assessed as inhibition of cell growth incubated for 96 hrs by coulter counter analysis
Antiproliferative activity against human MDA-MB-231 cells overexpressing ERnegative and Her2 assessed as inhibition of cell growth incubated for 96 hrs by coulter counter analysis
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[PMID: 37121522] |
| NCI-H460 | IC50 |
>10 μM
Compound: 11
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Cytotoxicity against human H460 cells after 48 hrs by MTT assay
Cytotoxicity against human H460 cells after 48 hrs by MTT assay
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[PMID: 25136911] |
| Oocyte | EC50 |
36 μM
Compound: 1
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Allosteric modulation of alpha1beta2gamma2S GABAA receptor expressed in Xenopus laevis oocytes assessed as stimulation of GABA-induced chloride current by electrophysiology
Allosteric modulation of alpha1beta2gamma2S GABAA receptor expressed in Xenopus laevis oocytes assessed as stimulation of GABA-induced chloride current by electrophysiology
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[PMID: 21082802] |
| SMMC-7721 | IC50 |
>10 μM
Compound: 11
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Cytotoxicity against human SMMC-7721 cells after 48 hrs by MTT assay
Cytotoxicity against human SMMC-7721 cells after 48 hrs by MTT assay
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[PMID: 25136911] |
Actein (0-30 µM, 24 h) significantly suppress cell proliferation and induce cell apoptosis of gastric cancer cells via Caspase-3 and p53 signaling pathway combined with tumor necrosis factor-related apoptosis-inducing ligand (TRAIL)[1].
Actein (0-40 μM, 24 h) suppresses cell proliferation, induces G2/M cell cycle arrest, autophagy and apoptosis in bladder cancer cells[2].
Actein (0-20 μM, 24 h) potentiates ROS generation and JNK phosphorylation and suppresses AKT pathway in BIU-87 and T24 cells[2].
Actein (10 nM and 10 μM, 5-10 min) increases calcium release into the cytoplasm of breast cancer cells and colon cancer cells[3].
Actein (0-40 μg/mL, 48 h) inhibits the NF-κB and MEK pathways by decreasing the level of IKKβ protein in 293T (null) and 293T (NF-κB) cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SNU-216 and AGS gastric cancer cell lines
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Concentration:0-30 µM
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Incubation Time:24 h
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Result:Exhibited a strong inhibitory effect on gastric cancer cell proliferation in a dose-dependent manner combined with TRAIL in gastric cancer cells.
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Cell Line:BIU-87 and T24 cells
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Concentration:0-20 μM
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Incubation Time:24 h
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Result:Exhibited dose-increased levels of oxidation-sensitive red fluorescence, indicating the elevation of ROS in BIU-87 and T24 cells.
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Cell Line:SNU-216 and AGS gastric cancer cell lines
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Concentration:0-30 µM
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Incubation Time:24 h
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Result:Dose-dependently reduced the AKT/mTOR and JAK2/STAT3 activity, while p38 and JNK were highly phosphorylated in BIU-87 and T24 cells.
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Cell Line:293T (null) and 293T (NF-κB) cells
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Concentration:0-40 μg/mL
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Incubation Time:48 h
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Result:Decreased the level of IKKβ protein in a dose dependent manner in 293T (null) and 293T (NF-κB) cells.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 18642-44-9
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Appearance Solid
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Molecular Weight 676.83
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Formula C37H56O11
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Color White to off-white
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SMILES
C[C@]12[C@@]3([H])[C@@]4(C[C@@H](OC(C)=O)[C@@]1([C@]5([H])[C@](O[C@]6([C@H]7[C@]([C@@H](O)O6)(C)O7)C[C@H]5C)([H])C2)C)[C@@]8([C@@](C(C)([C@@H](O[C@@]9([H])[C@@H]([C@H]([C@H](O)CO9)O)O)CC8)C)([H])CC3)C4
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 100 mg/mL (147.75 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.69 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (3.69 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Yang ZC, et al. Actein enhances TRAIL effects on suppressing gastric cancer progression by activating p53/Caspase-3 signaling. Biochem Biophys Res Commun. 2018 Mar 18;497(4):1177-1183. [Content Brief]
[2]. Ji L, et al. Actein induces autophagy and apoptosis in human bladder cancer by potentiating ROS/JNK and inhibiting AKT pathways. Oncotarget. 2017 Nov 1;8(68):112498-112515. [Content Brief]
[3]. Einbond LS, et al. Actein induces calcium release in human breast cancer cells. Fitoterapia. 2013 Dec;91:28-38. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.4775 mL | 7.3874 mL | 14.7748 mL | 36.9369 mL |
| 5 mM | 0.2955 mL | 1.4775 mL | 2.9550 mL | 7.3874 mL | |
| 10 mM | 0.1477 mL | 0.7387 mL | 1.4775 mL | 3.6937 mL | |
| 15 mM | 0.0985 mL | 0.4925 mL | 0.9850 mL | 2.4625 mL | |
| 20 mM | 0.0739 mL | 0.3694 mL | 0.7387 mL | 1.8468 mL | |
| 25 mM | 0.0591 mL | 0.2955 mL | 0.5910 mL | 1.4775 mL | |
| 30 mM | 0.0492 mL | 0.2462 mL | 0.4925 mL | 1.2312 mL | |
| 40 mM | 0.0369 mL | 0.1847 mL | 0.3694 mL | 0.9234 mL | |
| 50 mM | 0.0295 mL | 0.1477 mL | 0.2955 mL | 0.7387 mL | |
| 60 mM | 0.0246 mL | 0.1231 mL | 0.2462 mL | 0.6156 mL | |
| 80 mM | 0.0185 mL | 0.0923 mL | 0.1847 mL | 0.4617 mL | |
| 100 mM | 0.0148 mL | 0.0739 mL | 0.1477 mL | 0.3694 mL |
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