CCT018159
Based on 1 Customer Validation
CCT018159 is an ATP-competitive HSP90β inhibitor, with an IC50 of 3.2 μM against human HSP90β ATPase and 6.6 μM against yeast HSP90β ATPase. CCT018159 induces cell cycle arrest and apoptosis in tumor cells, and inhibits invasion and angiogenesis. CCT018159 is applicable to cancer-related research.
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- Pureza: 99.30%
- No. CAS: 171009-07-7
- Fòrmula: C20H20N2O4
- Peso molecular:352.38
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Almacenamiento:
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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Apoptosis Compound Library
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Actividad biológica
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human Hsp90β 3.2 μM (IC50) |
yeast Hsp90 6.6 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | GI50 |
4.1 μM
Compound: 35, CCT018159
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Antiproliferative against human HCT116 cells
Antiproliferative against human HCT116 cells
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[PMID: 19017562] |
| HCT-116 | GI50 |
4.1 μM
Compound: 3a CCT018159
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Inhibition of HCT116 human colon cancer cell proliferation
Inhibition of HCT116 human colon cancer cell proliferation
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[PMID: 15955698] |
| HCT-116 | GI50 |
5.8 μM
Compound: 5, CCT018159
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Growth inhibition of human HCT116 cells after 24 hrs by SRB assay
Growth inhibition of human HCT116 cells after 24 hrs by SRB assay
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[PMID: 18020435] |
| HCT-116 | GI50 |
5.8 μM
Compound: 1
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Inhibitory concentration against cell proliferation of human HCT116 cells
Inhibitory concentration against cell proliferation of human HCT116 cells
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[PMID: 15974572] |
| HCT-116 | IC50 |
5.8 μM
Compound: 1, CCT018159
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Antiproliferative activity against HCT116 cell line
Antiproliferative activity against HCT116 cell line
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[PMID: 16480864] |
CCT018159 inhibits the growth of human cancer cell lines with a mean GI50 of 5.3 μM, and its activity against HUVECs (GI50 0.87 μM) is stronger than that against most cancer cell lines[1].
CCT018159 (24 h) induces characteristic molecular markers of HSP90 inhibition, including upregulation of HSP72, depletion of client proteins (C-RAF, CDK4, ERBB2, mutant B-RAF), and decreased phosphorylation level of ERK1/2 in human cancer cells, as well as modulates angiogenesis-related client proteins in HUVECs[1].
CCT018159 (41 μM; 16-72 h) induces cell cycle arrest and apoptosis in SKMEL 5 melanoma cells[1].
CCT018159 (0-4.4 μm; 24-48 h) inhibits the key functions of endothelial cells as well as invasion-related functions of tumor cells[1].
CCT018159 (0.1-50 μM) reduces the viability of NCI-H295R cells in a dose-dependent manner, with an EC50 of 11.5 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SKMEL 5
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Concentration:41 μmol/L
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Incubation Time:16, 24, 48, 72 h
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Result:Caused marked accumulation of SKMEL 5 melanoma cells in the G1 phase by 16 h, with cells arrested in the initial G1 or subsequent G1 phase through 72 h.
Chemical Information
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No. CAS 171009-07-7
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Appearance Solid
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Peso molecular 352.38
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Fòrmula C20H20N2O4
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Color White to off-white
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SMILES
CC1=C(C2=CC3=C(OCCO3)C=C2)C(C4=CC(CC)=C(O)C=C4O)=NN1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvente y solubilidad
DMSO : 100 mg/mL (283.78 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 (7.09 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.
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.
Pureza y Documentación
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Ficha de datos (281 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Sharp SY, et al. In vitro biological characterization of a novel, synthetic diaryl pyrazole resorcinol class of heat shock protein 90 inhibitors. Cancer Res. 2007;67(5):2206-2216. [Content Brief]
[2]. Sbiera S, et al. Hsp90 inhibition in adrenocortical carcinoma: Limited drug synergism with mitotane. Mol Cell Endocrinol. 2019;480:36-41. [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 | 2.8378 mL | 14.1892 mL | 28.3785 mL | 70.9461 mL |
| 5 mM | 0.5676 mL | 2.8378 mL | 5.6757 mL | 14.1892 mL | |
| 10 mM | 0.2838 mL | 1.4189 mL | 2.8378 mL | 7.0946 mL | |
| 15 mM | 0.1892 mL | 0.9459 mL | 1.8919 mL | 4.7297 mL | |
| 20 mM | 0.1419 mL | 0.7095 mL | 1.4189 mL | 3.5473 mL | |
| 25 mM | 0.1135 mL | 0.5676 mL | 1.1351 mL | 2.8378 mL | |
| 30 mM | 0.0946 mL | 0.4730 mL | 0.9459 mL | 2.3649 mL | |
| 40 mM | 0.0709 mL | 0.3547 mL | 0.7095 mL | 1.7737 mL | |
| 50 mM | 0.0568 mL | 0.2838 mL | 0.5676 mL | 1.4189 mL | |
| 60 mM | 0.0473 mL | 0.2365 mL | 0.4730 mL | 1.1824 mL | |
| 80 mM | 0.0355 mL | 0.1774 mL | 0.3547 mL | 0.8868 mL | |
| 100 mM | 0.0284 mL | 0.1419 mL | 0.2838 mL | 0.7095 mL |
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