S516
Based on 1 Customer Validation
S516 (Compound 22) is an active metabolite of CKD-516 and a potent tubulin polymerization inhibitor with an IC50 of 4.29 μM. S516 has marked antitumor activity.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 98.03%
- No. CAS: 1016543-77-3
- Fòrmula: C21H19N5O4S
- Peso molecular:437.47
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
IC50 & Target
IC50: 4.29 μM (tubulin polymerization)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
42.8 nM
Compound: 22
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Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay
Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay
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[PMID: 20690624] |
| HCT-15 | IC50 |
24.9 nM
Compound: 22
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Cytotoxicity against human HCT15 cells after 72 hrs by MTT assay
Cytotoxicity against human HCT15 cells after 72 hrs by MTT assay
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[PMID: 20690624] |
| HCT-15 | IC50 |
4.29 μM
Compound: 22
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Inhibition of tubulin polymerization in multidrug-resistant human HCT15 cells after 1 hr
Inhibition of tubulin polymerization in multidrug-resistant human HCT15 cells after 1 hr
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[PMID: 20690624] |
| HL-60 | IC50 |
0.0048 μM
Compound: 1
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Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay
Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay
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[PMID: 20850313] |
| HL-60 | IC50 |
4.8 nM
Compound: 22
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Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
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[PMID: 20690624] |
| MDA-MB-231 | IC50 |
9.8 nM
Compound: 1
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Antiproliferative activity against P-gp expressing multidrug-resistant human MDA-MB-231 cells after 72 hrs by MTT assay
Antiproliferative activity against P-gp expressing multidrug-resistant human MDA-MB-231 cells after 72 hrs by MTT assay
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[PMID: 20850313] |
In Vitro
S516 has potent cytotoxicity with IC50s of 4.8 nM, 42.8 nM and 24.9 nM for HL-60, HCT116 and HCT15 cells, respectively[1].
S516 (Compound 22; 30 nM; 16 hours; HL60 cells) treatmemt causes significant arrest of cells at the G2/M phase, resulting in apoptosis with concomitant loss of G0/G1 phase[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:HL60 cells
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Concentration:30 nM
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Incubation Time:16 hours
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Result:Caused significant arrest of cells at the G2/M phase, resulting in apoptosis with concomitant loss of G0/G1 phase.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice bearing 3LL lung cancer[1]
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Dosage:5 mg/kg, 10 mg/kg
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Administration:Intraperitoneal injection
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Result:Had promising antitumor activity (inhibition ratio (IR)> 63%).
Chemical Information
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No. CAS 1016543-77-3
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Appearance Solid
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Peso molecular 437.47
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Fòrmula C21H19N5O4S
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Color Light yellow to yellow
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SMILES
O=C(C1=CC=C(C2=CSC(N)=N2)C=C1N3N=CN=C3)C4=CC(OC)=C(OC)C(OC)=C4
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 12.5 mg/mL (28.57 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. 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. 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)
In Vivo:
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: ≥ 1.25 mg/mL (2.86 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
In Vivo Dissolution Calculator
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.
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.
Protocolo
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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. 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 | 2.2859 mL | 11.4294 mL | 22.8587 mL | 57.1468 mL |
| 5 mM | 0.4572 mL | 2.2859 mL | 4.5717 mL | 11.4294 mL | |
| 10 mM | 0.2286 mL | 1.1429 mL | 2.2859 mL | 5.7147 mL | |
| 15 mM | 0.1524 mL | 0.7620 mL | 1.5239 mL | 3.8098 mL | |
| 20 mM | 0.1143 mL | 0.5715 mL | 1.1429 mL | 2.8573 mL | |
| 25 mM | 0.0914 mL | 0.4572 mL | 0.9143 mL | 2.2859 mL |
S516 Related Classifications
HY-130233 Related Classifications
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