CLZ-8
Based on 1 Customer Validation
CLZ-8 (Compound 8) is an orally active Mcl-1-PUMA interface inhibitor, with a Ki of 0.3 μM. CLZ-8 exhibits dual activity on reduce PUMA-dependent apoptosis while deactivating Mcl-1-mediated anti-apoptosis in cancer cells.
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- Pureza: 99.14%
- No. CAS: 678158-55-9
- Fòrmula: C22H23N3O2S
- Peso molecular:393.50
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Actividad biológica
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Mcl-1 0.3 μM (Ki) |
PUMA |
CLZ-8 (Compound 8) (0-160 μM, 48 h) significantly inhibits PUMA-dependent apoptosis[1].
CLZ-8 (0-1 μM, 2 h) significantly enhance the irradiated cell viability in a dose-dependent manner, provides significant protection for HUVECs, and inhibits overexpressed PUMA[2].
CLZ-8 (0-1 μM, 24 h) attenuates the radiation-induced apoptosis[2].
CLZ-8 (1 μM, 2 h) protects HUVECs from DNA breaks[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:DLD-1 cells or HUVEC cells
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Concentration:0-160 μM (DLD-1) or 0.01, 0.1 and 1 μM (HUVECs)
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Incubation Time:48 h (DLD-1) or 24 h (HUVECs)
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Result:Significantly inhibited PUMA-dependent apoptosis with an IC50 of 38.93 ± 0.91 μM.
Attenuated the radiation-induced apoptosis.
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Cell Line:HUVEC cells
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Concentration:0.001, 0.01, 0.1 and 1 μM
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Incubation Time:2 h
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Result:Suppressed induction of PUMA after radiation, significantly decreased the level of p53.
Significantly decreased the level of MCL-1 and increased the level of Bcl-XL.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:6-8 week-old male BALB/c mice[2]
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Dosage:100, 200 and 400 mg/kg
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Administration:Intragastric administration, once, 30 min prior to irradiation
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Result:Increased the survival rate of irradiated mice.
Chemical Information
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No. CAS 678158-55-9
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Appearance Solid
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Peso molecular 393.50
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Fòrmula C22H23N3O2S
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Color Light yellow to yellow
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SMILES
O=C1N=C(N2CCN(CCO)CC2)S/C1=C\C3=CC=C(C4=CC=CC=C4)C=C3
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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 2 years -20°C 1 year
Solvente y solubilidad
DMSO : 50 mg/mL (127.06 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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.
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.
Pureza y Documentación
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Ficha de datos (275 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5413 mL | 12.7065 mL | 25.4130 mL | 63.5324 mL |
| 5 mM | 0.5083 mL | 2.5413 mL | 5.0826 mL | 12.7065 mL | |
| 10 mM | 0.2541 mL | 1.2706 mL | 2.5413 mL | 6.3532 mL | |
| 15 mM | 0.1694 mL | 0.8471 mL | 1.6942 mL | 4.2355 mL | |
| 20 mM | 0.1271 mL | 0.6353 mL | 1.2706 mL | 3.1766 mL | |
| 25 mM | 0.1017 mL | 0.5083 mL | 1.0165 mL | 2.5413 mL | |
| 30 mM | 0.0847 mL | 0.4235 mL | 0.8471 mL | 2.1177 mL | |
| 40 mM | 0.0635 mL | 0.3177 mL | 0.6353 mL | 1.5883 mL | |
| 50 mM | 0.0508 mL | 0.2541 mL | 0.5083 mL | 1.2706 mL | |
| 60 mM | 0.0424 mL | 0.2118 mL | 0.4235 mL | 1.0589 mL | |
| 80 mM | 0.0318 mL | 0.1588 mL | 0.3177 mL | 0.7942 mL | |
| 100 mM | 0.0254 mL | 0.1271 mL | 0.2541 mL | 0.6353 mL |