S55746 hydrochloride
Based on 1 publication(s) in Google Scholar
S55746 hydrochloride (BCL201 hydrochloride) is a potent, orally active and selective BCL-2 inhibitor, with a Ki of 1.3 nM and a Kd of 3.9 nM. S55746 hydrochloride (BCL201 hydrochloride) has antitumor activity with low toxicity.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 98.83%
- CAS. Nr.: 1448525-91-4
- Formel: C43H43ClN4O6
- Molecular Weight:747.28
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Speicherung:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) S55746 hydrochloride
More
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
Bcl-2 1.3 nM (Ki) |
Bcl-xL 520 nM (Ki) |
Bcl-2 3.9 nM (Kd) |
Bcl-xL 186 nM (Kd) |
In Vitro
S55746 (0-1 μM) potently and selectively induces cell death[1].
S55746 selectively induces apoptosis through BCL-2 inhibition in a BAX/BAK-dependent manner[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:H146 and RS4;11 cell lines.
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Concentration:0, 0.1, 0.3 and 1 μM.
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Incubation Time:72 hours.
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Result:Potently induced RS4;11 cell killing after 72 h of treatment with an IC50 of 71.6 nM.
In Vivo
S55746 (20-100 mg/kg, p.o.) inhibits xenograft growth in RS4;11 and Toledo models time- and dose-dependently[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female SCID/beige mice implanted subcutaneously with 3×106 Toledo or RS4;11[1].
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Dosage:20, 50, 100 mg/kg.
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Administration:Oral gavage daily for 7 consecutive days.
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Result:Induced significant anti-tumor activity time- and dose-dependently.
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Animal Model:SCID/beige female mice with RS4;11 tumor xenografts[1].
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Dosage:25 and 100 mg/kg.
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Administration:Single oral gavage treatment.
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Result:Did not induce platelet loss in vivo at 25 and 100 mg/kg.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 1448525-91-4
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Appearance Solid
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Molecular Weight 747.28
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Formel C43H43ClN4O6
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Color White to yellow
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SMILES
O=C(C1=C2CCCCN2C(C3=C(C(N4CC5=C(C=CC=C5)C[C@H]4CN6CCOCC6)=O)C=C(OCO7)C7=C3)=C1)N(C8=CC=C(O)C=C8)C9=CC=CC=C9.Cl
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Synonyms
BCL201 hydrochloride
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (1)
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Journal Impact Factor
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Most Recent
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Biomed Pharmacother
Foeniculum vulgare seed extract induces apoptosis in lung cancer cells partly through the down-regulation of Bcl-2. [Abstract]2021 Mar:135:111213. PMID: 33395604
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 200 mg/mL (267.64 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 (stored under nitrogen). 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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (6.69 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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.
Protokoll
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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.
Reinheit & Dokumentation
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Data Sheet (285 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)
Verweise
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 (stored under nitrogen). 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 |
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| DMSO | 1 mM | 1.3382 mL | 6.6909 mL | 13.3819 mL | 33.4547 mL |
| 5 mM | 0.2676 mL | 1.3382 mL | 2.6764 mL | 6.6909 mL | |
| 10 mM | 0.1338 mL | 0.6691 mL | 1.3382 mL | 3.3455 mL | |
| 15 mM | 0.0892 mL | 0.4461 mL | 0.8921 mL | 2.2303 mL | |
| 20 mM | 0.0669 mL | 0.3345 mL | 0.6691 mL | 1.6727 mL | |
| 25 mM | 0.0535 mL | 0.2676 mL | 0.5353 mL | 1.3382 mL | |
| 30 mM | 0.0446 mL | 0.2230 mL | 0.4461 mL | 1.1152 mL | |
| 40 mM | 0.0335 mL | 0.1673 mL | 0.3345 mL | 0.8364 mL | |
| 50 mM | 0.0268 mL | 0.1338 mL | 0.2676 mL | 0.6691 mL | |
| 60 mM | 0.0223 mL | 0.1115 mL | 0.2230 mL | 0.5576 mL | |
| 80 mM | 0.0167 mL | 0.0836 mL | 0.1673 mL | 0.4182 mL | |
| 100 mM | 0.0134 mL | 0.0669 mL | 0.1338 mL | 0.3345 mL |
S55746 hydrochloride Related Classifications
HY-117288A Related Classifications
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