A-385358
Based on 1 Customer Validation
A-385358 is a selective inhibitor of Bcl-XL with Kis of 0.80 and 67 nM for Bcl-XL and Bcl-2, respectively.
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- Pureté: 95.10%
- CAS No.: 406228-55-5
- Formule: C32H41N5O5S2
- Masse moléculaire:639.83
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
Bcl-xL 0.8 nM (Ki) |
Bcl-2 67 nM (Ki) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| DOHH-2 | EC50 |
>30 μM
Compound: 1a
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Inhibition of cell growth in human DoHH2 cells overexpressing Bcl2 in presence of 10% HS
Inhibition of cell growth in human DoHH2 cells overexpressing Bcl2 in presence of 10% HS
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[PMID: 17256834] |
| DOHH-2 | EC50 |
7.25 μM
Compound: 1a
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Inhibition of cell growth in human DoHH2 cells overexpressing Bcl2 in presence of 3% FBS
Inhibition of cell growth in human DoHH2 cells overexpressing Bcl2 in presence of 3% FBS
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[PMID: 17256834] |
| FL5.12 | EC50 |
0.47 μM
Compound: 1a
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Reversal of cytokine withdrawal protection in IL3 dependent Bcl-xL overexpressing mouse FL5.12 cells
Reversal of cytokine withdrawal protection in IL3 dependent Bcl-xL overexpressing mouse FL5.12 cells
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[PMID: 17256834] |
| FL5.12 | EC50 |
13 μM
Compound: 1a
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Reversal of cytokine withdrawal protection in IL3 dependent Bcl2 overexpressing mouse FL5.12 cells in presence of 3% FBS
Reversal of cytokine withdrawal protection in IL3 dependent Bcl2 overexpressing mouse FL5.12 cells in presence of 3% FBS
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[PMID: 17256834] |
| FL5.12 | EC50 |
2.2 μM
Compound: 1a
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Reversal of cytokine withdrawal protection in IL3 dependent Bcl2 overexpressing mouse FL5.12 cells
Reversal of cytokine withdrawal protection in IL3 dependent Bcl2 overexpressing mouse FL5.12 cells
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[PMID: 17256834] |
| FL5.12 | EC50 |
5.1 μM
Compound: 1a
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Reversal of cytokine withdrawal protection in IL3 dependent Bcl-xL overexpressing mouse FL5.12 cells in presence of 3% FBS
Reversal of cytokine withdrawal protection in IL3 dependent Bcl-xL overexpressing mouse FL5.12 cells in presence of 3% FBS
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[PMID: 17256834] |
| SUD4 | EC50 |
>30 μM
Compound: 1a
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Inhibition of cell growth in human SUDHL4 cells overexpressing Bcl2 in presence of 10% HS
Inhibition of cell growth in human SUDHL4 cells overexpressing Bcl2 in presence of 10% HS
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[PMID: 17256834] |
| SUD4 | EC50 |
5.25 μM
Compound: 1a
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Inhibition of cell growth in human SUDHL4 cells overexpressing Bcl2 in presence of 3% FBS
Inhibition of cell growth in human SUDHL4 cells overexpressing Bcl2 in presence of 3% FBS
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[PMID: 17256834] |
In Vitro
A-385358 is a selective inhibitor of Bcl-XL with Kis of 0.80 and 67 nM for Bcl-XL and Bcl-2, respectively, in fluorescence polarization assays. Treatment of IL-3-deprived FL5.12/Bcl-XL cells for 24 hours with A-385358 results in cell killing with an EC50 of 0.47±0.05 μM (n=68). This effect is accompanied by an increase in caspase-3 activity. Consistent with the greater affinity for the Bcl-XL versus Bcl-2 hydrophobic grooves, the EC50 of A-385358 for IL-3-depleted FL5.12/Bcl-2 cells (1.9±0.1 μM; n=55) is 4-fold higher relative to the cytokine-deprived FL5.12/Bcl-XL cells. In addition, A-385358 is more effective at stimulating cytochrome c release from mitochondria isolated from FL5.12/Bcl-XL versus Bcl-2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 406228-55-5
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Appearance Solid
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Masse moléculaire 639.83
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Formule C32H41N5O5S2
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Color White to yellow
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SMILES
O=C(NS(=O)(C1=CC=C(N[C@@H](CSC2=CC=CC=C2)CCN(C)C)C([N+]([O-])=O)=C1)=O)C3=CC=C(N4CCC(C)(C)CC4)C=C3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvant et solubilité
In Vitro:
DMSO : 50 mg/mL (78.15 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)
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: 2.5 mg/mL (3.91 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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 (3.91 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.
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.
Protocole
Kinase Assay[1]
FL5.12 cells suspended in EMB growth medium containing 4% fetal bovine serum (FBS) are incubated at 37°C for 1 hour in 10 μM A-385358. Compound concentration is determined by high-performance liquid chromatography before and after the 1-hour incubation following brief centrifugation. To analyze membrane-bound fractions following compound incubation, cells are washed once with 10 volumes of cold PBS and lysed with 4 mL of water. A-385358 concentration is determined from aliquots of lysate before and after centrifugation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay[1]
A549 cells (1×105) are plated in 96-well plates in medium containing 10% fetal bovine serum. Following attachment, A-385358 is added to one set of wells (final concentration of 50 μM in 10% FBS) and medium is added to another set. [3H]Paclitaxel (5 μM; 0.5 μCi/mL final concentration) is added to all wells and the cells are incubated at 37°C for various periods of time. For washout experiments, cells are exposed first to [3H]paclitaxel for 2 hours. The cells are washed once with medium and then incubated with fresh medium with or without 50 μM A-385358 at 37°C for various periods of time[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration[1]
For efficacy studies, male CD-1 nude mice are inoculated with a 1:5 dilution of tumor brei in 50% Matrigel and analysis is conducted. A-385358 is delivered in a vehicle containing 5% Tween 80, 20% propylene glycol, and 75% PBS (pH 3.8). Paclitaxel is formulated according to the recommendations of the manufacturer. For combination therapy of paclitaxel plus A-385358, both drugs are administered i.p. with the paclitaxel given several hours before treatment with A-385358 (except for immunohistochemistry studies looking at expression of MPM-2 and caspase-3 wherein the two drugs are given simultaneously)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (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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Instruction de manipulation (2659 KB)
Références
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 | 1.5629 mL | 7.8146 mL | 15.6292 mL | 39.0730 mL |
| 5 mM | 0.3126 mL | 1.5629 mL | 3.1258 mL | 7.8146 mL | |
| 10 mM | 0.1563 mL | 0.7815 mL | 1.5629 mL | 3.9073 mL | |
| 15 mM | 0.1042 mL | 0.5210 mL | 1.0419 mL | 2.6049 mL | |
| 20 mM | 0.0781 mL | 0.3907 mL | 0.7815 mL | 1.9536 mL | |
| 25 mM | 0.0625 mL | 0.3126 mL | 0.6252 mL | 1.5629 mL | |
| 30 mM | 0.0521 mL | 0.2605 mL | 0.5210 mL | 1.3024 mL | |
| 40 mM | 0.0391 mL | 0.1954 mL | 0.3907 mL | 0.9768 mL | |
| 50 mM | 0.0313 mL | 0.1563 mL | 0.3126 mL | 0.7815 mL | |
| 60 mM | 0.0260 mL | 0.1302 mL | 0.2605 mL | 0.6512 mL |
A-385358 Related Classifications
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