Bcl-xL antagonist 2
Based on 1 Customer Validation
Bcl-xL antagonist 2 is a potent, selective, and orally active antagonist of BCL-XL with an IC50 and Ki of 0.091 μM and 65 nM, respectively. Bcl-xL antagonist 2 promotes the apoptosis of cancer cells. Bcl-xL antagonist 2 has the potential for the research of the chronic lymphocytic leukemia (CLL) and non-Hodgkin’s lymphoma (NHL).
For research use only. We do not sell to patients.
- Purity: 98.86%
- CAS No.: 1235032-75-3
- Formula: C21H16N4O3S2
- Molecular Weight:436.51
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
0.091 μM (BCL-XL)[1]
| iv (1 mg/kg) | po (5 mg/kg) | ||
| CLp (mL/min/kg) | Vss (L/kg) | t 1/2 (h) | F % |
| 0.47 | 0.16 | 6.0 | 16 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1235032-75-3
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Appearance Solid
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Molecular Weight 436.51
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Formula C21H16N4O3S2
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Color Light yellow to green yellow
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SMILES
O=C(C1=C(CN(C2=NC(C(O)=O)=CS2)CC3)C3=CC=C1)NC4=NC5=C(S4)C=CC=C5
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 62.5 mg/mL (143.18 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)
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.
Purity & Documentation
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Data Sheet (289 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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Handling Instructions (2659 KB)
References
[1]. Koehler MF, et al. Structure-Guided Rescaffolding of Selective Antagonists of BCL-XL. ACS Med Chem Lett. 2014;5(6):662-667. [Content Brief]
[2]. Wang L, et al. Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-XL Inhibitor. ACS Med Chem Lett. 2020;11(10):1829-1836. [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. 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 | 2.2909 mL | 11.4545 mL | 22.9090 mL | 57.2725 mL |
| 5 mM | 0.4582 mL | 2.2909 mL | 4.5818 mL | 11.4545 mL | |
| 10 mM | 0.2291 mL | 1.1454 mL | 2.2909 mL | 5.7272 mL | |
| 15 mM | 0.1527 mL | 0.7636 mL | 1.5273 mL | 3.8182 mL | |
| 20 mM | 0.1145 mL | 0.5727 mL | 1.1454 mL | 2.8636 mL | |
| 25 mM | 0.0916 mL | 0.4582 mL | 0.9164 mL | 2.2909 mL | |
| 30 mM | 0.0764 mL | 0.3818 mL | 0.7636 mL | 1.9091 mL | |
| 40 mM | 0.0573 mL | 0.2864 mL | 0.5727 mL | 1.4318 mL | |
| 50 mM | 0.0458 mL | 0.2291 mL | 0.4582 mL | 1.1454 mL | |
| 60 mM | 0.0382 mL | 0.1909 mL | 0.3818 mL | 0.9545 mL | |
| 80 mM | 0.0286 mL | 0.1432 mL | 0.2864 mL | 0.7159 mL | |
| 100 mM | 0.0229 mL | 0.1145 mL | 0.2291 mL | 0.5727 mL |