Sabutoclax
Based on 1 publication(s) in Google Scholar
Sabutoclax is a potent and effective Bcl-2 Family (Bcl-2, Bcl-XL, Mcl-1, Bfl-1) inhibitor with IC50s of 0.32 μM, 0.31 μM, 0.20 μM, and 0.62 μM, respectively. Sabutoclax increases Bax, Bim, PUMA and survivin expression.
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- 純度: 98.03%
- CAS 番号: 1228108-65-3
- 分子式: C42H40N2O8
- 分子量:700.78
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
MedChemExpress(MCE)の使用を引用している文献 Sabutoclax
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生物活性
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Bcl-xL 0.31 μM (IC50) |
BCL2 0.32 μM (IC50) |
Mcl-1 0.2 μM (IC50) |
Bfl-1 0.62 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NCI-H1299 | EC50 |
3.2 μM
Compound: 8r
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Cytotoxicity against human H1299 cells assessed as cell viability after 72 hrs by ATP-LITE assay
Cytotoxicity against human H1299 cells assessed as cell viability after 72 hrs by ATP-LITE assay
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[PMID: 19555126] |
| NCI-H460 | EC50 |
0.33 μM
Compound: 8r
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Cytotoxicity against human H460 cells assessed as cell viability after 72 hrs by ATP-LITE assay
Cytotoxicity against human H460 cells assessed as cell viability after 72 hrs by ATP-LITE assay
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[PMID: 19555126] |
Sabutoclax (0.001-10 μM; 72 h) potentially inhibits cell growth of human prostate cancer, lung cancer cell line[1].
Sabutoclax (0.01 μM-1 μM; 24-48 h) potentially induces cell apoptosis in human diffuse large B-cell lymphoma cell line[1].
Sabutoclax (0 μM-15 μM; 48 h) uptrgulates the level of pro-apoptotic proteins in chemoresistent cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PC-3 and H460
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Concentration:0.001 μM, 0.01 μM, 0.1 μM, 1 μM, 10 μM (PC-3), 0.05 μM, 0.1 μM, 1 μM, 5 μM, 10 μM (H460)
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Incubation Time:72 h
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Result:Showed effectively repressing cell growth in a dose-dependent manner.
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Cell Line:BP3 cell line
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Concentration:0.01 μM, 0.03 μM, 0.1 μM, 1 μM
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Incubation Time:24-48 h
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Result:Effectively induced apoptosis in a dose-dependent manner.
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Cell Line:MCF-7/A02, and CALDOX cells
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Concentration:0 μM, 7.5 μM, 15 μM (MCF-7/A02), 0 μM, 5 μM, 10 μM (CALDOX)
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Incubation Time:48 h
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Result:Showed increasing proteins level of Bax, Bim, PUMA and Survivin in a dose-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:athymic nude mice with tumor xenografts from M2182 cells in s.c.
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Dosage:1 mg/kg, 3 mg/kg, 5 mg/kg
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Administration:Intraperitoneal injection (i.p.)
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Result:Showed ihibiting tumor growth to about 60% of the tumor volume.
化学情報
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CAS 番号 1228108-65-3
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性状 Solid
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分子量 700.78
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分子式 C42H40N2O8
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Color Light brown to brown
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SMILES
O=C(C1=C(O)C(O)=CC2=C(O)[C@@]([C@@]3=C(C)C=C4C(C(NC[C@@H](C5=CC=CC=C5)C)=O)=C(O)C(O)=CC4=C3O)=C(C)C=C12)NC[C@@H](C6=CC=CC=C6)C
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別名
BI-97C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
溶剤 & 溶解度
DMSO : 36.67 mg/mL (52.33 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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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: ≥ 2.75 mg/mL (3.92 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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.
Please enter the basic information of animal experiments:
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-
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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.
純度とドキュメンテーション
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データシート (279 KB)
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SDS (393 KB)
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- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Wei J , et al. BI-97C1, an optically pure Apogossypol derivative as pan-active inhibitor of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins. J Med Chem. 2010 May 27; 53(10):4166-76. [Content Brief]
[2]. Yunhui Hu, et Al. Sabutoclax, pan-active BCL-2 protein family antagonist, overcomes drug resistance and eliminates cancer stem cells in breast cancer. Cancer Lett. 2018 Jun 1:423:47-59. [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 | 1.4270 mL | 7.1349 mL | 14.2698 mL | 35.6745 mL |
| 5 mM | 0.2854 mL | 1.4270 mL | 2.8540 mL | 7.1349 mL | |
| 10 mM | 0.1427 mL | 0.7135 mL | 1.4270 mL | 3.5675 mL | |
| 15 mM | 0.0951 mL | 0.4757 mL | 0.9513 mL | 2.3783 mL | |
| 20 mM | 0.0713 mL | 0.3567 mL | 0.7135 mL | 1.7837 mL | |
| 25 mM | 0.0571 mL | 0.2854 mL | 0.5708 mL | 1.4270 mL | |
| 30 mM | 0.0476 mL | 0.2378 mL | 0.4757 mL | 1.1892 mL | |
| 40 mM | 0.0357 mL | 0.1784 mL | 0.3567 mL | 0.8919 mL | |
| 50 mM | 0.0285 mL | 0.1427 mL | 0.2854 mL | 0.7135 mL |