Bohemine
Based on 1 publication(s) in Google Scholar
Bohemine is a purine analogue and is a synthetic and selective CDK inhibitor with IC50s of 4.6 μM, 83 μM, and 2.7 μM for Cdk2/cyclin E, Cdk2/cyclin A, and Cdk9/cyclin T1, respectively. Bohemine also inhibits ERK2 with an IC50 of 52 μM and has less inhibitory effect on CDK1, CDK4 and CDK6. Bohemine has a broad spectrum anti-cancer activities.
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- 純度: 98.93%
- CAS 番号: 189232-42-6
- 分子式: C18H24N6O
- 分子量:340.42
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 Bohemine
More
生物活性
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CDK2/cyclinE 4.6 μM (IC50) |
cdk2/cyclin A 83 μM (IC50) |
CDK9/cyclinT1 2.7 μM (IC50) |
ERK2 52 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CCRF-CEM | IC50 |
27 μM
Compound: Bohemine
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In vitro cytotoxic effect on CEM cancer cell line
In vitro cytotoxic effect on CEM cancer cell line
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[PMID: 12392733] |
| G-361 | IC50 |
45 μM
Compound: Bohemine
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In vitro cytotoxic effect on G361 cancer cell line
In vitro cytotoxic effect on G361 cancer cell line
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[PMID: 12392733] |
| HOS | IC50 |
58 μM
Compound: Bohemine
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In vitro cytotoxic effect on HOS cancer cell line
In vitro cytotoxic effect on HOS cancer cell line
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[PMID: 12392733] |
| K562 | IC50 |
113 μM
Compound: Bohemine
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In vitro cytotoxic effect on K562 cancer cell line
In vitro cytotoxic effect on K562 cancer cell line
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[PMID: 12392733] |
| MCF7 | IC50 |
28 μM
Compound: Bohemine
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In vitro cytotoxic effect on MCF-7 cancer cell line
In vitro cytotoxic effect on MCF-7 cancer cell line
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[PMID: 12392733] |
Bohemine (0-30 μM; 72 hours; ME-750 cells) treatment inhibits cell growth. Addition of Bohemine at concentrations in the range of 1-10 μM results in a short-term arrest of growth and of monoclonal antibody production. The short-term suppression of cell functions is followed by a significant temporary increase of specific growth rate and of specific production rate[1].
Hybridoma cells are retarded both at the G1/S boundary and at the G2/M boundary, depending on Bohemine (0-30 μM) concentration[1].
T-lymphoblastic cell line CEM is treated by Bohemine, five proteins are found to be downregulated, namely α-enolase, triosephosphate isomerase, initiation factor 5A, and α- and β-subunits of Rho GDP-dissociation inhibitor 1. These proteins play significant roles in glycolysis, proteosynthesis, and in cytoskeleton rearrangement[1].
Bohemine inhibits growth of human tumor cell lines with an IC50 of 27 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Mouse hybridoma ME-750 cells
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Concentration:0 µM, 1 µM, 3 µM, 10 µM and 30 µM
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Incubation Time:72 hours
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Result:At 10 µM and 30 µM concentrations, the viable cell count was significantly lower with respect to control, i.e., 77% and 48%, respectively.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c mice bearing the colon 26 murine tumor[2]
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Dosage:50 mg/kg
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Administration:Intravenous injection (Pharmacokinetic Analysis)
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Result:Cmax is 72,308 nM, observed clearance is 0.23 L/h and T1/2 is 1.39 h.
化学情報
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CAS 番号 189232-42-6
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性状 Solid
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分子量 340.42
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分子式 C18H24N6O
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Color White to off-white
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SMILES
OCCCNC1=NC(NCC2=CC=CC=C2)=C3N=CN(C(C)C)C3=N1
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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 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
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EMBO Rep
2022 Jun 7;23(6):e53932. PMID: 35403787
溶剤 & 溶解度
DMSO : 100 mg/mL (293.75 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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.34 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 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 (7.34 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.
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.
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 (252 KB)
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- Français - FR (252 KB)
- Deutsch - DE (252 KB)
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- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Franek F, et al. Diverse effects of the cyclin-dependent kinase inhibitor bohemine: Concentration- and time-dependent suppression or stimulation of hybridoma culture. Cytotechnology. 2001 Jul;36(1-3):117-23. [Content Brief]
[2]. Raynaud FI, et al. In vitro and in vivo pharmacokinetic-pharmacodynamic relationships for the trisubstituted aminopurine cyclin-dependent kinase inhibitors olomoucine, bohemine and CYC202. Clin Cancer Res. 2005 Jul 1;11(13):4875-87. [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 | 2.9375 mL | 14.6877 mL | 29.3755 mL | 73.4387 mL |
| 5 mM | 0.5875 mL | 2.9375 mL | 5.8751 mL | 14.6877 mL | |
| 10 mM | 0.2938 mL | 1.4688 mL | 2.9375 mL | 7.3439 mL | |
| 15 mM | 0.1958 mL | 0.9792 mL | 1.9584 mL | 4.8959 mL | |
| 20 mM | 0.1469 mL | 0.7344 mL | 1.4688 mL | 3.6719 mL | |
| 25 mM | 0.1175 mL | 0.5875 mL | 1.1750 mL | 2.9375 mL | |
| 30 mM | 0.0979 mL | 0.4896 mL | 0.9792 mL | 2.4480 mL | |
| 40 mM | 0.0734 mL | 0.3672 mL | 0.7344 mL | 1.8360 mL | |
| 50 mM | 0.0588 mL | 0.2938 mL | 0.5875 mL | 1.4688 mL | |
| 60 mM | 0.0490 mL | 0.2448 mL | 0.4896 mL | 1.2240 mL | |
| 80 mM | 0.0367 mL | 0.1836 mL | 0.3672 mL | 0.9180 mL | |
| 100 mM | 0.0294 mL | 0.1469 mL | 0.2938 mL | 0.7344 mL |
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