Bohemine 是一种嘌呤类似物,也是一种合成的选择性的CDK抑制剂,对Cdk2/cyclin E,Cdk2/cyclin A和Cdk9/cyclin T1的IC50分别为 4.6 μM,83 μM 和 2.7 μM。Bohemine 还抑制ERK2,IC50为 52 μM,对 CDK1,CDK4 和 CDK6 的抑制作用较小。Bohemine 具有广泛的抗癌活性。
生物活性 | Bohemine is a purine analogue and is a synthetic and selectiveCDKinhibitor withIC50s of 4.6 μM, 83 μM, and 2.7 μM forCdk2/cyclin E,Cdk2/cyclin A, andCdk9/cyclin T1, respectively. Bohemine also inhibitsERK2with anIC50of 52 μM and has less inhibitory effect onCDK1,CDK4andCDK6. Bohemine has a broad spectrum anti-cancer activities[1][2]. |
IC50& Target[2] | 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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体外研究 (In Vitro) | 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 IC50of 27 μM[2].
Cell Viability Assay[1] Cell Line: | Mouse hybridoma ME-750 cells | Concentration: | 0 μM, 1 μM, 3 μM, 10 μM and 30 μM | Incubation Time: | 72 hours | 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. |
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体内研究 (In Vivo) | Bohemine (50 mg/kg; intravenous injection; BALB/c mice) treatment shows Cmaxis 72,308 nM, observed clearance is 0.23 L/h and T1/2is 1.39 h[2].
Animal Model: | BALB/c mice bearing the colon 26 murine tumor[2] | Dosage: | 50 mg/kg | Administration: | Intravenous injection (Pharmacokinetic Analysis) | Result: | Cmaxis 72,308 nM, observed clearance is 0.23 L/h and T1/2is 1.39 h. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 100 mg/mL(293.75 mM;Need ultrasonic) 配制储备液 1 mM | 2.9375 mL | 14.6877 mL | 29.3755 mL | 5 mM | 0.5875 mL | 2.9375 mL | 5.8751 mL | 10 mM | 0.2938 mL | 1.4688 mL | 2.9375 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (7.34 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.34 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (7.34 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.34 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (7.34 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.34 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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