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Bohemine
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Bohemine图片
CAS NO:189232-42-6
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
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 ECdk2/cyclin ACdk9/cyclin T1IC50分别为 4.6 μM,83 μM 和 2.7 μM。Bohemine 还抑制ERK2IC50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)

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.
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.
分子量

340.42

性状

Solid

Formula

C18H24N6O

CAS 号

189232-42-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL(293.75 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.9375 mL14.6877 mL29.3755 mL
5 mM0.5875 mL2.9375 mL5.8751 mL
10 mM0.2938 mL1.4688 mL2.9375 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。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 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。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 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。