您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > MLN120B
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
MLN120B
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。
MLN120B图片
CAS NO:783348-36-7
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议

产品名称
ML120B
产品介绍
MLN120B (ML120B) 是一种有效的、ATP 竞争性的和具有口服活性的IKKβ抑制剂,IC50为 60 nM。MLN120B 在体内外抑制多发性骨髓瘤细胞生长,也可用于类风湿关节炎的相关研究。
生物活性

MLN120B (ML120B) is a potent, ATP competitive, and orally active inhibitor ofIKKβwith an IC50 of 60 nM. MLN120B inhibits multiple myeloma cell growth in vitro and in vivo and also can be used for the research of rheumatoid arthritis[1][2].

IC50& Target

IKKβ

60 nM (IC50)

体外研究
(In Vitro)

MLB120B (0-20 μM; 90 minutes) inhibits phosphorylation and degradation of IκB in RPMI 8226 and INA6 cells; however, no significant inhibition is observed in MM.1S cells[1].
MLB120B (1.25-20 μM; 90 minutes) completely abrogates TNF-a-induced phosphorylation and degradation of IκB in a dosedependent fashion. Phosphorylation of p65 NF-κB induced by TNF-a is also blocked by MLN120B[1].
MLN120B inhibits proliferation of multiple myeloma cell lines. MM.1S, MM.1R, RPMI 8226, RPMI-LR5, RPMI-Dox40, U266, and INA6 cells. Five percent to fifty percent and 18% to 70% inhibition in proliferation is observed at doses >20 uM and [3H]thymidine uptake, respectively[1].
MLN120B (1.25-40 μM; 72 hours) almost completely blocks stimulation of MM.1S, U266, and INA6 cell growth, as well as IL-6 secretion from BMSCs, induced by multiple myeloma cell adherence to BMSCs[1].
MLN120B shows an inhibitory effect on LPS induced NF-κB activation in RAW267.4 cells. The IC50 values of MLN120B is 1.4 μM, 14.8 μM or 27.3 μM for NF-κB2-luc2, IL8-luc2 or TNF-AIP3-luc2 reporter transfected cells, respectively[3].

Western Blot Analysis[1]

Cell Line:MM.1S cells
Concentration:1.25-20 μM
Incubation Time:90 minutes
Result:Inhibited p- IκB and p-P65 expression in a dose-dependent manner.

Cell Viability Assay[1]

Cell Line:Multiple myeloma cell lines: MM.1S, MM.1R, RPMI 8226, RPMI-LR5, RPMI-Dox40, U266, and INA6 cells
Concentration:1.25 μM-20 μM
Incubation Time:72 hours
Result:Inhibits proliferation of multiple myeloma cell lines.
体内研究
(In Vivo)

MLN120B (oral administration; 50 mg/kg; twice daily; 3 weeks) induces a reduction of shuIL-6R, marker of tumor growth, marker of tumor growth. It also leads to a rend toward prolonged survival in animals treated versus control[1].
MLN120B (oral administration; 1-30 mg/kg; twice daily; 3 weeks) inhibits paw swelling in a dose-dependent manner and offers significant protection against arthritis-induced weight loss as well as cartilage and bone erosion. NF-κB activity in arthritic joints is also reduced after MLN120B administration[2].

Animal Model:Two-month-old female Lewis rats[2]
Dosage:30 mg/kg, 10 mg/kg, 3 mg/kg, or 1 mg/kg
Administration:Oral administration; twice daily; 3 weeks
Result:Protected against bone and cartilage destruction in a rat model.
Animal Model:SCID mice implanted with human fetal bone chips and then INA6 cells are directly injected into mice[1]
Dosage:50 mg/kg
Administration:Oral administration; twice daily; 3 weeks
Result:Inhibited human multiple myeloma cell growth in vivo.
分子量

366.80

性状

Solid

Formula

C19H15ClN4O2

CAS 号

783348-36-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : ≥ 31 mg/mL(84.51 mM)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.7263 mL13.6314 mL27.2628 mL
5 mM0.5453 mL2.7263 mL5.4526 mL
10 mM0.2726 mL1.3631 mL2.7263 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    90%corn oil

    Solubility: ≥ 2.5 mg/mL (6.82 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.82 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。

  • 2.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.08 mg/mL (5.67 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.67 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 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
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: 2.08 mg/mL (5.67 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (5.67 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 20.8 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
*以上所有助溶剂都可在本网站选购。