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MLN120B dihydrochloride
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 dihydrochloride图片
CAS NO:1782573-78-7
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议

产品名称
ML120B dihydrochloride
产品介绍
MLN120B dihydrochloride (ML120B dihydrochloride) 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 dihydrochloride (ML120B dihydrochloride) 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].

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:5 μM; 10 μM; 20 μM
Incubation Time:90 mintues
Result:Inhibited p-IκB and p-P65 expression in a dose-dependent manner.

Cell Viability Assay[1]

Cell Line:Myeloma cell lines: MM.1S, MM.1R, RPMI 8226, RPMI-LR5, RPMI-Dox40, U266, and INA6 cells
Concentration:0-40 μM
Incubation Time:72 hours
Result:Inhibited 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; 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[3].

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.
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.
分子量

439.72

性状

Solid

Formula

C19H17Cl3N4O2

CAS 号

1782573-78-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : 16.67 mg/mL(37.91 mM;ultrasonic and warming and adjust pH to 8 with NaOH and heat to 80℃)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.2742 mL11.3709 mL22.7417 mL
5 mM0.4548 mL2.2742 mL4.5483 mL
10 mM0.2274 mL1.1371 mL2.2742 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 (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。