MLN120B dihydrochloride

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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。

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 mg

5 mg

10 mg

1 mM	2.2742 mL	11.3709 mL	22.7417 mL
5 mM	0.4548 mL	2.2742 mL	4.5483 mL
10 mM	0.2274 mL	1.1371 mL	2.2742 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。