ML 120B dihydrochloride(free base)|783348-36-7|(ML120B)-陌孚医药/Medlife

您当前的位置：

ML 120B dihydrochloride(free base) (Synonyms: ML120B)

目录号: PC11574 纯度: ≥98%

CAS No. :783348-36-7

商品编号	规格	价格	会员价	是否有货	数量
PC11574-10mg	10mg	¥4892.00	请登录
PC11574-50mg	50mg	¥20524.00	请登录

Medlife所售产品仅用于科学研究（非临床研究），非药品不可食用，不可用于人体或动物的临床诊断和治疗，我们不为个人提供产品及服务。产品COA等资料，可至下方“质量控制”中下载。

加入购物车在线咨询收藏产品大包装询价

中文名称

ML 120B dihydrochloride(free base)

中文别名

N-(6-氯-7-甲氧基-9H-吡啶并[3,4-B]吲哚-8-基)-2-甲基-3-吡啶甲酰胺;N-(6-氯-7-甲氧基-9h-吡啶并[3,4-b]吲哚-8-基)-2-甲基-3-吡啶羧酰胺

英文名称

ML 120B dihydrochloride(free base)

英文别名

N-(6-Chloro-7-methoxy-9H-pyrido[3,4-b]indol-8-yl)-2-methylnicotinamide;MLN120B;ML 120B Dihydrochloride;N-(6-chloro-7-methoxy-9H-pyrido[3,4-b]indol-8-yl)-2-methyl-3-Pyridinecarboxamide;N-(6-chloro-7-methoxy-9H-pyrido[3,4-b]indol-8-yl)-2-methylpyridine-3-carboxamide;CHEBI:700132;CHEMBL608154;CS-1291;ML120B;ML-120B;MLN-120B;SureCN1420073

Cas No.

783348-36-7

分子式

C₁₉H₁₅N₄O₂Cl

分子量

366.80

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

MLN120B (ML120B) is a potent, ATP competitive, and orally active inhibitor of IKKβ with an IC₅₀ of 60 nM. MLN120B inhibits multiple myeloma cell growth 体外研究 and in vivo and also can be used for the research of rheumatoid arthritis.

性状

Solid

IC50 & Target[1][2]

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.
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.
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 [H]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].

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis

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

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.
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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Two-month-old female Lewis rats
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
Dosage:	50 mg/kg
Administration:	Oral administration; twice daily; 3 weeks
Result:	Inhibited human multiple myeloma cell growth in vivo.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[1]. Hideshima T, et all. MLN120B, a novel IkappaB kinase beta inhibitor, blocks multiple myeloma cell growth 体外研究 and in vivo. Clin Cancer Res. 2006 Oct 1;12(19):5887-94. [Information]

[2]. Schopf L, et al. IKKbeta inhibition protects against bone and cartilage destruction in a rat model of rheumatoid arthritis. Arthritis Rheum. 2006 Oct;54(10):3163-73. [Information]

[3]. Ansaldi D, et al. Imaging pulmonary NF-kappaB activation and therapeutic effects of MLN120B and TDZD-8. PLoS One. 2011;6(9):e25093. [Information]

[4]. Nagashima K, et al. Rapid TNFR1-dependent lymphocyte depletion in vivo with a selective chemical inhibitor of IKKbeta. Blood. 2006 Jun 1;107(11):4266-73. [Information]

溶解度数据

体外研究:

DMSO : ≥ 31 mg/mL (84.51 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.7263 mL	13.6314 mL	27.2628 mL
5 mM	0.5453 mL	2.7263 mL	5.4526 mL
10 mM	0.2726 mL	1.3631 mL	2.7263 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： 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.

建议依照次序添加每种溶剂： 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 ddH?O 中，得到澄清透明的生理盐水溶液
3.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in 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 μL 20% 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

搜索质检报告(COA)

产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

相关产品

The molarity calculator equation

The dilution calculator equation