Powder: -20°C for 3 years | In solvent: -80°C for 1 year
MLN120B dihydrochloride (ML120B dihydrochloride) is a highly potent, orally active inhibitor of IKKβ. It competitively binds to ATP and exhibits an impressive IC50 value of 60 nM. This compound effectively suppresses the growth of multiple myeloma cells both in vitro and in vivo. Furthermore, MLN120B dihydrochloride is valuable in the field of rheumatoid arthritis research.
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 648 | 5日内发货 | ||
5 mg | ¥ 1,300 | 5日内发货 |
产品描述 | MLN120B dihydrochloride (ML120B dihydrochloride) is a highly potent, orally active inhibitor of IKKβ. It competitively binds to ATP and exhibits an impressive IC50 value of 60 nM. This compound effectively suppresses the growth of multiple myeloma cells both in vitro and in vivo. Furthermore, MLN120B dihydrochloride is valuable in the field of rheumatoid arthritis research. |
体外活性 | 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 [ 3 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 IC 50 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. |
体内活性 | 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. |
别名 | ML120B dihydrochloride |
分子量 | 439.72 |
分子式 | C19H17Cl3N4O2 |
CAS No. | 1782573-78-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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