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- 详细信息
- 文献和实验
- 技术资料
- 库存:
大量
- 英文名:
MLN2238(Ixazomib/MLN-2238)
- CAS号:
1072833-77-2
- 保质期:
2年
- 供应商:
翌圣生物科技(上海)股份有限公司
- 保存条件:
-20度
- 规格:
5mg
产品信息
| 产品名称 |
产品编号 |
规格 |
价格 |
| MLN2238(Ixazomib; MLN-2238) |
52802ES08 |
5 mg |
995 |
| MLN2238(Ixazomib; MLN-2238) |
52802ES10 |
10 mg |
1295 |
产品描述
MLN2238(Ixazomib; MLN-2238)选择性高效抑制20S proteasome的糜蛋白酶样蛋白水解(β5)位点,其IC50值是3.4 nM,Ki值是0.93 nM。同时,MLN2238抑制胱天蛋白酶样(β1)和胰蛋白酶样(β2)蛋白水解位点,其IC50值分别是31 nM和3500 nM。
产品性质
| 英文别名(English Synonym) |
(R)-1-(2-(2,5-dichlorobenzamido)acetamido)-3-methylbutylboronic acid |
| 中文名称 (Chinese Name) |
艾沙佐米 |
| 靶点(Target) |
20S proteasome |
| CAS号(CAS NO.) |
1072833-77-2 |
| 分子式(Formula) |
C14H19BCl2N2O4 |
| 分子量(Molecular Weight) |
361.03 |
| 外观(Appearance) |
粉末 |
| 纯度(Purity) |
≥95% |
| 溶解性(Solubility) |
易溶于DMSO |
| 结构式(Structure) |
|
运输和保存方法
冰袋运输。粉末直接保存于-20℃,有效期2年。建议分装后-20℃避光保存,避免反复冻融。
注意事项
1)为了您的安全和健康,请穿实验服并戴一次性手套操作。
2)粉末溶解前请先短暂离心,以保证产品全在管底。
3)本产品仅用于科研用途,禁止用于人身上。
使用浓度
【具体使用浓度请参考相关文献,并根据自身实验条件(如实验目的,细胞种类,培养特性等)进行摸索和优化。】
使用方法(数据来自于公开发表的文献,仅供参考)
(一)细胞实验(体外实验)
MLN2238(≤ 10 nM,1 h)作用Calu-6细胞,可抑制Calu-6细胞增殖,其IC50值为9.7 nM。[1]
(二)动物实验(体内实验)
MLN2238(11 mg/kg;静脉注射)处理携带DP54-Luc肿瘤的NOD-SCID小鼠,每周2次,持续17天,MLN2238降低肿瘤负荷(T/C值分别为0.48和0.22)。与硼替佐米相比,MLN2238在多种B细胞淋巴瘤和PCM(浆细胞恶性肿瘤)小鼠模型中的抗肿瘤活性有所提高。[2]
参考文献
[1]. Kupperman E, et al. Evaluation of the proteasome inhibitor MLN9708 in preclinical models of human cancer. Cancer Research, 2010, 70 (5): 1970-80.
[2]. Lee E C, et al. Antitumor activity of the investigational proteasome inhibitor MLN9708 in mouse models of B-cell and plasma cell malignancies.[J]. Clinical Cancer Research, 2011, 17(23):7313-7323.
HB211216
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文献和实验[1]. Kupperman E, et al. Evaluation of the proteasome inhibitor MLN9708 in preclinical models of human cancer. Cancer Research, 2010, 70 (5): 1970-80.
[2]. Lee E C, et al. Antitumor activity of the investigational proteasome inhibitor MLN9708 in mouse models of B-cell and plasma cell malignancies.[J]. Clinical Cancer Research, 2011, 17(23):7313-7323.
The 20S proteasome is a multicatalytic protein complex, present in all eukaryotic cells, that plays a major role in intracellular protein degradation. In mammalian cells, this symmetrical cylindrical complex is composed of two copies
Assays for Proteasome Inhibition
activity of the proteasome is contained within this central 20S core (MW=730 kDa), a multicatalytic protease that has three well characterized peptidase activities. The three peptidases: chymotryptic, tryptic, and postglutamyl peptide hydrolytic activities
Assays for Proteasome Assembly and Maturation
The 20S proteasome is a complex multisubunit protease that is present in all phylae of life. Eukaryotic 26S proteasomes, which are composed of 20S proteasomes and 19S activator complexes, mediate the degradation of ubiquitylated proteins
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