Ambeed 大中华区 CN | ZH

中文 - ZH English - EN

Ambeed.cn

搜索

关键字搜索批量搜索

首页 收藏 购物车0
首页 / 抑制剂/激动剂 / 泛素 / 蛋白酶体 / Ixazomib/艾沙佐米

Ixazomib/艾沙佐米 {[allProObj[0].p_purity_real_show]}

货号：A172813 同义名： 伊沙佐米(MLN2238) / MLN2238

Ixazomib（MLN2238）是一种选择性、强效和可逆的蛋白酶体抑制剂，靶向20S蛋白酶体的胰凝乳蛋白酶样蛋白水解（β5）位点，IC50为3.4 nM，Ki为0.93 nM。

Ixazomib/艾沙佐米 化学结构 CAS号：1072833-77-2
Ixazomib/艾沙佐米 化学结构
CAS号：1072833-77-2
Ixazomib/艾沙佐米 3D分子结构
CAS号：1072833-77-2
Ixazomib/艾沙佐米 化学结构 CAS号：1072833-77-2
Ixazomib/艾沙佐米 3D分子结构 CAS号：1072833-77-2
规格 价格 会员价 库存 数量
{[ item.pr_size ]}

{[ getRatePriceInt(item.pr_rmb, 1,1) ]}

{[ getRatePriceInt(item.pr_rmb_sale, 1,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]}

{[ getRatePriceInt(item.pr_rmb, 1,1) ]}

{[ getRatePriceInt(item.pr_rmb,item.pr_rate,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]} 		{[ getRatePriceInt(item.pr_rmb, 1,1) ]}{[ suihuo_tips(item.pr_tag_price, item.pr_am) ]} {[ getRatePrice(item.pr_rmb_sale, 1,1,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate,item.mem_isinteger) ]} 现货 1周 咨询 - +
购物车0 收藏 询单

Ixazomib/艾沙佐米 纯度/质量文件 产品仅供科研

货号：A172813 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
• Cell, 2025. Ambeed. [ A122167 ]
• Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]
• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
• Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]
更多 >
产品名称 20S proteasome ↓ Proteasome ↓ 其他靶点 纯度
Ixazomib ++++

20S proteasome, IC50: 3.4 nM

20S proteasome, Ki: 0.93 nM

 		99%+
Delanzomib +++

Chymotrypsin-like proteasome, IC50: 3.8 nM

 		98%
Celastrol +

20S proteasome, IC50: 2.5 μM

 		98%
MLN9708 +++

20S proteasome, IC50: 3.4 nM

20S proteasome, Ki: 0.93 nM

 		99%
Bortezomib ++++

20S proteasome, Ki: 0.6 nM

 		98%
Oprozomib ++

20S proteasome β5, IC50: 36 nM

20S proteasome LMP7, IC50: 82 nM

 		99%+
Epoxomicin ✔ 95%
PI-1840 ++

Chymotrypsin-like proteasome, IC50: 27 nM

 		98%
VR23 +++

Trypsin-like proteasomes, IC50: 1 nM

Chymotrypsin-like proteasomes, IC50: 3 μM

 		99%
Carfilzomib ++

Proteasome, IC50: 5 nM

 		98%
(R)-MG-132 +

Proteasome, IC50: 100 nM

 		98% (NMR）
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Ixazomib/艾沙佐米 生物活性

靶点

  • 20S proteasome

    20S proteasome, IC50:3.4 nM

    20S proteasome, Ki:0.93 nM
描述 The ubiquitin-proteasome system is responsible for the regulation of cellular protein homeostasis. By inhibiting proteasome activity, the anti-proliferative signals and the apoptotic pathways can be activated in cells, which makes proteasome an attractive therapeutic target in cancer treatment. Ixazomib is an N-capped dipeptidyl leucine boronic acid that inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with an IC50 value of 3.4 nmol/l (Ki value of 0.93 nmol/l). It also inhibits the caspase-like (β1) and trypsin-like (β2) proteolytic sites with IC50 values of 31 and 3500 nmol/l, respectively. The proteasome dissociation half-life (t1/2) for ixazomib is 18 minutes. In MDA-MB-231 cells expressing a 4  Ub-Luc reporter, ixazomib inhibited proteasome activity with an EC50 value of 525 nmol/l. In HEK293 cells stably expressing a NF-κB-Luc reporter, ixazomib inhibited TNF-α-induced activation of NF-κB pathway with an EC50 value of 55 nmol/l. The anti-proliferative effects of ixazomib in A375 (lung), H460 (lung), HCT-116 (colon), and HT-29 (colon) cells were determined by cell viability assay with LD50 values ranged from 19 – 58 nmol/l. In mice i.v. administrated with a single dose of ixazomib at 14 mg/kg, the blood volume distribution at steady state was 20.2 L/kg. In Sprague-Dawley rats i.v. injected with a single of ixazomib at 0.2 or 0.3 mg/kg, the plasma exposure (AUC0-48h) of ixazomib was 704 and 1070 h.ng/ml, respectively. In CB17-SCID mice bearing xenograft tumors, the maximum level of blood proteasome inhibition was 83.1% following an acute i.v. treatment of 14 mg/kg ixazomib. The tumor to blood AUE ratio for ixazomib in human prostate tumor (CWR22) and human lymphoma tumor (WSU-DLCL2s) xenografts was 1.56 and 2.03, respectively. Ixazomib dosed at 7 mg/kg or 14 mg/kg showed significant antitumor effects in xenografts 22 days after the administration.
作用机制 Ixazomib inhibits 20S proteasome by binding to the chymotrypsin-like proteolytic (β5) site of the proteasome.

Ixazomib/艾沙佐米 细胞实验

Cell Line
Concentration Treated Time Description References
MM.1S 12 nM 24 hours Induced accumulation of ubiquitinated proteins Clin Cancer Res. 2011 Aug 15;17(16):5311-21.
MM.1S 5 nM 3 hours Inhibited CT-L proteasome activity Clin Cancer Res. 2011 Aug 15;17(16):5311-21.
Hut78 12.5–1000nM 72 hours To evaluate the cytotoxicity and apoptosis-inducing effects of ixazomib on T-cell lymphoma cells, results showed that ixazomib induced significant cell death in all cell lines Cancer Res. 2016 Jun 1;76(11):3319-31.
HH 12.5–1000nM 72 hours To evaluate the cytotoxicity and apoptosis-inducing effects of ixazomib on T-cell lymphoma cells, results showed that ixazomib induced significant cell death in all cell lines Cancer Res. 2016 Jun 1;76(11):3319-31.
L428 25nM 24 hours To evaluate the cytotoxicity and apoptosis-inducing effects of ixazomib on Hodgkin lymphoma cells, results showed that L428 cells were less sensitive to ixazomib Cancer Res. 2016 Jun 1;76(11):3319-31.
L540 25nM 24 hours To evaluate the cytotoxicity and apoptosis-inducing effects of ixazomib on Hodgkin lymphoma cells, results showed that L540 cells were most sensitive to ixazomib Cancer Res. 2016 Jun 1;76(11):3319-31.
Jurkat 25nM 24 hours To evaluate the cytotoxicity and apoptosis-inducing effects of ixazomib on T-cell lymphoma cells, results showed that ixazomib induced significant cell death in all cell lines Cancer Res. 2016 Jun 1;76(11):3319-31.
DP54-Luc cells 24.6 nmol/L (LD50) Evaluate cytotoxicity of MLN2238 on DP54-Luc cells Clin Cancer Res. 2011 Dec 1;17(23):7313-23.
MN647D 100 nM 24 hours Evaluate the effect of MLN9708 on cell viability and apoptosis in NF2-deficient meningioma cell lines. Results showed that MLN9708 significantly reduced cell viability and induced apoptosis. Neuro Oncol. 2023 Sep 5;25(9):1617-1630.
MN597 100 nM 24 hours Evaluate the effect of MLN9708 on cell viability and apoptosis in NF2-deficient meningioma cell lines. Results showed that MLN9708 significantly reduced cell viability and induced apoptosis. Neuro Oncol. 2023 Sep 5;25(9):1617-1630.
MN1-LF 100 nM 24 hours Evaluate the effect of MLN9708 on cell viability and apoptosis in NF2-deficient meningioma cell lines. Results showed that MLN9708 significantly reduced cell viability and induced apoptosis. Neuro Oncol. 2023 Sep 5;25(9):1617-1630.
Ben-Men-1 100 nM 24 hours Evaluate the effect of MLN9708 on cell viability and apoptosis in NF2-deficient meningioma cell lines. Results showed that MLN9708 significantly reduced cell viability and induced apoptosis. Neuro Oncol. 2023 Sep 5;25(9):1617-1630.

Ixazomib/艾沙佐米 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice NF2-deficient meningioma and schwannoma models Oral gavage 7 mg/kg Every 3 days for 4-6 weeks Evaluate the antitumor efficacy of MLN9708 in NF2-deficient meningioma and schwannoma mouse models. Results showed that MLN9708 significantly delayed tumor growth. Neuro Oncol. 2023 Sep 5;25(9):1617-1630.
SCID mice Jurkat or L540 cell-derived xenograft models Intraperitoneal injection 0.36 or 0.72mg/kg Once daily for 5 days, continued for three weeks To evaluate the antitumor activity of ixazomib in vivo against T-cell lymphoma and Hodgkin lymphoma xenografts, results showed that ixazomib significantly inhibited tumor growth and improved survival Cancer Res. 2016 Jun 1;76(11):3319-31.
NOD.SCID/NCR mice A549 xenograft tumors Subcutaneous injection 15 mg/kg Daily for 3 weeks Evaluate the inhibitory effect of MLN9708 on tumor growth Nat Commun. 2021 Dec 3;12(1):6941.
NSG mice HCC PDX model Intraperitoneal injection (dinaciclib) and oral gavage (ixazomib) 7 mg/kg Three times a week until tumor volume reached 2000 mm³ To evaluate the inhibitory effects of MLN9708 in combination with dinaciclib on HCC PDX tumor growth. Results showed that the combination therapy significantly inhibited tumor growth, outperforming monotherapy and the standard treatment drug sorafenib. J Exp Clin Cancer Res. 2022 Aug 15;41(1):249.
CB-17 SCID mice Human plasmacytoma xenograft model Intravenous and oral 11 mg/kg (i.v), 8 mg/kg (oral) Twice weekly for 3 weeks Significantly inhibited tumor growth and prolonged survival Clin Cancer Res. 2011 Aug 15;17(16):5311-21.
Mice OCI-Ly10 and PHTX22L xenograft models Intravenous injection 8 mg/kg (OCI-Ly10), 14 mg/kg (PHTX22L) Once or twice weekly for 4 weeks Evaluate antitumor activity of MLN2238 in B-cell lymphoma models Clin Cancer Res. 2011 Dec 1;17(23):7313-23.

Ixazomib/艾沙佐米 动物研究

Dose Mice: 2 mg/kg - 14 mg/kg[2] (i.v.), 3.5 mg/kg[3] (p.o>), 8 mg/kg[2] (p.o.), 11 mg/kg[1] (p.o.) Rat: 0.2 mg/kg, 0.3 mg/kg[1] (i.v.)
Administration i.v., p.o.
Pharmacokinetics
Animal Mice[4]
Dose 14 mg/kg (i.v.)
11 mg/kg (p.o.)
Administration i.v.
p.o.
F 59.5% (p.o.)
Vd 20.2 L/kg (i.v.)
Cmax 10500 ng/ml (i.v.)
1710 ng/ml (p.o.)
AUC0→24h 9660 h·ng/ml (i.v.)
6310 h·ng/ml (p.o.)

Ixazomib/艾沙佐米 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02765854 Recurrent Plasma Cell Myeloma ... 展开 >> Refractory Plasma Cell Myeloma 收起 << Phase 2 Recruiting September 2020 United States, Georgia ... 展开 >> Grady Memorial Hospital Recruiting Atlanta, Georgia, United States, 30303 Contact: Stephanie McMillan, RN, MSN    404-778-1361    sjmcmil@emory.edu    Emory University/Winship Cancer Institute Recruiting Atlanta, Georgia, United States, 30322 Contact: Jennifer Shipp    404-778-4191    jennifer.shipp@emory.edu    United States, Michigan University of Michigan/Rogel Cancer Center Recruiting Ann Arbor, Michigan, United States, 48109 Contact: Craig Cole, MD       colec@med.umich.edu    United States, Missouri Washington University/Siteman Cancer Center Recruiting Saint Louis, Missouri, United States, 63110 Contact: Ravi Vij, MD       rvij@wustl.edu 收起 <<
NCT02400437 Waldenstrom's Macroglobulinemi... 展开 >>a 收起 << Phase 2 Active, not recruiting September 2021 United States, Massachusetts ... 展开 >> Dana-Farber Cancer Institute Boston, Massachusetts, United States, 02115 收起 <<
NCT02158975 Lymphoma, T-Cell Phase 2 Completed - United States, Michigan ... 展开 >> University of Michigan Hospital Ann Arbor, Michigan, United States, 48109 收起 <<

Ixazomib/艾沙佐米 参考文献

[1]Kupperman E, Lee EC, et al. Evaluation of the proteasome inhibitor MLN9708 in preclinical models of human cancer. Cancer Res. 2010;70(5):1970-80.

[2]Ghobadi A, Rettig MP, et al. Ixazomib, an oral proteasome inhibitor, induces rapid mobilization of hematopoietic progenitor cells in mice. Blood. 2018 Jun 7;131(23):2594-2596.

[3]Liu W, Chen J, et al. Preclinical efficacy and biological effects of the oral proteasome inhibitor ixazomib in diffuse large B-cell lymphoma. Oncotarget. 2017 Aug 21;9(1):346-360.

[4]MLN2238

Ixazomib/艾沙佐米 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.77mL

0.55mL

0.28mL

13.85mL

2.77mL

1.38mL

27.70mL

5.54mL

2.77mL

Ixazomib/艾沙佐米 技术信息

CAS号1072833-77-2
分子式C14H19BCl2N2O4
分子量 361.03
SMILES Code CC(C)C[C@@H](B(O)O)NC(CNC(C1=CC(Cl)=CC=C1Cl)=O)=O
MDL No. MFCD18251438
别名 伊沙佐米(MLN2238) ;MLN2238
运输蓝冰
InChI Key MXAYKZJJDUDWDS-LBPRGKRZSA-N
Pubchem ID 25183872
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, store in freezer, under -20°C
溶解方案

DMSO: 60 mg/mL(166.19 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案 一
方案 二
方案 三

Tags: Ixazomib | 1072833-77-2 | MLN2238 | MLN 2238 | MLN-2238 | Proteasome Inhibitor | Metabolic Enzyme/Protease | Autophagy | Proteasome | Autophagy | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Ixazomib/艾沙佐米 纯度/质量文件 | Ixazomib/艾沙佐米 亚型比较 | Ixazomib/艾沙佐米 生物活性 | Ixazomib/艾沙佐米 动物研究 | Ixazomib/艾沙佐米 临床数据 | Ixazomib/艾沙佐米 参考文献 | Ixazomib/艾沙佐米 实验方案 | Ixazomib/艾沙佐米 技术信息

AmBeed 相关网站 AmBeed.cn AmBeed.com
AmBeed
关于我们
联系我们
资讯中心
网站地图
产品手册
  • 批次文件查询
    • 客户支持
    技术支持
    专业术语
    缩略词释义
    质量手册
    产品咨询
    计算器
    活动政策
    订购方法
    积分商城
    活动声明
    联系我们
    400-920-2911 sales@ambeed.cn tech@ambeed.cn
    AmBeed 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质用途提供服务。

    尊敬的 AmBeed 客户您好，
    请您选择所在区域，我们将转接对应客服为您服务！

    热门区域

    A

    B

    C

    F

    G

    H

    J

    L

    N

    Q

    S

    T

    X

    Y

    Z

    热 A B C F G H J L N Q S T X Y Z