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首页 / 抑制剂/激动剂 / 泛素 / 蛋白酶体 / Ixazomib

艾沙佐米 /Ixazomib {[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 化学结构 CAS号：1072833-77-2
Ixazomib 化学结构
CAS号：1072833-77-2
Ixazomib 3D分子结构
CAS号：1072833-77-2
Ixazomib 化学结构 CAS号：1072833-77-2
Ixazomib 3D分子结构 CAS号：1072833-77-2
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Ixazomib 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:

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产品名称 20S proteasome ↓ Proteasome ↓ 其他靶点 纯度
Ixazomib ++++

20S proteasome, Ki: 0.93 nM

20S proteasome, IC50: 3.4 nM

 		99%+
Delanzomib +++

Chymotrypsin-like proteasome, IC50: 3.8 nM

 		98%
Celastrol +

20S proteasome, IC50: 2.5 μM

 		98%
MLN9708 +++

20S proteasome, Ki: 0.93 nM

20S proteasome, IC50: 3.4 nM

 		99%
Bortezomib ++++

20S proteasome, Ki: 0.6 nM

 		98%
Oprozomib ++

20S proteasome LMP7, IC50: 82 nM

20S proteasome β5, IC50: 36 nM

 		99%+
Epoxomicin ✔ 99%
PI-1840 ++

Chymotrypsin-like proteasome, IC50: 27 nM

 		98%
VR23 +++

Chymotrypsin-like proteasomes, IC50: 3 μM

Trypsin-like proteasomes, IC50: 1 nM

 		98%
Carfilzomib ++

Proteasome, IC50: 5 nM

 		98%
(R)-MG-132 +

Proteasome, IC50: 100 nM

 		98%
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 生物活性

靶点

  • 20S proteasome

    20S proteasome, Ki:0.93 nM

    20S proteasome, IC50:3.4 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 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 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 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 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 技术信息

CAS号1072833-77-2
分子式C14H19BCl2N2O4
分子量 361.029
别名 伊沙佐米(MLN2238) ;MLN2238
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Store in freezer, under -20°C
溶解度

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
动物实验配方

5% DMSO+45% PEG 300+water 17 mg/mL

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 纯度/质量文件 | Ixazomib 亚型比较 | Ixazomib 生物活性 | Ixazomib 动物研究 | Ixazomib 临床数据 | Ixazomib 参考文献 | Ixazomib 实验方案 | Ixazomib 技术信息

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