Ixazomib (MLN2238)

中文名称:伊沙佐米

Ixazomib (MLN2238)抑制20S proteasome的糜蛋白酶样蛋白水解(β5)位点,无细胞试验中IC50Ki分别为3.4 nM和0.93 nM,也抑制胱天蛋白酶样(β1)和胰蛋白酶样(β2)蛋白水解位点,IC50分别为31和3500 nM。Ixazomib (MLN2238)可诱导自噬。Phase 3。

Ixazomib (MLN2238) Chemical Structure

Ixazomib (MLN2238) Chemical Structure

CAS: 1072833-77-2

规格 价格 库存 购买数量
10mM (1mL in DMSO) 2047.74 现货
5mg 1390.99 现货
10mg 2601.18 现货
50mg 7944.55 现货
1g 57248.1 现货
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Ixazomib (MLN2238)相关产品

相关信号通路图

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
HEK293 Function assay 1 hr Inhibition of NFkappaB in HEK293 cells incubated for 1 hr prior to TNF-alpha challenge measured after 3 hrs by luciferase reporter gene assay relative to control, IC50 = 0.0062 μM. ChEMBL
Calu6 Function assay 1 hr Inhibition of 26S proteasome beta5 subunit in human Calu6 cells using Suc-LLVY-aminoluciferin as substrate after 1hr by luminescence assay, IC50 = 0.009 μM. ChEMBL
Calu6 Cytotoxicity assay 72 hrs Cytotoxicity against human Calu6 cells after 72 hrs by luminescence assay, LC50 = 0.014 μM. ChEMBL
U266B1 Cytotoxicity assay 72 hrs Cytotoxicity against human U266B1 cells assessed as reduction in cell viability after 72 hrs by CellTiter 96 aqueous one solution assay, IC50 = 0.05215 μM. 29934218
RPMI8226 Cytotoxicity assay 72 hrs Cytotoxicity against human RPMI8226 cells assessed as reduction in cell viability after 72 hrs by CellTiter 96 aqueous one solution assay, IC50 = 0.05532 μM. 29934218
ARH77 Cytotoxicity assay 72 hrs Cytotoxicity against human ARH77 cells assessed as reduction in cell viability after 72 hrs by CellTiter 96 aqueous one solution assay, IC50 = 0.0655 μM. 29934218
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells 29435139
fibroblast cells qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells 29435139
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生物活性

产品描述 Ixazomib (MLN2238)抑制20S proteasome的糜蛋白酶样蛋白水解(β5)位点,无细胞试验中IC50Ki分别为3.4 nM和0.93 nM,也抑制胱天蛋白酶样(β1)和胰蛋白酶样(β2)蛋白水解位点,IC50分别为31和3500 nM。Ixazomib (MLN2238)可诱导自噬。Phase 3。
特性 MLN2238是一流的蛋白酶抑制剂,在临床前期研究中,提高药物动力学活性,药效,及抗癌活性。
靶点
20S proteasome [1]
(Cell-free assay)
20S proteasome [1]
(Cell-free assay)
0.93 nM(Ki) 3.4 nM
体外研究(In Vitro)
体外研究活性 MLN2238是氮端加帽的二肽亮氨酸硼酸,抑制20S 蛋白酶体的糜蛋白酶类(β5)水解位点,IC50为3.4 nM,Ki值为0.93 nM。更高浓度时, MLN2238也抑制20S蛋白酶体的caspase类水解 (β1)位点和胰蛋白酶类水解(β2)位点,IC50分别为31 nM和3.5 µM。MLN2238是蛋白酶体的有效选择性可逆抑制剂,这种可逆性存在时间依赖性。MLN2238抑制Calu-6细胞,IC50为9.7 nM。MLN2238作用于肿瘤细胞,为蛋白酶体的有效选择性可逆抑制剂。MLN2238和Bortezomib都为蛋白酶体的可逆抑制剂,都存在时间依赖性,但是MLN2238作用于蛋白酶体的分离半衰期比Bortezomib作用快6倍 (分别为18和110分钟)。MLN2238从蛋白酶体中分离比Bortezomib快, 与Proteasome-Glo 实验中蛋白酶体活性更快恢复一致。 MLN2238 比Bortezomib具有更高的肿瘤药效。[1] MLN2238是MLN9708的生物活性形式。[2]
激酶实验 激酶实验
Calu-6细胞培养在含10%FBS和1%青霉素/链霉素的MEM培养基中,1天后,按每孔1×104个细胞加到384孔板上。加入荧光酶素和 Proteasome-Glo检测试剂,观察糜蛋白酶类底物Suc-LLVY-aminoluciferin的水解,测定蛋白酶体活性。使用LEADseeker设备测定荧光值。
细胞实验 细胞系 Calu-6 细胞
浓度 10nM 左右
孵育时间 1小时或30分钟
方法 Calu-6细胞培养在含10%FBS和1%青霉素/链霉素的MEM培养基中,1天后,按每孔1×104个细胞加到384孔板上。为了测定IC50值,用溶于DMSO (0.5%, v/v)的不同浓度bortezomib或MLN2238在37oC下处理细胞1小时。用于可逆性实验,用1 μmol/L bortezomib 或MLN2238在37oC下处理细胞30分钟,然后在培养基中洗三次洗去bortezomib或MLN2238。细胞在37oC下再温育4小时,然后移除培养基换上新的培养基。
实验图片 检测方法 检测指标 实验图片 PMID
Western blot PARP / Cleaved PARP / Caspase-3 / Cleaved Caspase-3 Mcl-1 / Bcl-2 p53 / p21 / NOXA / PUMA / pRb / E2F / Cyclin D1 / CDK6 27687684
Growth inhibition assay IC50 29416618
体内研究(In Vivo)
体内研究活性 MLN2238作用于移植瘤时,比bortezomib产生更强的药效反应。与bortezomib相比,作用于移植瘤时,MLN2238显示更高的最大值和持久的抑制肿瘤蛋白酶效果。说明用MLN2238处理的肿瘤,药效反应得到明显提高。MLN2238作用于CWR22移植瘤显示抗癌活性。与bortezomib 相比,作用于WSU-DLCL2移植瘤模型,MLN2238显示更强的肿瘤药效反应。[1] 另外,作用于OCI-Ly10和PHTX22L模型,MLN2238比 bortezomib具有更高的药效和抗癌活性。[2]
动物实验 Animal Models 皮下注射5.0×106个MM.1S细胞的CB-17 SCID鼠
Dosages 11 mg/kg
Administration 静脉注射,每周两次,持续三周
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00963820 Completed
Multiple Myeloma
Millennium Pharmaceuticals Inc.|Takeda
October 2009 Phase 1

化学信息&溶解度

分子量 361.03 分子式

C14H19BCl2N2O4

CAS号 1072833-77-2 SDF Download Ixazomib (MLN2238) SDF
Smiles B(C(CC(C)C)NC(=O)CNC(=O)C1=C(C=CC(=C1)Cl)Cl)(O)O
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 72 mg/mL ( (199.42 mM) ;DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Ethanol : 72 mg/mL (199.42 mM)

Water : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

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