Ixazomib
作者：齐岳
发布时间：2023-09-11
09:25:42
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产品名称：Ixazomib
产品描述：
| 产品描述 | MLN2238, a second generation, boron-containing peptide proteasome inhibitor (PI), inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome (IC50/Ki: 3.4/0.93 nM, in cell-free assays), also inhibits the caspase-like (β1) and trypsin-like (β2) proteolytic sites (IC50: 31/3500 nM). |
| 靶点活性 | caspase-like (β1):31nM, 20S proteasome:3.4 nM, trypsin-like (β2):3500 nM, 20S proteasome:0.93 nM(Ki) |
| 体外活性 | MLN2238对CWR22移植瘤具有抗癌活性.在WSU-DLCL2移植瘤模型中,MLN2238的肿瘤药效反应比bortezomib更强. 此外,在OCI-Ly10和PHTX22L模型中,MLN2238比 bortezomib具有更高的药效和抗癌活性.作用于移植瘤时,MLN2238的药效反应比bortezomib更较强,且其最大值更高,对肿瘤蛋白酶的抑制效果更持久. |
| 体内活性 | MLN2238是MLN9708的生物活性代谢物。MLN2238和Bortezomib均为时间依赖性的蛋白酶体可逆抑制剂,但与Bortezomib(110分钟)相比,MLN2238（18分钟）作用于蛋白酶体的分离半衰期要快6倍。MLN2238的肿瘤药效 要高于Bortezomib。MLN2238是氮端加帽的二肽亮氨酸硼酸,对20S 蛋白酶体中糜蛋白酶类的水解位点有抑制作用（IC50/Ki：3.4/0.93 nM）。更高浓度时,MLN2238对20S蛋白酶体的caspase类水解位点（IC50：31 nM）和胰蛋白酶类水解位点（IC50：3.5 μM）也有抑制作用。MLN2238抑制Calu-6细胞（IC50：9.7 nM）。 |
| 激酶实验 | Kinase assay : Calu-6 cells are cultured in MEM containing 10% fetal bovine serum and 1% penicillin/streptomycin and plated 1 day before the start of the experiment at 1 × 104 cells per well in a 384-well plate. Proteasome activity is assessed by monitoring hydrolysis of the chymotrypsin-like substrate Suc-LLVY-aminoluciferin in the presence of luciferase using the Proteasome-Glo assay reagents according to the manufacturer's instructions. Luminescence is measured using a LEADseeker instrument. |
| 细胞实验 | Calu-6 cells are cultured in MEM containing 10% FBS and 1% penicillin/streptomycin and plated 1 day before the start of the experiment at 1 × 104 cells per well in a 384-well plate. For IC50 determinations, cells are treated with varying concentrations of Bortezomib or MLN2238 in DMSO (0.5% final, v/v) for 1 hour at 37 °C. For reversibility experiments, cells are treated with either 1 μM Bortezomib or MLN2238 for 30 minutes at 37 °C and then washed thrice in medium to remove the Bortezomib or MLN2238. Cells are incubated for an additional 4 hours at 37 °C, after which the medium is removed and replaced with fresh medium. (Only for Reference) |
| 别名 | 艾沙佐米, MLN2238 |
| 分子量 | 361.03 |
| 分子式 | C14H19BCl2N2O4 |
| CAS No. | 1072833-77-2 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 67 mg/mL (185.6 mM)
Ethanol: 9 mg/mL (24.92 mM)
H2O: <1 mg/mL
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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公司介绍：
西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
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