Ixazomib
作者：齊岳
發(fā)布時(shí)間：2023-09-11
09:25:42
點(diǎn)擊數(shù)：
產(chǎn)品名稱：Ixazomib
產(chǎn)品描述：
| 產(chǎn)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). |
| 靶點(diǎn)活性 | caspase-like (β1):31nM, 20S proteasome:3.4 nM, trypsin-like (β2):3500 nM, 20S proteasome:0.93 nM(Ki) |
| 體外活性 | MLN2238對(duì)CWR22移植瘤具有抗*活性.在WSU-DLCL2移植瘤模型中,MLN2238的藥效反應(yīng)比bortezomib更強(qiáng). 此外,在OCI-Ly10和PHTX22L模型中,MLN2238比 bortezomib具有更高的藥效和抗*活性.作用于移植瘤時(shí),MLN2238的藥效反應(yīng)比bortezomib更較強(qiáng),且其大值更高,對(duì)蛋白酶的抑制效果更持久. |
| 體內(nèi)活性 | MLN2238是MLN9708的生物活性代謝物。MLN2238和Bortezomib均為時(shí)間依賴性的蛋白酶體可逆抑制劑,但與Bortezomib(110分鐘)相比,MLN2238（18分鐘）作用于蛋白酶體的分離半衰期要快6倍。MLN2238的藥效 要高于Bortezomib。MLN2238是氮端加帽的二肽亮氨酸硼酸,對(duì)20S 蛋白酶體中糜蛋白酶類的水解位點(diǎn)有抑制作用（IC50/Ki：3.4/0.93 nM）。更高濃度時(shí),MLN2238對(duì)20S蛋白酶體的caspase類水解位點(diǎn)（IC50：31 nM）和胰蛋白酶類水解位點(diǎn)（IC50：3.5 μM）也有抑制作用。MLN2238抑制Calu-6細(xì)胞（IC50：9.7 nM）。 |
| 激酶實(shí)驗(yàn) | 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. |
| 細(xì)胞實(shí)驗(yàn) | 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) |
| 別名 | 艾沙佐米, MLN2238 |
| 分子量 | 361.03 |
| 分子式 | C14H19BCl2N2O4 |
| CAS No. | 1072833-77-2 |
存儲(chǔ)
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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