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蛋白酶
Carfilzomib
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
阿拉丁 | 生产商 | 上海 | 现货 |
产品参数
货号 | CAS号 | 操作 |
---|---|---|
C127870-100mg | 868540-17-4 | 询价 |
C127870-10mg | 868540-17-4 | 询价 |
C127870-25mg | 868540-17-4 | 询价 |
C127870-50mg | 868540-17-4 | 询价 |
C127870-5mg | 868540-17-4 | 询价 |
产品介绍
属性
溶解性 |
|
存贮条件 | 储存温度-20°C |
描述
应用 | Proteasomel抑制剂,epoxomicin的类似物 |
产品介绍 | Carfilzomib (PR-171)是一种不可逆proteasome抑制剂,IC50为<5 nM,在体外优先抑制β5亚基的ChT-L活性,对PGPH和T-L活性很弱或没有作用。 |
备注 | Carfilzomib (PR-171) is an irreversible proteasome inhibitor with IC50 of <5 nM, displayed preferential in vitro inhibitory potency against the ChT-L activity in the β5 subunit, but little or no effect on the PGPH and T-L activities. |
生化机理 | Carfilzomib, an irreversible proteasome inhibitor, has a favorable safety profile and significant anti-tumor activity in patients with relapsed and refractory multiple myeloma (MM). Here we summarize the clinical pharmacokinetics (PK), metabolism, and drug-drug interaction (DDI) profile of carfilzomib. The PK of carfilzomib, infused over 2-10 min, was evaluated in patients with solid tumors or MM. The proteasome has emerged as an important target for cancer therapy with the approval of bortezomib, a first-in-class, reversible proteasome inhibitor, for relapsed/refractory multiple myeloma (MM). Carfilzomib induced a dose- and time-dependent inhibition of proliferation, ultimately leading to apoptosis. Carfilzomib showed increased efficacy compared with bortezomib and was active against bortezomib-resistant MM cell lines and samples from patients with clinical bortezomib resistance. Carfilzomib has entered in a Phase II clinical trial in the treatment of multiple myeloma |
别名 | Proteasomel抑制剂;卡非佐米; (alphaS)-alpha-[(4-吗啉基乙酰基)氨基]苯丁酰基-L-亮氨酰-N-[(1S)-3-甲基-1-[[(2R)-2-甲基环氧乙烷基]羰基]丁基]-L-苯丙氨酰胺;PR 171;PR171;PR-171; (alphaS)-alpha-[(4-Morpholinylacetyl)amino]benzenebutanoyl-L-leucyl-N-[(1S)-3-methyl-1-[[(2R)-2-methyloxiranyl]carbonyl]butyl]-L-phenylalaninamide |
Carfilzomib信息由上海阿拉丁生化科技股份有限公司为您提供,如您想了解更多关于Carfilzomib报价、型号、参数等信息,欢迎来电或留言咨询。
注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途