| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| C408614-1ml |
1ml |
现货  |
|
| 别名 | 卡非佐米（PR-171） |
|---|---|
| 英文别名 | L-Phenylalaninamide, (αS)-α-[[2-(4-morpholinyl)acetyl]amino]benzenebutanoyl-L-leucyl-N-[(1S)-3-methyl-1-[[(2R)-2-methyl-2-oxiranyl]carbonyl]butyl]- |
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Carfilzomib (PR-171) |
| 生化机理 | Carfilzomib（PR-171）是一种不可逆的蛋白酶体抑制剂，在ANBL-6细胞中的IC50小于5 nM，在体外对β5亚基的ChT-L活性有优先抑制效力，但对PGPH和T-L活性几乎没有影响。卡非佐米能激活前生存自噬并诱导细胞凋亡。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 26S 蛋白质体抑制剂 |
| 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。Proteasomel抑制剂,epoxomicin的类似物 Information Carfilzomib (PR-171) is an irreversibleproteasomeinhibitor withIC50of <5 nM in ANBL-6 cells, 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. Carfilzom Carfilzomib inhibits proliferation in a variety of cell lines and patient-derived neoplastic cells, including multiple myeloma, and induced intrinsic and extrinsic apoptotic signaling pathways and activation of c-Jun-N-terminal kinase (JNK). Carfilzomib reveals enhanced anti-MM activity compared with bortezomib, overcome resistance to bortezomib and other agents, and acts synergistically with dexamethasone (Dex). Carfilzomib shoes preferential in vitro inhibitory potency against the ChT-L activity in the β5 subunit, with over 80% inhibition at doses of 10 nM. Short exposure to low-dose Carfilzomib leads to preferential binding specificity for the β5 constitutive 20S proteasome and the β5i immunoproteasome subunits. Measurement of caspase activity in ANBL-6 cells pulsed with Carfilzomib reveals substantial increases in caspase-8, caspase-9, and caspase-3 activity after 8 hours, giving a 3.2-, 3.9- and 6.9-fold increase, respectively, over control cells after 8 hours. In carfilzomib pulse-treated cells, the mitochondrial membrane integrity is decreased to 41% (Q1 + Q2), compared with 75% in vehicle-treated control cells. In another study, Carfilzomib has also shown preclinical effectiveness against hematological and solid malignancies. Carfilzomib directly inhibits osteoclasts formation and bone resorption. In vivo Carfilzomib moderately reduces tumor growth in an in vivo xenograft model. Carfilzomib effectively decreases multiple myeloma cell viability following continual or transient treatment mimicking. Carfilzomib increases trabecular bone volume, decreases bone resorption and enhances bone formation in non-tumor bearing mice. cell lines： Concentrations：100 nM Incubation Time：1 hour Powder Purity:≥98% |
| 分子类型 | 蛋白质 |
|---|---|
| Canonical SMILES | CC(C)CC(NC(=O)C(CCC1=CC=CC=C1)NC(=O)CN2CCOCC2)C(=O)NC(CC3=CC=CC=C3)C(=O)NC(CC(C)C)C(=O)C4(C)CO4 |
| 分子量 | 719.91 |
| 溶解性 | Solubility (25°C) In vitro Ethanol: mg/mL |
|---|
| Concentration | |
|---|---|
| Proton NMR spectrum | Conforms to Structure |
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