| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| T408173-1ml |
1ml |
现货  |
|
| 英文别名 | (S)-cyclopentyl 2-((R)-2-((S)-1-hydroxy-2-(hydroxyamino)-2-oxoethyl)-4-methylpentanamido)-2-phenylacetate |
|---|---|
| 规格或纯度 | 10mM in DMSO |
| 英文名称 | Tosedostat (CHR2797) |
| 生化机理 | Tosedostat (CHR2797) 是一种氨肽酶抑制剂，对 LAP、PuSA 和氨肽酶 N 的 IC50 分别为 100 nM、150 nM 和 220 nM，对 PILSAP、MetAP-2、LTA4 水解酶或 MetAP-2 均无有效抑制作用。第 2 阶段 |
| 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 | 氨基肽酶抑制剂 |
| 产品介绍 |
Tosedostat (CHR-2797) 是一种氨基肽酶 (aminopeptidase) 抑制剂。CHR-2797 对多种肿瘤细胞系均具有抗增殖作用。作用于LAP， PuSA和Aminopeptidase N时，IC50分别为100 nM， 150 nM 和220 nM，不能有效抑制PILSAP， MetAP-2， LTA4水解酶，和MetAP-2。 Information Tosedostat (CHR2797) Tosedostat (CHR2797) is an aminopeptidase inhibitor for LAP , PuSA and Aminopeptidase N with IC50 of 100 nM, 150 nM and 220 nM, respectively, and does not effectively inhibit either PILSAP, MetAP-2, LTA4 hydrolase, or MetAP-2. Phase CHR-2797 has almost no effect on Aminopeptidase B, PILSAP, LTA4 hydrolase and MetAP-2 activity with IC50 values of >1 uM, >5 uM, >10 uM and >30 uM, respectively. CHR-2797 is converted into a pharmacologically active acid product (CHR-79888) inside cells, which shows significant inhibitory activity towards LTA4 hydrolase with IC50 of 8 nM. CHR-2797 exhibits profound anti-proliferative effects against a range of cancer cell lines such as U-937, HL-60, KG-1 and GDM-1 with IC50 values of 10 nM, 30 nM, 15 nM and 15 nM, respectively, but is inactive against HuT 78 and Jurkat E6-1 with IC50 values of >10 uM. There is no obvious correlation between sensitivity to CHR-2797 and the mutational status of p53, PTEN, or K-Ras in cells. CHR-2797 shows selectivity for transformed cells (MrC5-SV2 or K-ras NRK) over non-transformed cells (MrC5 or NRK). CHR-2797 (6 μM) treatment leads to the up-regulation of genes involved in amino acid transport and metabolic pathways, the phosphorylation of eukaryotic initiation factor 2α, the inhibition of phosphorylation of mTOR substrates and reduced protein synthesis in HL-60 cells. In vivo Administration of CHR-2797 (~100 mg/kg) decreases tumor volumes in vivo, compared to controls, in a dose-response manner in the rat HOSP.1 lung colonisation model, the rat HSN LV10 chondrosarcoma liver colonisation model, the human MDA-MB-435 breast cancer spontaneous metastasis model, and the human MDA-MB-468 cell xenograft model. cell lines： Concentrations：Dissolved in DMSO, final concentration ~1 mM Incubation Time：72 hours Powder Purity:≥95% |
| 分子类型 | 小分子 |
|---|---|
| 分子量 | 406.47 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 100 mg/mL (127.39 mM); |
|---|
| Concentration | 9-11（mmol/L） |
|---|---|
| Proton NMR spectrum | Conforms to Structure |
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