| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| I408334-1ml |
1ml |
现货  |
|
| 英文别名 | [1,4'-Bipiperidine]-1'-carboxylic acid, (4S)-4,11-diethyl-3,4,12,14-tetrahydro-4-hydroxy-3,14-dioxo-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinolin-9-yl ester, hydrochloride, hydrate (1:1:3) |
|---|---|
| 规格或纯度 | 10mM in DMSO |
| 英文名称 | Irinotecan (CPT-11) HCl Trihydrate |
| 生化机理 | 伊立替康（CPT-11）通过抑制拓扑异构酶 1 防止 DNA 解旋。 |
| 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 | DNA 拓扑异构酶 I 抑制剂 |
| 产品介绍 |
Irinotecan HCl Trihydrate通过抑制Topoisomerase 1（拓扑异构酶1）而防止DNA解链。An inhibitor of Topo I. Information Irinotecan (CPT-11) prevents DNA from unwinding by inhibition oftopoisomerase 1. Irinotecan is activated to SN-38 by carboxylesterases to become able to interact with its target, topoisomerase I. Irinotecan induces similar amounts of cleavable complexes at its IC50 in LoVo cells and HT-29 cell lines. SN-38 induces a concentration-dependent formation of cleavable complexes, which is not significantly different in LoVo cells and HT-29 cell lines. Cell accumulation of Irinotecan is markedly different, reaching consistently higher levels in HT-29 cells than in LoVo cells. The lactone E-ring of Irinotecan and SN-38 hydrolyses reversibly in aqueous solutions, and the interconversion between the lactone and carboxylate forms is dependent on pH and temperature. Liver is primarily responsible for the activation of Irinotecan to SN-38. At equal concentrations of Irinotecan and SN-38 glucuronide, the rate of beta-glucuronidase-mediated SN-38 production is higher than that formed from Irinotecan in both tumour and normal tissue. Irinotecan is also converted to SN-38 in intestines, plasma and tumor tissues. Irinotecan is significantly more active in SCLC than in NSCLC cell lines, whereas no significant difference between histological types is observed with SN-38. In vivo In COLO 320 xenografts, Irinotecan induces a maximum growth inhibition of 92%. A single dose of Irinotecan significantly increases amounts of topoisomerase I covalently bound to DNA in stomach, duodenum, colon and liver. Concomitantly, the Irinotecan-treated group shows significantly higher amounts of DNA strand breaks in colon mucosa cells compared to the control group. cell lines： Concentrations：0 μM -100 μM Incubation Time：48 hours Powder Purity:≥99% |
| Isomeric SMILES | CCC1=C2CN3C(=CC4=C(C3=O)COC(=O)[C@@]4(CC)O)C2=NC5=C1C=C(C=C5)OC(=O)N6CCC(CC6)N7CCCCC7.O.O.O.Cl |
|---|---|
| PubChem CID | 60837 |
| 分子量 | 677.18 |
| Reaxy-Rn | 4838283 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 71 mg/mL (200.63 mM); Water: 16 mg/mL (45.21 mM); Ethanol: 15 mg/mL (42.38 mM); |
|---|---|
| 比旋光度 | 24° (C=1,MeOH) |
| 沸点 | 257°C |
| 象形图 | GHS08, GHS07 |
|---|---|
| 信号词 | Danger |
| 危险声明 |
H341: 怀疑引起遗传缺陷 H302: 吞食有害 H360: 可能损害生育力或未出生的孩子 |
| 预防措施声明 |
P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P405: 密闭存放 P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P281: 根据需要使用个人防护设备。 P270: 使用本产品时，请勿进食、饮水或吸烟。 P330: 漱口 P203: 使用前，获取、阅读并遵守所有安全说明。 P301+P317: 如果被吞咽：请寻求医疗帮助。 P318: 如果暴露或担心，请就医。 |
| RTECS | DW1060750 |
| Merck Index | 5091 |
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