100286-90-6
基本信息
伊立替康
盐酸伊立替康
盐酸依立替康
CAMPTOTHECIN 11 HYDROCHLORIDE
CAMPTOTHECIN 11 HYDROCHLORIDE,TOPOTECIN
CPT-11
IRINOTECAN HCL
IRINOTECAN HYDROCHLORIDE
(S)-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
TOPOTECIN HYDROCHLORIDE
(1,4’-bipiperidine)-1’-carboxylicacid,3,4,12,14-tetrahydro-4,11-diethyl-4-hyd
(s)-ydrochlorid
7-ethyl-10-(4-(1-piperidino)-1-piperidino)carbonyloxycamptothecinhydrochlor
campto
roxy-3,4-dioxo-1h-pyrano(3’,4’:6,7)indolizino(1,2-b)quinolin-9-ylester,monoh
topotecin
u10144oe
[1,4Bipiperidine]-1carboxylic acid (S)-4,11-diethyl-3,4,12,14-tetrahydro-4-hydroxy-3,14-dioxo-1H-pyrano[346,7]indolizino[1,2-b]quinolin-9-yl ester, Hcl Trihydrate
[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, monohydrochloride (9CI)
[1,4'-Bipiperidine]-1'-carboxylic acid, 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, monohydrochloride, (S)-
7-Ethyl-10-[[4-(1-piperidyl)-1-piperidyl]carbonyloxy]camptothecin hydrochloride
Camptothecin 11
物理化学性质
| 外观 | 淡黄色粉末或淡黄色结晶性粉末，无臭,在水、乙醇或氯仿中微溶，在丙酮中不溶。 |
| 熔点 | 250-256°C (dec.) |
| 沸点 | 257 °C |
| 折射率 | 67.7 ° (C=1, H2O) |
| 储存条件 | 2-8°C |
| 储存条件 | Refrigerator |
| 溶解度 | Soluble in DMSO or DMF at approximately 20mg/ml. Sparingly soluble in aqueous buffers. /n |
| 储藏 | 真空密封、避光、低温保存。 |
| 形态 | 黄色粉末 |
| 颜色 | White to yellow |
| 生物来源 | plant (Fructus camptothecae) |
| 水溶解性 | Soluble in DMSO at 100mg/ml. Soluble in water at 25mg/ml with warming |
| Merck | 5091 |
| InChIKey | GURKHSYORGJETM-GCUJQDEHNA-N |
| SMILES | C(C1C2=CC(OC(N3CCC(N4CCCCC4)CC3)=O)=CC=C2N=C2C3=CC4[C@@](C(=O)OCC=4C(=O)N3CC=12)(O)CC)C.Cl |&1:28,r| |
| CAS 数据库 | 100286-90-6(CAS DataBase Reference) |
安全数据
| 危险性符号(GHS) |  GHS07 |
| 警示词 | 警告 |
| 危险性描述 | H302 |
| 防范说明 | P264-P270-P301+P312a-P330-P501a |
| 危险品标志 | Xn |
| 危险类别码 | 22 |
| WGK Germany | 3 |
| RTECS号 | DW1060750 |
| 海关编码 | 29399990 |
| 存储类别 | 11 - Combustible Solids |
| 危险性类别 | Acute Tox. 4 Oral |
制备方法
4897-50-1
86639-52-3
100286-90-6
一般步骤：将(S)-4,11-二乙基-4,9-二羟基-1H-吡喃并[3',4':6,7]吲哚嗪并[1,2-b]喹啉-3,14(4H,12H)-二酮（4.5g）和吡啶（60ml）加入反应容器中。在30-40℃下缓慢滴加[1,4'-联哌啶基]-1'-碳酰氯盐酸盐（3.44g）和三乙胺（4.8ml）溶于75ml二氯甲烷的溶液。维持反应温度在30-40℃，持续搅拌1.5小时。随后加入4-哌啶基哌啶（0.58g），继续搅拌0.5小时。通过减压蒸馏去除二氯甲烷和吡啶，直至反应混合物体积浓缩至约25ml。加入乙腈（100ml），将混合物加热至60℃并保持一段时间。待混合物冷却至室温后，缓慢加入15ml 5％盐酸水溶液。室温下搅拌反应混合物约20小时。将混合物冷却至0±5℃，过滤收集析出的结晶产物，依次用乙腈:水（10:1，10ml）和乙腈（10ml）洗涤。最后，将产物在减压条件下干燥，得到目标化合物(S)-4,11-二乙基-4-羟基-3,14-二氧代-3,4,12,14-四氢-1H-吡喃并[3',4';6,7]吲哚并[1,2-b]喹啉-9-基[1,4'-联哌啶]-1'-羧酸盐酸盐6.4克，收率90%。
参考文献：
[1] Patent: WO2006/84940, 2006, A1. Location in patent: Page/Page column 5-6
常见问题列表
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Topoisomerase I
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Irinotecan hydrochloride is a topoisomerase I inhibitor. Irinotecan inhibits the growth of LoVo and HT-29 cells, with IC 50 s of 15.8 ± 5.1 and 5.17 ± 1.4 μM, respectively, and induces similar amounts of cleavable complexes in both in LoVo and HT-29 cells. Irinotecan suppresses the proliferation of human umbilical vein endothelial cells (HUVEC), with an IC 50 of 1.3 μM.
Irinotecan (CPT-11, 5 mg/kg) significantly inhibits the growth of tumors by intratumoral injection daily for 5 days, on two consecutive weeks in rats, and such effects also occur via continuous intraperitoneal infusion by osmotic minipump into mice. However, Irinotecan (10 mg/kg) shows no effect on the growth of tumor by i.p. Irinotecan (CPT-11, 100-300 mg/kg, i.p.) apparently suppresses tumor growth of HT-29 xenografts in athymic female mice by day 21. The two groups of Irinotecan (125 mg/kg) plus TSP-1 (10 mg/kg per day) or Irinotecan (150 mg/kg) in combination TSP-1 (20 mg/kg per day) are nearly equally effective and inhibit tumor growth 84% and 89%, respectively, and both are more effective than Irinotecan alone at doses of 250 and 300 mg/kg.
知名试剂公司产品信息
盐酸伊立替康价格(试剂级)
| 报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
| 2025/12/22 | HY-16562A | 盐酸伊立替康 Irinotecan hydrochloride | 100286-90-6 | 10 mg | 291元 |
| 2025/12/22 | HY-16562A | 盐酸伊立替康 Irinotecan hydrochloride | 100286-90-6 | 10mM * 1mLin DMSO | 320元 |
| 2025/12/22 | HY-16562A | 盐酸伊立替康 Irinotecan hydrochloride | 100286-90-6 | 25 mg | 465元 |