Irinotecan HCl Trihydrate
(Synonyms: 盐酸伊立替康三水合物; (+)-Irinotecan hydrochloride trihydrate; CPT-11 hydrochloride trihydrate) 目录号 : GC11048
A potent inhibitor of DNA topoisomerase I
Cas No.:136572-09-3
Sample solution is provided at 25 µL, 10mM.
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Irinotecan HCl Trihydrate (CPT-11) is a semisynthetic derivative of camptothecin with IC50 value of 3.4μM in P388 leukemia [1].
CPT-11 is synthesized to avoid toxicity and to improve therapeutic efficacy of camptothecin. It has been approved by FDA for the treatment of patients with metastatic carcinoma of the colon or rectum whose disease has recurred or progressed following 5-fluorouracil-based therapy. CPT-11 is a soluble prodrug of SN-38, it is converted into SN-38 by carboxylesterase enzymes in vivo. SN-38 is a potent inhibitor of topoisomerase I [2].
CPT-11 is found to have efficacy against drug-resistant as well as drug-sensitive tumor cells. It inhibits the growth of the tumors which are VCR- resistant or ADM-resistant. The inhibition can also occur in VCR- and ADM-resistant tumor bearing mice [1].
References:
[1] Tsuruo T, Matsuzaki T, Matsushita M, Saito H, Yokokura T. Antitumor effect of CPT-11, a new derivative of camptothecin, against pleiotropic drug-resistant tumors in vitro and in vivo. Cancer Chemother Pharmacol. 1988;21(1):71-4.
[2] Slatter JG, Schaaf LJ, Sams JP, Feenstra KL, Johnson MG, Bombardt PA, Cathcart KS, Verburg MT, Pearson LK, Compton LD, Miller LL, Baker DS, Pesheck CV, Lord RS 3rd. Pharmacokinetics, metabolism, and excretion of irinotecan (CPT-11) following I.V. infusion of [(14)C]CPT-11 in cancer patients. Drug Metab Dispos. 2000 Apr;28(4):423-33.
Cell experiment: | Exponentially growing cells are seeded in 20 cm2 dishes with an optimal cell number for each cell line (20,000 for LoVo cells, 100,000 for HT-29 cells). They are treated 2 days later with increasing concentrations of irinotecan or SN-38 for one cell doubling time (24 h for LoVo cells, 40 h for HT-29 cells). After washing with 0.15 M NaCl, the cells are further grown for two doubling times in normal medium, detached from the support with trypsin-EDTA and counted in a hemocytometer. The IC50 values are then estimated as the drug concentrations responsible for 50% growth inhibition as compared with cells incubated without drug[2]. |
Animal experiment: | Irinotecan has been administered by intratumoral injection at 0.1 cc volume of the appropriate solution, for a doses of 5 mg/kg daily for 5 days, on two consecutive weeks, followed by a 7-days rest period, referred to as one cycle of therapy. Rats receive three cycles over a period of 8 weeks. Control animals receive 0.1 cc of sterile 0.9% sodium chloride solution by intratumoral injection in the same rule of administration as that of animals of group II[1]. |
References: [1]. Morales C, et al. Antitumoral effect of irinotecan (CPT-11) on an experimental model of malignant neuroectodermal tumor. J Neurooncol. 2002 Feb;56(3):219-26. | |
| Cas No. | 136572-09-3 | SDF | |
| 别名 | 盐酸伊立替康三水合物; (+)-Irinotecan hydrochloride trihydrate; CPT-11 hydrochloride trihydrate | ||
| 化学名 | (S)-4,11-diethyl-4-hydroxy-3,14-dioxo-3,4,12,14-tetrahydro-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinolin-9-yl [1,4'-bipiperidine]-1'-carboxylate hydrochloride trihydrate | ||
| Canonical SMILES | O=C(N1CCC(CC1)N2CCCCC2)OC3=CC4=C(CC)C5=C(C(N6C5)=CC(C7(CC)O)=C(COC7=O)C6=O)N=C4C=C3.Cl.O.O.O | ||
| 分子式 | C33H45ClN4O9 | 分子量 | 677.18 |
| 溶解度 | ≥ 23.1mg/mL in DMSO, ≥ 2.5mg/mL in Water | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.4767 mL | 7.3836 mL | 14.7671 mL |
| 5 mM | 0.2953 mL | 1.4767 mL | 2.9534 mL |
| 10 mM | 0.1477 mL | 0.7384 mL | 1.4767 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet