9-amino Camptothecin是一种强效、不溶于水且具有抗肿瘤活性的拓扑异构酶I抑制剂。
Cas No.:91421-43-1
Sample solution is provided at 25 µL, 10mM.
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9-amino Camptothecin is a potent, water-insoluble topoisomerase I inhibitor with antitumor activity[1]. Topoisomerase I regulates DNA topology through a relaxation-annealing mechanism and participates in key nuclear processes such as DNA replication, transcription, and repair without requiring ATP[2]. 9-amino Camptothecin induces apoptosis and DNA damage and is commonly used in the treatment and research of ovarian cancer, lymphoma, and colorectal cancer[3,4,5].
In vitro, treatment of human breast cancer MCF-7, bladder cancer MGH-U1, and colon cancer HT-29 cells with 9-amino Camptothecin (0.27-274nM) for 4-240h resulted in cytotoxicity that increased with both drug concentration and exposure time. Following treatment with 9-amino Camptothecin (137nM) for 24h, all MCF-7, MGH-U1, and HT-29 cells exhibited S-phase accumulation[6]. Treatment of human prostate cancer PC-3, PC-3M, LNCaP, and DU145 cell lines with 9-amino Camptothecin (1-500nM) for 96h inhibited cell viability in a time- and concentration-dependent manner, with IC50 values of 34.1nM, 10nM, 8.9nM, and 6.5nM, respectively[7].
In vivo, 9-amino Camptothecin (0.35, 0.75, and 1mg/kg/day; 5 days/week; 3 weeks) was administered by oral gavage to nude mice bearing PC-3 xenografts. The 0.35mg/kg/day dose completely inhibited tumor growth, while the 0.75 and 1mg/kg/day doses both resulted in tumor volume reduction[7].
References:
[1] TANIZAWA A, FUJIMORI A, FUJIMORI Y, et al. Comparison of topoisomerase I inhibition, DNA damage, and cytotoxicity of camptothecin derivatives presently in clinical trials[J]. Journal of the National Cancer Institute, 1994, 86(11): 836-842.
[2] POMMIER Y, POURQUIER P, FAN Y I, et al. Mechanism of action of eukaryotic DNA topoisomerase I and drugs targeted to the enzyme[J]. Biochimica et Biophysica Acta (BBA)-Gene Structure and Expression, 1998, 1400(1-3): 83-106.
[3] HUANG G E, WANG H, YANG L X. Enhancement of radiation-induced DNA damage and inhibition of its repair by a novel camptothecin analog[J]. Anticancer Research, 2010, 30(3): 937-944.
[4] TAKIMOTO C H, THOMAS R. The clinical development of 9-aminocamptothecin[J]. Annals of the New York Academy of Sciences, 2000, 922(1): 224-236.
[5] HOCHSTER H, PLIMACK E R, RUNOWICZ C D, et al. Biweekly 72-hour 9-aminocamptothecin infusion as second-line therapy for ovarian carcinoma: phase II study of the New York Gynecologic Oncology Group and the Eastern Cooperative Oncology Group[J]. Journal of Clinical Oncology, 2004, 22(1): 120-126.
[6] LI M L, HORN L, FIRBY P S, et al. Pharmacological determinants of 9-aminocamptothecin cytotoxicity[J]. Clinical Cancer Research, 2001, 7(1): 168-174.
[7] DE SOUZA P L, COOPER M R, IMONDI A R, et al. 9-Aminocamptothecin: a topoisomerase I inhibitor with preclinical activity in prostate cancer[J]. Clinical cancer research: an official journal of the American Association for Cancer Research, 1997, 3(2): 287-294.
9-amino Camptothecin是一种强效、不溶于水且具有抗肿瘤活性的拓扑异构酶I抑制剂[1]。拓扑异构酶I通过松弛-退火机制调节DNA拓扑结构，无需ATP即可参与DNA复制、转录和修复等关键核内过程[2]。9-amino Camptothecin能诱导细胞凋亡和DNA损伤，通常用于卵巢癌、淋巴癌和结直肠癌的治疗和研究[3,4,5]。
在体外，9-amino Camptothecin（0.27-274nM）处理人乳腺癌MCF-7、膀胱癌MGH-U1和结肠癌HT-29细胞4-240h，细胞毒性随药物浓度和暴露时间的增加而增强。9-amino Camptothecin（137nM）处理MCF-7、MGH-U1和HT-29细胞24h，所有细胞均出现S期积累[6]。9-amino Camptothecin（1-500nM） 处理人前列腺癌 PC-3、PC-3M、LNCaP和DU145细胞系96 h，细胞活力呈时间和浓度依赖性抑制，IC50值分别为 34.1nM、10nM、8.9nM 和6.5nM[7]。
在体内，9-amino Camptothecin（0.35, 0.75, and 1mg/kg/day; 5 days/week; 3 weeks）通过口服灌胃治疗携带PC-3异种移植瘤的裸鼠，0.35mg/kg/day剂量可完全抑制肿瘤生长，0.75和1mg/kg/day剂量均可使肿瘤体积缩小[7]。
| Cell experiment [1]: | |
Cell lines | MCF-7, MGH-U1, and HT-29 cells |
Preparation Method | Exponentially growing cells were resuspended in media, cell number was determined using an electronic counter, and 100-250 cells were inoculated in triplicate onto 60 15-mm dishes containing 5mL of medium. After an overnight incubation, 5mL of 9-amino Camptothecin stock solutions were added to the dishes to achieve final concentrations of 0, 0.27, 1.37, 2.74, 13.7, 27.4, 137, and 274nM . After 4-, 8-, 12-, 24-, 48-, 72-, and 240-h exposures, medium was removed by aspiration and fresh medium was added to the dishes. Percentage of survival at each drug concentration with different exposure time was determined from the ratio of the number of the colonies in the drug-treated sample:the number in the control (DMSO vehicle-treated) sample. |
Reaction Conditions | 0.27, 1.37, 2.74, 13.7, 27.4, 137, and 274nM; 4-240h |
Applications | Cytotoxicity increased with increasing 9-amino Camptothecin concentration and exposure time. |
| Animal experiment [2]: | |
Animal models | Nude mice carrying PC-3 xenograft tumors |
Preparation Method | PC-3 cells (2×106 cells/mouse) mixed with Matrigel were subcutaneously inoculated into the bilateral flanks of nude mice. Treatment was initiated on day 5 post-inoculation. 9-amino Camptothecin was administered by oral gavage at doses of 0.35, 0.75, and 1mg/kg/day according to a schedule of 5 days on and 2 days off for 3 consecutive weeks. Tumor size was measured twice weekly, and tumor volume was calculated. |
Dosage form | 0.35, 0.75, 1mg/kg/day; 5 days/week; 3 weeks; p.o. |
Applications | A dose of 0.35mg/kg/day of 9-amino Camptothecin completely inhibited tumor growth, while doses of 0.75 and 1mg/kg/day reduced tumor volume. |
References: | |
| Cas No. | 91421-43-1 | SDF | |
| 别名 | 9-氨基喜树碱; 9-amino-20(S)-camptothecin | ||
| 化学名 | (4S)-10-amino-4-ethyl-4-hydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione | ||
| Canonical SMILES | O=C([C@@]1(CC)O)OCC2=C1C=C(C(N=C(C=CC=C3N)C3=C4)=C4C5)N5C2=O | ||
| 分子式 | C20H17N3O4 | 分子量 | 363.4 |
| 溶解度 | ≤1mg/ml in DMSO;1mg/ml in dimethyl formamide | 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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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7518 mL | 13.7589 mL | 27.5179 mL |
| 5 mM | 550.4 μL | 2.7518 mL | 5.5036 mL |
| 10 mM | 275.2 μL | 1.3759 mL | 2.7518 mL |
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动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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