9-氨基喜树碱
- CAS号:91421-43-1
- 英文名:9-Aminocamptothecin
- 中文名:9-氨基喜树碱
- CBNumber:CB5125434
- 分子式:C20H17N3O4
- 分子量:363.37
- MOL File:91421-43-1.mol
- 熔点 :142.0-145.0 °C
- 沸点 :819.6±65.0 °C(Predicted)
- 密度 :1.55±0.1 g/cm3(Predicted)
- 储存条件 :2-8°C(protect from light)
- 溶解度 :≤1mg/ml in DMSO;1mg/ml in dimethyl formamide
- 形态 :powder to crystal
- 酸度系数(pKa) :11.23±0.20(Predicted)
- 颜色 :Light yellow to Yellow to Orange
- Merck :14,431
- InChIKey :FUXVKZWTXQUGMW-FQEVSTJZSA-N
- CAS 数据库 :91421-43-1(CAS DataBase Reference)
- RTECS号 :UQ0490500
- 海关编码 :29349990
9-氨基喜树碱性质、用途与生产工艺
- 生物活性 9-amino-CPT (9-Aminocamptothecin, 9-AC, Aminocamptothecin, 9-amino-20(S)-camptothecin)是一种 Topoisomerase I 抑制剂并具有有效的抗癌活性。9-amino-CPT (9-Aminocamptothecin) 是喜树碱的一种具有活性的、不溶于水的衍生物。
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靶点
Target Value Topo I
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体外研究
In human breast (MCF-7), bladder (MGH-U1), and colon (HT-29) cancer cell lines, 9-Aminocamptothecin cytotoxicity increases with both higher drug concentrations and longer exposure times. Minimal cell killing is also observed unless 9-Aminocamptothecin concentrations exceeds a threshold of 2.7 nm. 9-Aminocamptothecin inhibits PC-3, PC-3M, DU145, and LNCaP cells with IC 50 values of 34.1, 10, 6.5, and 8.9 nM, respectively after 96 h of drug exposure.
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体内研究
9-amino-CPT (9-amino-20(S)-camptothecin) inhibits tumor growth at the lowest oral dose (0.35 mg/kg/day), whereas higher oral doses (0.75 and 1 mg/kg/day) and s.c. administration (4 mg/kg/week) causes tumor regression. 9-amino-CPT (9-amino-20(S)-camptothecin) is well tolerated at all doses, with no toxic death or weight loss of more than 10% observed in any group. 9-amino-CPT (9-amino-20(S)-camptothecin) induces complete remissions in 55 % of SCID mice engrafted with human myeloid leukemia. The oral and intravenous routes are equally effective. The results with this pre-clinical model support the evaluation of 9-Aminocamptothecin as antileukemic agent in a phase I trial in patients with AML.
- 化学性质 黄色结晶粉末,可溶于甲醇、乙醇、DMSO等有机溶剂,来源于珙桐科植物喜树Camptotheca acuminata Decne.的果实。
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用途
用于含量测定/鉴定/药理实验等。
药理药效:抗肿瘤 - 用途 中药对照品
- 更新日期:2024/11/08
- 产品编号:HY-100309
- 产品名称:9-Aminocamptothecin
- CAS编号:
- 包装:2 mg
- 价格:600元
- 更新日期:2024/11/08
- 产品编号:HY-100309
- 产品名称:9-Aminocamptothecin
- CAS编号:
- 包装:5 mg
- 价格:1150元
- 公司名称:Toronto Research Chemicals Inc.
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- 国家:加拿大
- 产品数:6668
- 优势度:58
- 公司名称:TORONTO
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- 电子邮件:info@trc-canada.com
- 国家:加拿大
- 产品数:6038
- 优势度:71