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9-amino-CPT

9-amino-CPT (Aminocamptothecin) 是一种拓扑异构酶I 的抑制剂，具有抗肿瘤活性。

CAS号

91421-43-1

分子式

C20H17N3O4

主要靶点

Topoisomerase

仅限科研使用

Cat No : CM02617

Print datasheet

Synonyms

9-氨基喜树碱|Aminocamptothecin|9-amino-2(S)-camptothecin|9-Aminocamptothecin

验证数据展示

  • CAS No.: 91421-43-1

    9-amino-CPT
    CAS#: 91421-43-1

产品信息

9-Aminocamptothecin is an inhibitor of topoisomerase I with potent anticancer activity.

CAS号 91421-43-1
分子式 C20H17N3O4
主要靶点 Topoisomerase
主要通路 DNA损伤和修复
分子量 363.4
纯度 99.82%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 9-氨基喜树碱|Aminocamptothecin|9-amino-2(S)-camptothecin|9-Aminocamptothecin

体内活性

9-Aminocamptothecin 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 [1]. 9-Aminocamptothecin induces complete remissions in 55 % of SCID mice engrafted with human myeloid leukemia. The oral and intravenous routes are equally effective [3].

体外活性

9-Aminocamptothecin inhibits PC-3, PC-3M, DU145, and LNCaP cells with IC50 values of 34.1, 10, 6.5, and 8.9 nM, respectively after 96 h of drug exposure [1]. In human bladder (MGH-U1), breast (MCF-7), 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 exceed a threshold of 2.7 nM [2].

溶解度

DMSO:3.33 mg/mL (9.16 mM)

参考文献

1.de Souza PL, et al. 9-Aminocamptothecin: a topoisomerase I inhibitor with preclinical activity in prostate cancer. Clin Cancer Res. 1997 Feb;3(2):287-94.
2.Li ML, et al. Pharmacological determinants of 9-aminocamptothecin cytotoxicity. Clin Cancer Res. 2001 Jan;7(1):168-74.
3.Jeha S, et al. Activity of oral and intravenous 9-aminocamptothecin in SCID mice engrafted with human leukemia. Leuk Lymphoma. 1998 Dec;32(1-2):159-64.

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The dilution calculator equation

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