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9-Aminocamptothecin

CAS No. : 91421-43-1

MCE 站：9-Aminocamptothecin

产品活性：9-Aminocamptothecin (9-Amino-CPT) 是拓扑异构酶 I 的抑制剂，具有有效地抗肿瘤活性。

研究领域：Cell Cycle/DNA Damage

作用靶点：Topoisomerase

结构分类：生物碱  |  吲哚类生物碱  |  结构分类

来源：植物  |  蓝果树科  |  喜树

In Vitro: 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 IC₅₀ values of 34.1, 10, 6.5, ａnd 8.9 nM, respectively after 96 h of drug exposure.

In Vivo: 9-Aminocamptothecin (9-Amino-CPT) 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-Aminocamptothecin is well tolerated at all doses, with no toxic death or weight loss of more than 10% observed in any group. 9-Aminocamptothecin 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.

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