10-羟基喜树

中文名称:

10-羟基喜树碱

中文同义词:

10-羟基喜树碱;10-(±)羟基喜树碱标准品;10-羟基喜树碱(CAS号:64439-81-2)

英文名称:

10-Hydroxycamptothecin

英文同义词:

10-HYDROXYCAMPTOTHECIN ACETATE;10-HYDROXYCAMPTOTHECIN ACETATE SALT;7-ETHYL-10-HYDROXY CAMPTHOTECIN;Hydroxy Camptothecine;77-Ethyl-10-hydroxy campthotecin;(20S)- 7-Ethyl-10-Hydroxycamptothecin;10-Hydroxycamp-totecin;7ETHYHYDROXYCAMPTOTHECIN

CAS号:

64439-81-2

分子式:

C20H16N2O5

分子量:

364.35

EINECS号:

613-598-9

相关类别:

医药中间体;其它有机试剂;对照品,标准品;小分子抑制剂;小分子抑制剂，天然产物;原料药;喜树碱系列;原料;医药、农药及染料中间体;贝尔卡主打;陕西林奈主打产品;Antineoplastic;Camptothecin series;Inhibitors

Mol文件:

64439-81-2.mol

熔点 

230-237°C

沸点 

820.7±65.0 °C(Predicted)

密度 

1.60

储存条件 

−20°C

酸度系数(pKa)

8.93±0.40(Predicted)

形态

Pale yellow powder

InChIKey

LCZZWLIDINBPRC-FQEVSTJZSA-N

CAS 数据库

64439-81-2(CAS DataBase Reference)

生物活性

(±)-10-Hydroxycamptothecin 是从喜树中分到的生物碱，能够抑制拓扑异构酶 I (topoisomerase I) 的活性，具有广谱的抗肿瘤活性。

靶点

Target Value DNA topoisomerase I ()

Target

Value

DNA topoisomerase I ()

体外研究

(±)-10-Hydroxycamptothecin (10-OH-camptothecin) is an inhibitor of topo I. (±)-10-Hydroxycamptothecin (10-HCPT, 5-20 nM) markedly inhibits the proliferation of Colo 205 cells in a dose-dependent manner. (±)-10-Hydroxycamptothecin (5-20 nM) arrests Colo 205 cells in the G2 phase of the cell cycle and triggers apoptosis through a caspase-3-dependent pathway. (±)-10-Hydroxycamptothecin (HPT, 0.01-10 μg/mL) causes cell shrinage, nuclear fragmentation and condensed chromosomes and induces apoptosis of human urinary bladder cancer cell line (T24).

体内研究

(±)-10-Hydroxycamptothecin (10-HCPT, 2.5-7.5 mg/kg/2 days, p.o.) significantly suppresss tumor growth in mouse xenografts. (±)-10-Hydroxycamptothecin (1-7.5 mg/kg, p.o., once per 2 or 4 days) causes no obvious acute toxicity in nude mice.

用途 

抗肿瘤植物药。

危险品标志 

Xi,T

危险类别码 

36/37/38-25

安全说明 

26-36-45

危险品运输编号 

UN 2811 6.1 / PGIII

WGK Germany 

3

RTECS号

UQ0491000