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CAS No.: 7689-03-4

喜树碱 Catalog No. CSN16581

Synonyms: 喜树碱;Campathecin;(S)-(+)-Camptothecin

Camptothecin is a potent DNA enzyme topoisomerase I (topo I) inhibitor with an IC50 and IC70 of 50 nM and 0.225 μM for breast cancer cell line MDA-MB-231.

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400-920-2911

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Topoisomerase I

IC70:0.225μM MMP2

Ki:13.9nM
描述Eukaryotic DNA topoisomerases I and II are essential nuclear enzymes responsible for the organization and modulation of the topological features of DNA and facilitate cell replication, transcription and repairment of genetic information. Camptothecin, a pentacyclic alkaloid natural product with antitumor properties, is a Topoisomerase I inhibitor with IC50 value of 679nM (measured by Topoisomerase I cleavable complex assay). A series of Topoisomerase inhibitors containing a closed lactone necessary for topoisomerase I inhibition, such as Irinotecan, SN-38, are the derivatives of campathecin. Campathecin inhibited the cell proliferation with IC50 values of 46nM, 48nM, 207nM, 37nM and 41nM for HT29, LOX, T47D, SKOV3 and SKVLB cell lines. Camptothecin produces DNA single-strand breaks and DNA-protein cross-links in mammalian cells. The sensitivity to camptothecin in cells may be modulated by autophagy in some cell lines. Increased expression levels of apoptosis-associated proteins, including increased cleaved caspase-9 and caspase-3, and increased DNA damage-sensor γH2AX, can be observed in H1299 cells treated with low dose of Camptothecin at 0.5μM. But the resistance in response to higher concentrations of Camptothecin could be observed at concentration of 5 μM. This may due to the autophagy induced by high dose of Camptothecin, shown as the markedly increased LC3B-II. Meanwhile, the Camptothecin-induced autophagy could also protect lung cancer cells from programmed cell death.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
A2780	-	cytotoxicity assay	-	IC50=4 nM	11858737
A427	~1 μM	Growth inhibitory assay	-	IC50=24 nM	9876111
A549	-	cytotoxicity assay	-	IC50=67 nM	10841808

动物研究

剂量

Rat: 30 mg/kg^[3] (i.g.)

给药途径

i.g.

动物药代数据

Animal	Rats^[3]
Dose	30 mg/kg
Administration	p.o.
F	1
T_1/2	1.843 ± 0.394 h
T_max	0.500 ± 0.000 h
C_max	0.656 ± 0.055 nmol/mL
AUC_0→∞	2.749 ± 0.329 nmol/ml·h
AUC_0→t	2.694 ± 0.312 nmol/ml·h

参考文献

[1] Luzzio MJ, Besterman JM, et al. Synthesis and antitumor activity of novel water soluble derivatives of camptothecin as specific inhibitors of topoisomerase I. J Med Chem. 1995 Feb 3;38(3):395-401.
[2] Hsiang YH, Hertzberg R, et al. Camptothecin induces protein-linked DNA breaks via mammalian DNA topoisomerase I. J Biol Chem. 1985 Nov 25;260(27):14873-8.
[3] Xiao L, Zhou Y, et al. Transporter-Targeted Bile Acid-Camptothecin Conjugate for Improved Oral Absorption. Chem Pharm Bull (Tokyo). 2019 Oct 1;67(10):1082-1087.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.8707 mL
- 14.3534 mL
- 28.7068 mL
- 5 mM
- 0.5741 mL
- 2.8707 mL
- 5.7414 mL
- 10 mM
- 0.2871 mL
- 1.4353 mL
- 2.8707 mL

技术信息

CAS号

7689-03-4

储存条件

粉末: Keep in dark place,Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H16N2O4

运输

蓝冰

分子量

348.35

别名

喜树碱;Campathecin;(S)-(+)-Camptothecin;CPT

溶解度

DMSO	3.0 mg/mL (8.6 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

A2780	-	cytotoxicity assay	-	IC50=4 nM	11858737
A427	~1 μM	Growth inhibitory assay	-	IC50=24 nM	9876111
A549	-	cytotoxicity assay	-	IC50=67 nM	10841808
A549	-	cytotoxicity assay	-	IC50=14 nM	11334569
A549	-	cytotoxicity assay	-	IC50=2.53 μM	12639541
Caki-2	-	cytotoxicity assay	-	IC50=3.96 μM	12639541
CCRF-CEMc	-	cytotoxicity assay	-	IC50=3 nM	17254669
CCRF-SB	-	cytotoxicity assay	-	IC50=3 nM	17254669
Col2	~1 μM	cytotoxicity assay	-	ED50=57 nM	15043407
CPT-K5	~10 μM	cytotoxicity assay	-	IC50>10 μM	15482929
CRL 7065	-	cytotoxicity assay	-	IC50=400 nM	17254669
DU145	-	cytotoxicity assay	-	IC50=10 nM	17254669
DU-145	-	Growth inhibitory assay	-	IC50=10 nM	11020283
DU-145	~10 μM	cytotoxicity assay	-	GI50=10 nM	15509164
F-539	~10 μM	cytotoxicity assay	-	GI50=10 nM	15509164
H128	-	cytotoxicity assay	-	IC50=18 nM	11334569
HCT116	-	cytotoxicity assay	-	IC50=9 nM	11858737
HCT-116	-	Growth inhibitory assay	-	IC50=30 nM	11020283
HCT-116	~10 μM	cytotoxicity assay	-	GI50=30 nM	15509164
HEC-1-B	-	cytotoxicity assay	-	IC50=8.64 μM	12639541
HepG2	-	cytotoxicity assay	-	IC50=30 nM	17254669
HL-60	-	cytotoxicity assay	-	IC50=66 nM	12639541
HOP-62	-	Growth inhibitory assay	-	IC50=10 nM	11020283
HOP-62	~10 μM	cytotoxicity assay	-	GI50=10 nM	15509164
HT29	-	cytotoxicity assay	-	IC50=87.8 nM	9003520
HT29	-	cytotoxicity assay	-	IC50=80 nM	10841808
HT-29	-	cytotoxicity assay	-	IC50=1.4 μM	12639541
HUVEC	~1 μM	cytotoxicity assay	-	ED50=258 nM	15043407
IMR-32	~10 μM	cytotoxicity assay	-	IC50=2.21 nM	12617894
JLC	-	cytotoxicity assay	-	IC50=5.6 nM	12620081
K562adr	~1 μM	Growth inhibitory assay	-	IC50=57 nM	9876111
KB	-	cytotoxicity assay	-	IC50=8 nM	9003520
KB	~1 μM	cytotoxicity assay	-	ED50=22 nM	15043407
KB3-1	~10 μM	cytotoxicity assay	-	IC50=40 nM	15482929
KB7D	-	Growth inhibitory assay	-	IC50=35 nM	10411476
KBCamp	-	Growth inhibitory assay	-	IC50=1.04 μM	10411476
KBH	~10 μM	cytotoxicity assay	-	IC50=440 nM	15482929
KBMDR	-	Growth inhibitory assay	-	IC50=70 nM	10411476
KBV-1 + MDR1	~10 μM	cytotoxicity assay	-	IC50=440 nM	15482929
KBV20C	-	Growth inhibitory assay	-	IC50=30 nM	10411476
KBwt	-	Growth inhibitory assay	-	IC50=40 nM	10411476
LCNaP	~1 μM	cytotoxicity assay	-	ED50=28 nM	15043407
Lewis	-	cytotoxicity assay	-	IC50=33 nM	12620081
Lu1	~1 μM	cytotoxicity assay	-	ED50=29 nM	15043407
LX-1	-	cytotoxicity assay	-	IC50=120 nM	11858737
MCF-7	-	cytotoxicity assay	-	IC50=40 nM	17254669
MCF7mdr	~1 μM	Growth inhibitory assay	-	IC50=3.1 nM	9876111
MDA-MB-435	-	Growth inhibitory assay	-	IC50=40 nM	11020283
MDA-MB-435	~10 μM	cytotoxicity assay	-	GI50=40 nM	15509164
MKN45	-	cytotoxicity assay	-	IC50=17 nM	11334569
MT-4	-	cytotoxicity assay	-	IC50=4 nM	17254669
OVCAR-3	-	Growth inhibitory assay	-	IC50=220 nM	11020283
OVCAR-3	~10 μM	cytotoxicity assay	-	GI50=220 nM	15509164
P388	-	Growth inhibitory assay	-	IC50=32 nM	10346933
P388	-	cytotoxicity assay	-	IC50=13 nM	12620081
P388	~10 μM	cytotoxicity assay	-	IC50=14 nM	15482929
P388/CPT45	~10 μM	cytotoxicity assay	-	IC50>10 μM	15482929
P388CPT5 R	-	Growth inhibitory assay	-	IC50=2.8 μM	10346933
PC-3	~1 μM	Growth inhibitory assay	-	IC50=57 nM	9876111
RPMI8402	~10 μM	cytotoxicity assay	-	IC50=6 nM	15482929
SF-539	-	Growth inhibitory assay	-	IC50=10 nM	11020283
SK-BR-3	-	cytotoxicity assay	-	IC50=20 nM	11334569
SK-MEL-28b	-	cytotoxicity assay	-	IC50=40 nM	17254669
SKMES-1	-	cytotoxicity assay	-	IC50=10 nM	17254669
SKOV3	-	cytotoxicity assay	-	IC50=51 nM	9003520
SK-OV-3	-	cytotoxicity assay	-	IC50=20 nM	11334569
SKVLB	-	cytotoxicity assay	-	IC50=53 nM	9003520
SN12C	-	Growth inhibitory assay	-	IC50=20 nM	11020283
SN12C	~10 μM	cytotoxicity assay	-	GI50=20 nM	15509164
T24	-	cytotoxicity assay	-	IC50=88 nM	10841808
UACC-62	-	Growth inhibitory assay	-	IC50=10 nM	11020283
UACC-62	~10 μM	cytotoxicity assay	-	GI50=10 nM	15509164
WiDr	-	cytotoxicity assay	-	IC50=17 nM	11334569
WIL-2NSd	-	cytotoxicity assay	-	IC50=5 nM	17254669

靶点	Description	IC50
Topoisomerase I		IC70:0.225μM
MMP2		Ki:13.9nM

喜树碱 Catalog No. CSN16581

靶点选择性

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