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Camptothecin.

Campathecin 是有效的 DNA拓扑异构酶 I 抑制剂，IC50 值为 679 nM。

目录号: PC10269 纯度: ≥98%

CAS No. :7689-03-4

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中文名称	Camptothecin.
中文别名	喜树碱;4-乙基-4-羟基-1H-吡喃[3’,4’：6,7]氮茚[1,2]喹啉-3,14(4H,12H)-二酮;(+)-喜树碱;(S)-(+)-喜树碱;黄岑苷;5,6,7-三羥黃酮-7-葡萄糖醛酸酯;貝加靈;5,6,7-三羟黄酮-7-葡萄糖醛酸酯;(S)-4-乙基-4-羟基-1H-吡喃并[3’,4’:6,7]吲嗪并[1,2-b]喹啉-3,14-(4H,12H)-二酮;喜树碱对照品;马比木提取物;天麻素;喜树碱标准品;喜树碱喜树提取物马比木提取物;喜树碱（标准品）;喜树碱植物提取物,标准品,对照品;辛弗林;(S)-4-乙基-4-羟基-1H-吡喃并[3',4':6,7]吲嗪并[1,2-b]喹啉-3,14-(4H,12H)-二酮;4-乙基-4-羟基-1H-吡喃[3',4'：6,7]氮茚[1,2]喹啉-3,14(4H,12H)-二酮;分析对照品;((+)-喜树碱)
英文名称	Camptothecin
英文别名	Camptothecine;1,6-DIHYDROXY-7-GLUCURONOSYLFLAVONE;(20S)-CAMPTOTHECIN;4-ETHYL-4-HYDROXY-1H-PYRANO[3',4':6,7]INDOLIZINO[1,2-B]QUINOLINE-3,14(4H,12H)DIONE;5,6-DIHYDROXY-4-OXO-2-PHENYL-4H-1-BENZOPYRAN-7-YL BETA-D-GLUCOPYRANOSIDURONIC ACID;5,6-DIHYDROXY-7-GLUCURONOSYLFLAVONE;BAICALEIN-7-O-GLUCURONIDE;BAICALIN;(+)-CAMPTOTHECIN;CAMPTOTHECIN, CAMPTOTHECA ACUMINATA;(S)-4-ETHYL-4-HYDROXY-1,12-DIHYDRO-4H-2-OXA-6,12A-DIAZA-DIBENZO[B,H]FLUORENE-3,13-DIONE;(S)-4-ETHYL-4-HYDROXY-1H-PYRANO-[3',4':6,7]INDOLIZINO[1,2-B]QUINOLINE-3,14(4H,12H)-DIONE;(S)-(+)-CAMPTOTHECIN;(s)-droxy;1h-pyrano(3’,4’:6,7)indolizino(1,2-b)quinoline-3,14(4h,12h)-dione,4-ethyl-4-hy;20(s)-camptothecine;21,22-secocamptothecin-21-oicacidlactone;nsc100880;nsc94600;S-(+)-Camptothecin;camptothecin;Camptothecin (CPT,Camptohecine, NSC100880,NSC 94600);CAMPTOTHECIN(P);-(+)-Camptothecin;(S)-4-ethyl-4-hydroxy-1H-pyrano-[3',4':6,7]indolizinol[1,2-b]quinoline-3,14(4H,12H)-dione;Baicalin std.;CaMpathecin;Camptohecin;CPT;d-Camptothecin;4-Ethyl-4-hydroxy-1H-pyrano-[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione;[ "" ];(+)-Camptothecine;(S)-Camptothecin;Camptothecine (8CI);20(S)-Camptothecin;Camptothecine (S,+);MLS000766223;XT3Z54Z28A;VSJKWCGYPAHWDS-FQEVSTJZSA-N;Camptoth;(S)-4-ethyl-4-hydroxy-1H-Pyrano[3',4':6,7]indolizino[1,2-b]quinoline
Cas No.	7689-03-4
分子式	C₂₀H₁₆N₂O₄
分子量	348.35
包装储存	4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

生物活性

Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC₅₀ of 679 nM. Camptothecin (CPT) exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers, modulates hypoxia-inducible factor-1α (HIF-1α) activity by changing microRNAs (miRNA) expression patterns in human cancer cells.

性状

Solid

IC50 & Target[1][2]

Topoisomerase I

679 nM (IC₅₀)

Camptothecins

体外研究(In Vitro)

High TOP1 enzymatic activity MCF7 (Luminal subtype) and HCC1419 (HER2 subtype) show high sensitivity toward Camptothecin (0.1?μM to 5?μM; 72?hours) treatment, exhibiting the IC₅₀ values of 0.089?μM and 0.067?μM, respectively.
Camptothecin (0.5?μM; 6 and 24 hours) reduces desferrioxamine-activated VEGF expression.
Camptothecin (0.5?μM; 8 to 24 hours) strongly prevents the desferrioxamine-dependent HIF-1a accumulation.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line:	MCF7 (Luminal subtype) and HCC1419 (HER2 subtype)
Concentration:	0.1?μM to 5?μM
Incubation Time:	72?hours
Result:	High TOP1 enzymatic activity MCF7 (Luminal subtype) and HCC1419 (HER2 subtype) show high sensitivity toward CPT (0.1?μM to 5?μM; 72?hours) treatment, exhibiting the IC₅₀ values of 0.089?μM and 0.067?μM, respectively.

RT-PCR

Cell Line:	HeLa and HEK293 cell lines
Concentration:	0.5 μmol/L
Incubation Time:	6 and 24 hours
Result:	Reduces desferrioxamine-activated VEGF expression in both cell lines after 6 and 24 hours of treatment, whereas in normoxic condition camptothecin does not affect the VEGF mRNA level.

Western Blot Analysis

Cell Line:	HeLa and HEK293 cell lines
Concentration:	0.5 μmol/L
Incubation Time:	8 to 24 hours
Result:	Strongly prevents the desferrioxamine-dependent HIF-1a accumulation after 8 to 24 hours, whereas it does not affect HIF-1b levels.

体内研究(In Vivo)

Camptothecin (2 mg/kg every other day) treats mice, has developed numerous pulmonary metastases.
Treatment with both kinase inhibitor of nuclear factor-kappaB-1 (KINK-1) and Camptothecin led to a statistically significant reduction in the number of pulmonary metastases.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	C57BL6 mice (injected with B16F10 melanoma cells)
Dosage:	2 mg/kg
Administration:	every other day, after 19 days
Result:	Has developed numerous pulmonary metastases.

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

ClinicalTrial

结构分类

来源

参考文献

[1]. Luzzio MJ, et al. Synthesis and antitumor activity of novel water soluble derivatives of camptothecin as specific inhibitors of topoisomerase I. Synthesis and antitumor activity of novel water soluble derivatives of camptothecin as specific inhibitors of topoisomerase I. [Information]

[2]. Bertozzi D, et al. The natural inhibitor of DNA topoisomerase I, camptothecin, modulates HIF-1α activity by changing miR expression patterns in human cancer cells. Mol Cancer Ther. 2014;13(1):239-248. [Information]

[3]. Huang Q, et al. Evolution in medicinal chemistry of E-ring-modified Camptothecin analogs as anticancer agents. Eur J Med Chem. 2013;63:746-757. [Information]

[4]. Tesauro C, et al. Topoisomerase I activity and sensitivity to camptothecin in breast cancer-derived cells: a comparative study. BMC Cancer. 2019;19(1):1158. Published 2019 Nov 29. [Information]

[5]. Sch?n M, et al. KINK-1, a novel small-molecule inhibitor of IKKbeta, and the susceptibility of melanoma cells to antitumoral treatment. J Natl Cancer Inst. 2008;100(12):862-875.. [Information]

溶解度数据

体外研究:

1M NaOH : 10 mg/mL (28.71 mM; ultrasonic and adjust pH to 11 with NaOH)

DMSO : 6.25 mg/mL (17.94 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 15% Cremophor EL 85% Saline
Solubility: 10 mg/mL (28.71 mM); Suspended solution; Need ultrasonic

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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