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

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Camptothecin (Synonyms: 喜树碱; Campathecin; (S)-(+)-Camptothecin; CPT) 纯度: 99.69%

Camptothecin (CPT)，一种生物碱，是一种 DNA topoisomerase I (Topo I) 抑制剂，其 IC50 值为 679 nM。Camptothecin (CPT) 对结直肠癌、乳腺癌、肺癌和卵巢癌具有强大的抗肿瘤活性，通过改变人类癌细胞中的 miRNA 表达模式来调节 hypoxia-inducible factor-1α (HIF-1α) 活性。

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

Camptothecin Chemical Structure

CAS No. : 7689-03-4

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生物活性

Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC50 of 679 nM[1]. 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[2][3].

IC50 & Target[3]

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[4].
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[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[4]

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[2]

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[2]

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[5].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL6 mice (injected with B16F10 melanoma cells)[5]
Dosage: 2 mg/kg
Administration: every other day, after 19 days
Result: Has developed numerous pulmonary metastases.

Clinical Trial

分子量

348.35

Formula

C20H16N2O4
CAS 号

7689-03-4
中文名称

喜树碱
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, protect from light

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

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

配制储备液
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

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，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，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
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.

    [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.

    [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.

    [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.

    [5]. Schön 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..

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