Camptothecin (Synonyms:喜树碱; Campathecin; (S-(+)-Camptothecin; CPT))
目录号 : KM10664 CAS No. : 7689-03-4 纯度 : 98%

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。

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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. 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.

IC50&Target

Topoisomerase I

679 nM (IC50)

Camptothecins

 

体外研究

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.

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

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.

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.
分子式
C20H16N2O4
分子量
348.35
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。

临床试验
科研文献
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计算结果:

工作液浓度 mg/ml;

DMSO母液配制方法 mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,

体内配方配制方法μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。

配置后的溶液总体积

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           2. 一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。