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。
| 生物活性 | Camptothecin (CPT), a kind of alkaloid, is aDNAtopoisomeraseI (Topo I) inhibitorwith anIC50of 679 nM[1]. Camptothecin (CPT) exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers, modulateshypoxia-inducible factor-1α (HIF-1α)activity by changingmicroRNAs(miRNA)expression patterns in humancancercells[2][3]. |
| IC50& Target[3] | Topoisomerase I 679 nM (IC50) | Camptothecins |
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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 IC50values 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].
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 IC50values 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. |
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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].
| 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. |
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| 结构分类 | - Alkaloids
- Quinoline Alkaloids
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| 来源 | - Plants
- Nyssaceae
- Camptotheca acuminataDecne.
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| 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: 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) 配制储备液 | 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℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro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. 请依序添加每种溶剂： 15% Cremophor EL 85% Saline Solubility: 10 mg/mL (28.71 mM); Suspended solution; Need ultrasonic
*以上所有助溶剂都可在本网站选购。 |
