标签归档：camptothecin

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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Sodium Camptothecin(Synonyms: 喜树碱钠盐)

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Sodium Camptothecin (Synonyms: 喜树碱钠盐)

Sodium Camptothecin 是一种具有抗肿瘤活性的植物生物碱。Sodium Camptothecin 是一种可逆的 RNA 合成 (RNA synthesis) 抑制剂。Sodium Camptothecin 是一种有效的腺病毒复制抑制剂。Sodium Camptothecin 能抑制 DNA 合成 (DNA synthesis)，并引起细胞内预形成的病毒 DNA 断裂。

Sodium Camptothecin(Synonyms: 喜树碱钠盐)

Sodium Camptothecin Chemical Structure

CAS No. : 25387-67-1

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生物活性

Sodium Camptothecin is a plant alkaloid, with antitumor activity. Sodium Camptothecin is a reversible inhibitor of RNA synthesis. Sodium Camptothecin is an effective inhibitor of adenovirus replication. Sodium Camptothecin inhibits DNA synthesis and causes breaks in intracellular preformed viral DNA[1][2].

体外研究
(In Vitro)

Sodium Camptothecin (5 μM; 10 min) causes a severe inhibition of heterogeneously sedimenting nuclear RNA (HnRNA) synthesis[1].
Sodium Camptothecin also blocks a specific step in the processing of ribosomal precursor RNA, allowing the conversion of 45S RNA to 32S RNA, but inhibiting the conversion of 32S RNA to 28S RNA [1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

388.35

Formula

C20H17N2NaO5
CAS 号

25387-67-1
中文名称

喜树碱钠盐
运输条件

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

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. R S Wu, et al. Ribosome formation is blocked by camptothecin, a reversible inhibitor of RNA synthesis. Proc Natl Acad Sci U S A. 1971 Dec;68(12):3009-14.

    [2]. M S Horwitz, et al. Camptothecin: mechanism of inhibition of adenovirus formation. Virology. 1972 Jun;48(3):690-8

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Camptothecin-d5(Synonyms: Campathecin-d5; (S)-(+)-Camptothecin-d5; CPT-d5)

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Camptothecin-d5 (Synonyms: Campathecin-d5; (S)-(+)-Camptothecin-d5; CPT-d5)

Camptothecin-d5 (Campathecin-d5) 是 Camptothecin 的氘代物。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-d5(Synonyms: Campathecin-d5; (S)-(+)-Camptothecin-d5; CPT-d5)

Camptothecin-d5 Chemical Structure

CAS No. : 1329616-37-6

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生物活性

Camptothecin-d5 (Campathecin-d5) is the deuterium labeled Camptothecin. 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].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

353.38

Formula

C20H11D5N2O4
CAS 号

1329616-37-6
中文名称

喜树碱 d5
运输条件

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

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. 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.

    [3]. 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.

    [4]. 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.

    [5]. 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.

    [6]. 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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Camptothecin-20(S)-O-propionate(Synonyms: Camptothecin-20-O-propionate)

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Camptothecin-20(S)-O-propionate (Synonyms: Camptothecin-20-O-propionate) 纯度: 98.43%

Camptothecin-20(S)-O-propionate (CZ48) 是喜树碱 (CPT) 的类似物，是强效的抗肿瘤化合物。Camptothecin-20(S)-O-propionate (CZ48) 是拓扑异构酶 I (topoisomerase-Ι) 的抑制剂。

Camptothecin-20(S)-O-propionate(Synonyms: Camptothecin-20-O-propionate)

Camptothecin-20(S)-O-propionate Chemical Structure

CAS No. : 194414-69-2

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3850 In-stock
5 mg ￥3500 In-stock
10 mg ￥5800 In-stock
50 mg ￥16500 In-stock
100 mg ￥25500 In-stock
200 mg   询价  
500 mg   询价  

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生物活性

Camptothecin-20(S)-O-propionate (CZ48), the C20-propionate ester of CPT, is a highly effective anticancer agent. Camptothecin-20(S)-O-propionate (CZ48) is a topoisomerase-Ι inhibitor[1][2][3].

体内研究
(In Vivo)

Camptothecin-20(S)-O-propionate (CZ48, gavage, 100 to 2000 mg/kg/day) exhibits anti-tumor activity in CLO-breast carcinoma (100 mg/kg) and PC3-prostate carcinoma (1000 mg/kg) models in mice[3].

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: A tumor xenograft growing in a nude mouse (size, ∼1 cm3)[3].
Dosage: 100-1000 mg/kg/day.
Administration: Oral gavage, for 2, 4 and 6 days, respectively.
Result: Exhibited anti-tumor effect.

Clinical Trial

分子量

404.42

Formula

C23H20N2O5
CAS 号

194414-69-2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 9.09 mg/mL (22.48 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4727 mL 12.3634 mL 24.7268 mL
5 mM 0.4945 mL 2.4727 mL 4.9454 mL
10 mM 0.2473 mL 1.2363 mL 2.4727 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。-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]. Zhisong Cao, et al. Crystalline camptothecin-20(S)-O-propionate hydrate: a novel anticancer agent with strong activity against 19 human tumor xenografts. Cancer Res. 2009 Jun 1;69(11):4742-9.

    [2]. Zhisong Cao, et al. Crystalline camptothecin-20(S)-O-propionate hydrate: a novel anticancer agent with strong activity against 19 human tumor xenografts. Cancer Res. 2009 Jun 1;69(11):4742-9.

    [3]. Xing Liu, et al. Correlation between the sensitivity of tumors to treatment with CZ48 and local concentrations of the active metabolite CPT within the tumors. Biomed Rep. 2013 Mar;1(2):202-206.

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