标签归档：cpt

9-amino-CPT(Synonyms: 9-氨基喜树碱; 9-amino-20(S)-camptothecin)

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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。

9-amino-CPT (Synonyms: 9-氨基喜树碱; 9-amino-20(S)-camptothecin) 纯度: 99.05%

9-amino-CPT (9-amino-20(S)-camptothecin) 是拓扑异构酶I的抑制剂，具有有效地抗肿瘤活性。

9-amino-CPT(Synonyms: 9-氨基喜树碱; 9-amino-20(S)-camptothecin)

9-amino-CPT Chemical Structure

CAS No. : 91421-43-1

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1150 In-stock
2 mg ￥600 In-stock
5 mg ￥1200 In-stock
10 mg ￥1800 In-stock
25 mg ￥3300 In-stock
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生物活性

9-amino-CPT (9-amino-20(S)-camptothecin) is a topoisomerase I inhibitor with potent anticancer activity.

IC50 & Target[1]

Topoisomerase I

 

体外研究
(In Vitro)

In human breast (MCF-7), bladder (MGH-U1), and colon (HT-29) cancer cell lines, 9-Aminocamptothecin cytotoxicity increases with both higher drug concentrations and longer exposure times. Minimal cell killing is also observed unless 9-Aminocamptothecin concentrations exceeds a threshold of 2.7 nm[1]. 9-Aminocamptothecin inhibits PC-3, PC-3M, DU145, and LNCaP cells with IC50 values of 34.1, 10, 6.5, and 8.9 nM, respectively after 96 h of drug exposure[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.
体内研究
(In Vivo)

9-amino-CPT (9-amino-20(S)-camptothecin) inhibits tumor growth at the lowest oral dose (0.35 mg/kg/day), whereas higher oral doses (0.75 and 1 mg/kg/day) and s.c. administration (4 mg/kg/week) causes tumor regression. 9-amino-CPT (9-amino-20(S)-camptothecin) is well tolerated at all doses, with no toxic death or weight loss of more than 10% observed in any group[2]. 9-amino-CPT (9-amino-20(S)-camptothecin) induces complete remissions in 55 % of SCID mice engrafted with human myeloid leukemia. The oral and intravenous routes are equally effective. The results with this pre-clinical model support the evaluation of 9-Aminocamptothecin as antileukemic agent in a phase I trial in patients with AML[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.
分子量

363.37

Formula

C20H17N3O4
CAS 号

91421-43-1
中文名称

9-氨基喜树碱
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 : 3.33 mg/mL (9.16 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7520 mL 13.7601 mL 27.5202 mL
5 mM 0.5504 mL 2.7520 mL 5.5040 mL
10 mM — — —

*

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。

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： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 0.33 mg/mL (0.91 mM); Clear solution

    此方案可获得 ≥ 0.33 mg/mL (0.91 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 3.3 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 0.33 mg/mL (0.91 mM); Clear solution

    此方案可获得 ≥ 0.33 mg/mL (0.91 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 3.3 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 0.33 mg/mL (0.91 mM); Clear solution

    此方案可获得 ≥ 0.33 mg/mL (0.91 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 3.3 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Li ML, et al. Pharmacological determinants of 9-aminocamptothecin cytotoxicity. Clin Cancer Res. 2001 Jan;7(1):168-74.

    [2]. de Souza PL, et al. 9-Aminocamptothecin: a topoisomerase I inhibitor with preclinical activity in prostate cancer. Clin Cancer Res. 1997 Feb;3(2):287-94.

    [3]. Jeha S, et al. Activity of oral and intravenous 9-aminocamptothecin in SCID mice engrafted with human leukemia. Leuk Lymphoma. 1998 Dec;32(1-2):159-64.
Cell Assay
[1]

The cytotoxicity of 9-amino-CPT (9-amino-20(S)-camptothecin) is assessed by clonogenic assay. Exponentially growing cells are resuspended in media, cell number is determined using an electronic counter, and 100–250 cells are inoculated in triplicate onto 60 15-mm dishes containing 5 mL of medium. After an overnight incubation, 5 μL of 9-Aminocamptothecin stock solutions are added to the dishes to achieve final concentrations of 0, 0.27, 1.37, 2.74, 13.7, 27.4, 137, and 274 nM. After 4-, 8-, 12-, 24-, 48-, 72-, and 240-h exposures, medium is removed by aspiration and fresh medium is added to the dishes. Percentage of survival at each drug concentration with different exposure time is determined from the ratio of the number of the colonies in the drug-treated sample:the number in the control (DMSO vehicle-treated) sample[1].

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 Administration
[3]

Mice: Treatment with 9-Aminocamptothecin is started on day 7 after inoculation with KBM-3 cells. Five groups of 5 mice each (average weight of 22 g) are used and treatment is administered daily 4 days a week for 3 weeks as follows: 1) group 1 control mice are injected IV with PBS; 2) group 2 mice receive 1.33 mg/kg 9-Aminocamptothecin IV, 3) group 3 mice receive 1.33 mg/kg 9-Aminocamptothecin orally by gavage; 4) group 4 mice receive 2.0 mg/kg 9-Aminocamptothecin IV; 5) group 5 mice receive 2.0 mg/kg 9-Aminocamptothecin orally by gavage[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.
参考文献

  • [1]. Li ML, et al. Pharmacological determinants of 9-aminocamptothecin cytotoxicity. Clin Cancer Res. 2001 Jan;7(1):168-74.

    [2]. de Souza PL, et al. 9-Aminocamptothecin: a topoisomerase I inhibitor with preclinical activity in prostate cancer. Clin Cancer Res. 1997 Feb;3(2):287-94.

    [3]. Jeha S, et al. Activity of oral and intravenous 9-aminocamptothecin in SCID mice engrafted with human leukemia. Leuk Lymphoma. 1998 Dec;32(1-2):159-64.

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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

规格 是否有货
1 mg Check price and availability
5 mg Check price and availability

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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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CPT-Se3

发表于由

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。

CPT-Se3 

CPT-Se3 是喜树碱 (CPT) 的一种含硒前体药物，在杀死癌细胞和抑制肿瘤生长方面表现出更高的效力。CPT-Se3 降低 GSH/GSSG 比率和总硫醇，提高 Hep G2 细胞中的 ROS 水平，并最终诱导癌细胞凋亡 (apoptosis)。CPT-Se3 对 HeLa、Hep G2、A549 和 SMMC-7721 细胞具有细胞毒性（IC50= 2.19-4.7 μM）。

CPT-Se3

CPT-Se3 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

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生物活性

CPT-Se3, a selenoprodrug of Camptothecin (CPT), shows improved potency in killing cancer cells and inhibiting tumor growth. CPT–Se3 decreases the GSH/GSSG ratio and total thiols, elevates the ROS level in Hep G2 cells, and eventually induces apoptosis of cancer cells. CPT-Se3 shows cytotoxicity against HeLa, Hep G2, A549, and SMMC-7721 cells (IC50= 2.19-4.7 μM)[1].

分子量

590.35

Formula

C24H20N2O6Se2
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]. Zhao J, et al. Integration of a Diselenide Unit Generates Fluorogenic Camptothecin Prodrugs with Improved Cytotoxicity to Cancer Cells. J Med Chem. 2021;64(24):17979-17991.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

CPT-Se4

发表于由

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。

CPT-Se4 

CPT-Se4 是喜树碱 (CPT) 的一种含硒前体药物，在杀死癌细胞和抑制肿瘤生长方面表现出更高的效力。CPT-Se4 降低 GSH/GSSG 比率和总硫醇，提高 Hep G2 细胞中的 ROS 水平，并最终诱导癌细胞凋亡 (apoptosis)。CPT-Se4 对 HeLa、Hep G2、A549 和 SMMC-7721 细胞具有细胞毒性（IC50=2.54-6.4 μM）。

CPT-Se4

CPT-Se4 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

CPT-Se4, a selenoprodrug of Camptothecin (CPT), shows improved potency in killing cancer cells and inhibiting tumor growth. CPT-Se4 decreases the GSH/GSSG ratio and total thiols, elevates the ROS level in Hep G2 cells, and eventually induces apoptosis of cancer cells. CPT-Se4 shows cytotoxicity against HeLa, Hep G2, A549, and SMMC-7721 cells (IC50= 2.54-6.4 μM)[1].

分子量

622.39

Formula

C25H24N2O7Se2
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]. Zhao J, et al. Integration of a Diselenide Unit Generates Fluorogenic Camptothecin Prodrugs with Improved Cytotoxicity to Cancer Cells. J Med Chem. 2021;64(24):17979-17991.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

CPT-Se3

发表于由

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。

CPT-Se3 

CPT-Se3 是喜树碱 (CPT) 的一种含硒前体药物，在杀死癌细胞和抑制肿瘤生长方面表现出更高的效力。CPT-Se3 降低 GSH/GSSG 比率和总硫醇，提高 Hep G2 细胞中的 ROS 水平，并最终诱导癌细胞凋亡 (apoptosis)。CPT-Se3 对 HeLa、Hep G2、A549 和 SMMC-7721 细胞具有细胞毒性（IC50= 2.19-4.7 μM）。

CPT-Se3

CPT-Se3 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

CPT-Se3, a selenoprodrug of Camptothecin (CPT), shows improved potency in killing cancer cells and inhibiting tumor growth. CPT–Se3 decreases the GSH/GSSG ratio and total thiols, elevates the ROS level in Hep G2 cells, and eventually induces apoptosis of cancer cells. CPT-Se3 shows cytotoxicity against HeLa, Hep G2, A549, and SMMC-7721 cells (IC50= 2.19-4.7 μM)[1].

分子量

590.35

Formula

C24H20N2O6Se2
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]. Zhao J, et al. Integration of a Diselenide Unit Generates Fluorogenic Camptothecin Prodrugs with Improved Cytotoxicity to Cancer Cells. J Med Chem. 2021;64(24):17979-17991.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

CPT-Se4

发表于由

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。

CPT-Se4 

CPT-Se4 是喜树碱 (CPT) 的一种含硒前体药物，在杀死癌细胞和抑制肿瘤生长方面表现出更高的效力。CPT-Se4 降低 GSH/GSSG 比率和总硫醇，提高 Hep G2 细胞中的 ROS 水平，并最终诱导癌细胞凋亡 (apoptosis)。CPT-Se4 对 HeLa、Hep G2、A549 和 SMMC-7721 细胞具有细胞毒性（IC50=2.54-6.4 μM）。

CPT-Se4

CPT-Se4 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

CPT-Se4, a selenoprodrug of Camptothecin (CPT), shows improved potency in killing cancer cells and inhibiting tumor growth. CPT-Se4 decreases the GSH/GSSG ratio and total thiols, elevates the ROS level in Hep G2 cells, and eventually induces apoptosis of cancer cells. CPT-Se4 shows cytotoxicity against HeLa, Hep G2, A549, and SMMC-7721 cells (IC50= 2.54-6.4 μM)[1].

分子量

622.39

Formula

C25H24N2O7Se2
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]. Zhao J, et al. Integration of a Diselenide Unit Generates Fluorogenic Camptothecin Prodrugs with Improved Cytotoxicity to Cancer Cells. J Med Chem. 2021;64(24):17979-17991.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

CPT-Se3

发表于由

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。

CPT-Se3 

CPT-Se3 是喜树碱 (CPT) 的一种含硒前体药物，在杀死癌细胞和抑制肿瘤生长方面表现出更高的效力。CPT-Se3 降低 GSH/GSSG 比率和总硫醇，提高 Hep G2 细胞中的 ROS 水平，并最终诱导癌细胞凋亡 (apoptosis)。CPT-Se3 对 HeLa、Hep G2、A549 和 SMMC-7721 细胞具有细胞毒性（IC50= 2.19-4.7 μM）。

CPT-Se3

CPT-Se3 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

CPT-Se3, a selenoprodrug of Camptothecin (CPT), shows improved potency in killing cancer cells and inhibiting tumor growth. CPT–Se3 decreases the GSH/GSSG ratio and total thiols, elevates the ROS level in Hep G2 cells, and eventually induces apoptosis of cancer cells. CPT-Se3 shows cytotoxicity against HeLa, Hep G2, A549, and SMMC-7721 cells (IC50= 2.19-4.7 μM)[1].

分子量

590.35

Formula

C24H20N2O6Se2
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]. Zhao J, et al. Integration of a Diselenide Unit Generates Fluorogenic Camptothecin Prodrugs with Improved Cytotoxicity to Cancer Cells. J Med Chem. 2021;64(24):17979-17991.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

CPT-Se4

发表于由

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。

CPT-Se4 

CPT-Se4 是喜树碱 (CPT) 的一种含硒前体药物，在杀死癌细胞和抑制肿瘤生长方面表现出更高的效力。CPT-Se4 降低 GSH/GSSG 比率和总硫醇，提高 Hep G2 细胞中的 ROS 水平，并最终诱导癌细胞凋亡 (apoptosis)。CPT-Se4 对 HeLa、Hep G2、A549 和 SMMC-7721 细胞具有细胞毒性（IC50=2.54-6.4 μM）。

CPT-Se4

CPT-Se4 Chemical Structure

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生物活性

CPT-Se4, a selenoprodrug of Camptothecin (CPT), shows improved potency in killing cancer cells and inhibiting tumor growth. CPT-Se4 decreases the GSH/GSSG ratio and total thiols, elevates the ROS level in Hep G2 cells, and eventually induces apoptosis of cancer cells. CPT-Se4 shows cytotoxicity against HeLa, Hep G2, A549, and SMMC-7721 cells (IC50= 2.54-6.4 μM)[1].

分子量

622.39

Formula

C25H24N2O7Se2
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]. Zhao J, et al. Integration of a Diselenide Unit Generates Fluorogenic Camptothecin Prodrugs with Improved Cytotoxicity to Cancer Cells. J Med Chem. 2021;64(24):17979-17991.

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

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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 (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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Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥500 In-stock
100 mg ￥395 In-stock
500 mg ￥1252 In-stock
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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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CU-CPT22

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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。

CU-CPT22  纯度: 98.61%

CU-CPT22 是一种有效的 toll 样受体 1 和 2 (TLR1/2) 蛋白复合物抑制剂，可与 TLR1/2 结合的合成三酰脂蛋白 (Pam3CSK4) 竞争，Ki 值为 0.41 µM。 CU-CPT22 阻断 Pam3CSK4 诱导的 TLR1/2 激活，IC50 值为 0.58 µM。

CU-CPT22

CU-CPT22 Chemical Structure

CAS No. : 1416324-85-0

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生物活性

CU-CPT22 is a potent protein complex of toll-like receptor 1 and 2 (TLR1/2) inhibitor, and competes with the synthetic triacylated lipoprotein (Pam3CSK4) binding to TLR1/2 with a Ki of 0.41 µM. CU-CPT22 blocks Pam3CSK4-induced TLR1/2 activation with an IC50 of 0.58 µM[1].

IC50 & Target

Ki: 0.41 μM (TLR1/2)[1]
体外研究
(In Vitro)

CU-CPT22 is a toll-like receptor 1 and 2 (TLR1/2) inhibitor with an IC50 of 0.58±0.09 µM. It is demonstrated that CU-CPT22 is able to compete with Pam3CSK4 for binding to TLR1/2 with an inhibition constant (Ki) of 0.41±0.07 µM, which is consistent with its potency observed in the whole cell assay. Increasing the concentration of CU-CPT22 to 6 µM decreases the anisotropy to background levels. It is found that CU-CPT22 inhibits TLR1/2 signaling without affecting other TLRs, showing it is highly selective in intact cells. CU-CPT22 is found to have no significant cytotoxicity at various concentrations up to 100 µM in RAW 264.7 cells. The result demonstrates that CU-CPT22 can inhibit about 60% of TNF-αand 95% of IL-1β at 8 µM[1].

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.
分子量

362.37

Formula

C19H22O7
CAS 号

1416324-85-0
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 : ≥ 125 mg/mL (344.95 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7596 mL 13.7981 mL 27.5961 mL
5 mM 0.5519 mL 2.7596 mL 5.5192 mL
10 mM 0.2760 mL 1.3798 mL 2.7596 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。

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： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.90 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.90 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (6.90 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (6.90 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: 2.5 mg/mL (6.90 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (6.90 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Cheng K, et al. Discovery of small-molecule inhibitors of the TLR1/TLR2 complex. Angew Chem Int Ed Engl. 2012 Dec 3;51(49):12246-9.
Kinase Assay
[1]

RAW 264.7 cells are planted in 6-well plates at 1,000,000 cells per well with 3 mL of medium and grown for 24 h at 37°C in a 5% CO2 humidified incubator. After 24 h, non-adherent cells and media are removed and replaced with fresh RPMI 1640 medium (3 mL/well). Two wells of adherent macrophages are treated with Pam3CSK4 (300 ng/mL) as the positive control, two wells are treated with 8 μM CU-CPT22, and the other two wells are treated with 8 μM compound DMSO. Plates are then incubated for an additional 24 h. The medium is removed, the cells are washed with PBS (3×1 mL), the plate is put on ice, then 500 μL of lysis buffer is added to each well. The production of the cytokine interleukin-1β (IL-1β) and TNF-α is quantified with enzyme-linked immunosorbent assays (ELISA). The cytokine level in each sample is determined in duplicate[1].

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.
参考文献

  • [1]. Cheng K, et al. Discovery of small-molecule inhibitors of the TLR1/TLR2 complex. Angew Chem Int Ed Engl. 2012 Dec 3;51(49):12246-9.

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