Camptothecins
Camptothecins act through DNA topoisomerase I (Top1), an enzyme essential for DNA replication and transcription[1][2]. Mechanistically, camptothecin, topotecan, and irinotecan stabilize Top1-DNA cleavable complexes, block DNA resealing, and generate replication-associated DNA double-strand breaks[3][4]. This Top1-focused mechanism distinguishes camptothecins from Top2 inhibitors, which can induce DNA damage in both replicating and non-replicating cells[3]. In intact cells, topotecan-induced Top1-DNA covalent complexes can be detected by immunoblotting, immunofluorescence, or flow cytometry, supporting mechanism-based pharmacodynamic analysis[5]. In cancer models, ATR inhibition sensitizes cells to camptothecin-class Top1 inhibitors by disabling DNA replication initiation and fork elongation responses[6]. Camptothecin derivatives also poison Leishmania DNA topoisomerase IB and reduce parasitic burden in infected splenocytes[7]. For colorectal cancer research, SN-38 suppresses Nrf2 transcriptional activity and can enhance sensitivity to Nrf2-sensitive anticancer drugs[8].
References:
- [1]. Wang W, et al. The optimal choice for pancreatic anastomosis after pancreaticoduodenectomy: A network meta-analysis of randomized control trials. Int J Surg. 2018 Sep;57:111-116. [Content Brief]
- [2]. Jain CK, et al. Natural Compounds as Anticancer Agents Targeting DNA Topoisomerases. Curr Genomics. 2017 Feb;18(1):75-92. [Content Brief]
- [3]. Zhao H, et al. Relationship of DNA Damage Signaling to DNA Replication Following Treatment with DNA Topoisomerase Inhibitors Camptothecin/Topotecan, Mitoxantrone, or Etoposide. Cytometry A. 2011 Dec 2;79A:21172. [Content Brief]
- [4]. Yakkala PA, et al. Prospects of Topoisomerase Inhibitors as Promising Anti-Cancer Agents. Pharmaceuticals (Basel). 2023 Oct 13;16(10):1456. [Content Brief]
- [5]. Patel AG, et al. Immunodetection of human topoisomerase I-DNA covalent complexes. Nucleic Acids Res. 2016 Apr 7;44(6):2816-26. [Content Brief]
- [6]. Jossé R, et al. ATR inhibitors VE-821 and VX-970 sensitize cancer cells to topoisomerase i inhibitors by disabling DNA replication initiation and fork elongation responses. Cancer Res. 2014 Dec 1;74(23):6968-79. [Content Brief]
- [7]. Prada CF, et al. Gimatecan and other camptothecin derivatives poison Leishmania DNA-topoisomerase IB leading to a strong leishmanicidal effect. Biochem Pharmacol. 2013 May 15;85(10):1433-40. [Content Brief]
- [8]. Wang J, et al. SN-38, an active metabolite of irinotecan, inhibits transcription of nuclear factor erythroid 2-related factor 2 and enhances drug sensitivity of colorectal cancer cells. Mol Carcinog. 2024 Apr;63(4):742-756. [Content Brief]
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Camptothecins Related Products (42)
Related Products (42)
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Exatecan Intermediate 2 hydrochloride
0 ImagesExatecan Intermediate 2 hydrochloride (Compound B) is an intermediate of Exatecan (DX-8951, HY-13631). Exatecan is an anticancer agent belonging to the class of camptothecin analogs. Exatecan interferes with the proliferation and division of tumor cells by interacting with DNA, thereby inhibiting tumor growth. Exatecan is primarily used for research of a variety of cancers including ovarian, lung and breast cancers.
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Exatecan Intermediate 4
0 ImagesExatecan Intermediate 4 (Compound 14f) is an intermediate of Exatecan (DX-8951, HY-13631). Exatecan is an anticancer agent belonging to the class of camptothecin analogs. Exatecan interferes with the proliferation and division of tumor cells by interacting with DNA, thereby inhibiting tumor growth. Exatecan is primarily used for research of a variety of cancers including ovarian, lung and breast cancers.
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Exatecan Intermediate 3
0 ImagesExatecan Intermediate 3 is the intermediate of Exatecan (HY-13631) And Exatecan (DX-8951) is a DNA topoisomerase I inhibitor with an IC50 value of 2.2 μM (0.975 μg/mL) that can be used in cancer research. Exatecan Intermediate 3 can be used to synthesize Antibody-Drug Conjugates (ADCs).
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Exatecan Intermediate 7
0 ImagesCat. No.: HY-45157CAS No.: 182182-32-7Exatecan Intermediate 7 is the intermediate of Exatecan (HY-13631) And Exatecan (DX-8951) is a DNA topoisomerase I inhibitor with an IC50 value of 2.2 μM (0.975 μg/mL) that can be used in cancer research. Exatecan Intermediate 7 can be used to synthesize Antibody-Drug Conjugates (ADCs).
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Exatecan-methylacetamide-OH
0 ImagesCat. No.: HY-156849CAS No.: 2594423-51-3Exatecan-methylacetamide-OH (compound 6) is a Exatecan derivative with anticancer effects. Exatecan-methylacetamide-OH is an ADC cytotoxin that can be used to synthesize Antibody-Drug Conjugates (ADCs) (CN112125915A; compound 6).
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Exatecan-amide-cyclopropanol
0 ImagesExatecan-amide-cyclopropanol (compound 1) is a anticancer agent. Exatecan-amide-cyclopropanol shows anti-proliferation activity against SK-BR-3 and U87 cells, with IC50 values of 0.12 and 0.23 nM, respectively.
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Exatecan Intermediate 4 dihydrochloride
0 ImagesCat. No.: HY-W021377CPurity: 99.92%Exatecan Intermediate 4 dihydrochloride (Compound 14f) is an intermediate of Exatecan (DX-8951, HY-13631). Exatecan is an anticancer agent belonging to the class of camptothecin analogs. Exatecan interferes with the proliferation and division of tumor cells by interacting with DNA, thereby inhibiting tumor growth. Exatecan is primarily used for research of a variety of cancers including ovarian, lung and breast cancers.
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Top1 inhibitor 1
0 ImagesTop1 inhibitor 1 (compound 28) is a potent human topoisomerase I (Top1) inhibitor with an IC50 value of 29 nM.
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(5-Cl)-Exatecan
0 ImagesCat. No.: HY-160806CAS No.: 2813268-66-3(5-Cl)-Exatecan is a derivative of Exatecan (HY-13631) and a DNA topoisomerase inhibitor. (5-Cl)-Exatecan serves as the cytotoxic payload component in antibody-drug conjugates (ADC) targeting ROR1-positive cancers. (5-Cl)-Exatecan is applicable for the research of ROR1-positive cancers.
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Exatecan mesylate dihydrate
0 ImagesCat. No.: HY-13631PCAS No.: 197720-53-9Synonyms: DX-8951 mesylate dihydrateExatecan (DX-8951) mesylate dihydrate is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research.
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Gly-Cyclopropane-Exatecan
0 ImagesCat. No.: HY-148696ACAS No.: 2414254-49-0Gly-Cyclopropane-Exatecan involves in the synthesis of anti-B7-H4 ADC, containing Exatecan (HY-13631), a DNA Topoisomerase I inhibitor. Gly-Cyclopropane-Exatecan participated in the formation of the ADC hu2F7-Exatecan (compound 34), which showed antitumor activity in vivo and in vitro.
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Exatecan-amide-bicyclo[1.1.1]pentan-1-ylmethanol
![Exatecan-amide-bicyclo[1.1.1]pentan-1-ylmethanol](https://file.medchemexpress.com/product_pic/hy-160598.gif "Click to View Exatecan-amide-bicyclo[1.1.1]pentan-1-ylmethanol Product Detail")
0 ImagesCat. No.: HY-160598CAS No.: 2891774-71-1Exatecan-amide-bicyclo[1.1.1]pentan-1-ylmethanol (compound 45) is a camptothecin compound that can inhibit cell proliferation, with an IC50 of 2.92 ng/mL for MDA‑MB‑468 cells. Exatecan-amide-bicyclo[1.1.1]pentan-1-ylmethanol can be used for the research of cancer.
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Exatecan-amide-bicyclo[1.1.1]pentan-1-ol
![Exatecan-amide-bicyclo[1.1.1]pentan-1-ol](https://file.medchemexpress.com/product_pic/hy-160597.gif "Click to View Exatecan-amide-bicyclo[1.1.1]pentan-1-ol Product Detail")
0 ImagesCat. No.: HY-160597CAS No.: 2866299-06-9
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(1-OH)-Exatecan
0 ImagesCat. No.: HY-156642CAS No.: 2894780-53-9(1-OH)-Exatecan is a quinoline ring compound. (1-OH)-Exatecan has substantial antiproliferative effects. (1-OH)-Exatecan can be used for cancer diseases research.
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Exatecan analogue 1
0 ImagesCat. No.: HY-157795CAS No.: 2671770-58-2Exatecan analogue 1 (Icp-3) is a Exatecan (HY-13631) analogue. Exatecan analogue 1 can be used in the synthesis of antibody-drug conjugates (ADCs)
