Camptothecin (CPT)

製品コードS1288 バッチS128804

印刷

化学情報

Chemical Structure Synonyms Campathecin, (S)-(+)-Camptothecin,NSC-100880 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C20H16N2O4
分子量 348.35 CAS No. 7689-03-4
Solubility (25°C)* 体外 DMSO 2 mg/mL (5.74 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Camptothecin (CPT) is a specific inhibitor of DNA topoisomerase I (Topo I) with IC50 of 0.68 μM in a cell-free assay. Camptothecin induces apoptosis in cancer cells via microRNA-125b-mediated mitochondrial pathways. Phase 2.
in vitro Camptothecin (CPT), a plant alkaloid originally isolated from *Camptotheca acuminate* in 1966,[1] is noted to halt cells during the S phase of mitosis. This compound displays nanomolar potency in cytotoxicity against many human tumor cell lines, including HT29, LOX, SKOV3, and SKVLB, with IC50 values ranging from 37 nM to 48 nM.[2] In combination with TNF, it induces apoptosis in primary mouse hepatocytes, with an IC50 value of 13 μM. It also abrogated the TNF-induced NF-κB activation, as well as the expression of TNF-receptor associated factor 2 (TRAF2), X-linked inhibitor of apoptosis protein (X-IAP), and FLICE-inhibitory protein (FLIP).[4] In HCT116 cells, CPT (5 μM) induces proteasome-mediated degradation of mixed lineage leukemia 5 (MLL5) protein, which leads to phosphorylation of p53 at Ser392.[5] Due to its low solubility and adverse effects, various analogues have been developed, and two of them, topotecan and irinotecan, have been approved by the FDA and are used in cancer chemotherapy.
in vivo Camptothecin (CPT) (8 mg/kg) displays complete growth inhibition and regression in mice xenografts of various tumors, including colon, lung, breast, stomach, and ovary tumors. [3] In mice, combinations of this compound (50 mg/kg) and TNF (5 and 7 μg/kg), but not it alone, induces liver damage. [4]

プロトコル(参考用のみ)

キナーゼアッセイ Topoisomerase I Cleavable Complex Assay
Topoisomerase I is isolated from calf thymus and is devoid of topoisomerase II. All reactions are carried out in 10 mL volumes of reaction buffer (50 mM Tris-HCl, pH 7.5, 100 mM KCl, 0.5 mM EDTA, and 30 pg/mL BSA) in microtiter plates. This compound is dissolved in DMSO at 10 mg/mL and serially diluted in 96-well microtiter plates to which the 32P end-labeled pBR322 DNA and topoisomerase enzyme are added. The reaction mixture is incubated at room temperature for 30 min and then the reaction stopped by adding 2 mL of a mixture of sodium dodecyl sulfate and proteinase K (1.6% and 0.14 mg/mL final concentrations, respectively). The plates are heated at 50 °C for 30 min, 10 mL of standard stop mixture containing 0.45 N NaOH is added in order to generate single-stranded DNA, and the samples are electrophoresed in 1.5% agarose gels in TBE buffer. Gels are blotted on nitrocellulose paper, dried, and exposed to X-ray film. The units of cleavage are calculated from the autoradiographs and plotted against the log drug concentration. The IC50 values are then obtained. Camptothecin (CPT) is used as the test compound.
細胞アッセイ 細胞株 U87MG, A549 and H838 cells
濃度 0.17 nM–10 mM
反応時間 48 hours
実験の流れ Tumor cells are plated in 100 μL of medium in 96-well microtiter plates at a density of 1500 to 4000 cells per well and allowed to adhere overnight. Cells are incubated with Camptothecin (CPT) for 48 hours and then with fresh medium for 48 hours. This compound at each concentration is added in quadruplicate. Following a 4-hour incubation of treated cells with MTT, the reduced dye product is extracted from the cells with 0.2 mL of DMSO followed by 50 μL of Sorensen's buffer. The plates are shaken briefly, and the absorbance at 570 nm is read and quantitated. Curves are fitted to the MTT assay data using a four-parameter logistic equation.
動物実験 動物モデル Nude mice (NIH-I high fertility strain) bearing xenografts of CASE, SW48, DOY, SPA, and CLO cells
投薬量 0–8 mg/kg
投与方法 Administered via i.m. or i.v. injection

参考

  • http://pubs.acs.org/doi/abs/10.1021/ja00968a057
  • https://pubmed.ncbi.nlm.nih.gov/7853331/
  • https://pubmed.ncbi.nlm.nih.gov/2032244/
  • https://pubmed.ncbi.nlm.nih.gov/15122760/
  • https://pubmed.ncbi.nlm.nih.gov/21423215/

カスタマーフィードバック

Data from [Data independently produced by PLoS One, 2014, 9(7), e101844]

Data from [EMBO Rep, 2010, 11(12), 962-8]

Data from [EMBO Rep, 2010, 11(12), 962-8]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Non-canonical functions of DNMT3A in hematopoietic stem cells regulate telomerase activity and genome integrity [ Cell Stem Cell, 2025, S1934-5909(25)00256-5] PubMed: 40680747
Inherited deficiency of DIAPH1 identifies a DNA double strand break repair pathway regulated by γ-actin [ Nat Commun, 2025, 16(1):4491] PubMed: 40368919
A novel biosensor for the spatiotemporal analysis of STING activation during innate immune responses to dsDNA [ EMBO J, 2025, 10.1038/s44318-025-00370-y] PubMed: 39984755
DSCC1 restrains 53BP1/RIF1 signaling at DNA double-strand breaks to promote homologous recombination repair [ Cell Rep, 2025, 44(4):115452] PubMed: 40117291
Steroid-Modulated Transcription Synergistically Forms DNA Double-Strand Breaks With Topoisomerase II Inhibitor [ Cancer Sci, 2025, 10.1111/cas.70081] PubMed: 40231641
The novel role of LCK and other PcDEGs in the diagnosis and prognosis of sepsis: Insights from bioinformatic identification and experimental validation [ Int Immunopharmacol, 2025, 149:114194] PubMed: 39904039
The Kinase Inhibitor GNF-7 Is Synthetically Lethal in Topoisomerase 1-Deficient Ewing Sarcoma [ Cancers (Basel), 2025, 17(15)2475] PubMed: 40805174
Peroxiredoxin 1 inhibits tumorigenesis by activating the NLRP3/GSDMD pathway to induce pyroptosis of colorectal cancer cells [ World J Gastroenterol, 2025, 31(36):111557] PubMed: 41025079
Discovery and Characterization of Small Molecule Inhibitors Targeting Exonuclease 1 for Homologous Recombination-Deficient Cancer Therapy [ ACS Chem Biol, 2025, 10.1021/acschembio.5c00117] PubMed: 40378357
DDX18 influences chemotherapy sensitivity in colorectal cancer by regulating genomic stability [ Exp Cell Res, 2025, 444(1):114344] PubMed: 39577603

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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