Catalog No.S1288

Camptothecin is a specific inhibitor of DNA topoisomerase I (Topo I) with IC50 of 0.68 μM in a cell-free assay. Phase 2.

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Camptothecin Chemical Structure

Camptothecin Chemical Structure
Molecular Weight: 348.35

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Product Description

Biological Activity

Description Camptothecin is a specific inhibitor of DNA topoisomerase I (Topo I) with IC50 of 0.68 μM in a cell-free assay. Phase 2.
Targets Topo I [2]
(Cell-free assay)
IC50 0.68 μM
In vitro Camptothecin, a plant alkaloid orignially isolated from Camptotheca acuminate in 1966. [1] Camptothecin is noted to halt cells during the S phase of mitosis. Camptothecin 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, Camptothecin induces apoptosis in primary mouse hepatocytes, with an IC50 value of 13 μM. Camptothecin 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, Camptothecin (5 μM) induces proteasome-mediated degradation of mixed lineage leukemia 5 (MLL5) protein, which leads to phosphorylation of p53 at Ser392. [5] Due to the low solubility and adverse effects of Camptothecin, various Camptothecin analogues have been developed, and two of them, topotecan and irinotecan, has been approved by FDA and are used in cancer chemotherapy.
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
P388CPT5 RMnPJS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?NF7sVnpKSzVyPUKuPEDPxE1?M1vqUlExOzR4OUOz
KBV-1 + MDR1MmL4Z5l1d3SxeHnjbZR6KGG|c3H5MlLRglExKM7:TR?=NVHiN3NuUUN3ME20OFAhdk1?M2[0VFE2PDh{OUK5
CRL 7065MnHJZ5l1d3SxeHnjbZR6KGG|c3H5NVLGO2VjUUN3ME20NFAhdk1?NYP0TVlbOTd{NUS2Olk>

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In vivo Camptothecin (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 Camptothecin (50 mg/kg) and TNF (5 and 7 μg/kg), but not Camptothecin alone, induces liver damage. [4]

Protocol(Only for Reference)

Kinase Assay: [2]

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. Camptothecin 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 obtaine

Cell Assay: [2]

Cell lines U87MG, A549 and H838 cells
Concentrations 0.17 nM–10 mM
Incubation Time 48 hours
Method 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 for 48 hours and then with fresh medium for 48 hours. Camptothecin 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.

Animal Study: [3]

Animal Models Nude mice (NIH-I high fertility strain) bearing xenografts of CASE, SW48, DOY, SPA, and CLO cells
Formulation Finely grounded and dispersed in intralipid 20% at 1 mg/mL by sonication
Dosages 0–8 mg/kg
Administration Administered via i.m. or i.v. injection

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[1] Wall ME, et al. J Am Chem Soc, 1966, 88 (16), 3888–3890.

[2] Luzzio MJ, et al. J Med Chem, 1995, 38(3), 395-401.

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Clinical Trial Information( data from, updated on 2016-06-25)

NCT Number Recruitment Conditions Sponsor
Start Date Phases
NCT01803269 Terminated Extensive Stage Small Cell Lung Cancer|Recurrent Small Cell Lung Cancer University of Chicago|National Cancer Institute (NCI) January 2013 Phase 2
NCT01612546 Completed Adenocarcinoma of the Esophagus|Adenocarcinoma of the Gastroesophageal Junction|Diffuse Adenocarcinoma of the Stomach|Intestinal Adenocarcinoma of  ...more Adenocarcinoma of the Esophagus|Adenocarcinoma of the Gastroesophageal Junction|Diffuse Adenocarcinoma of the Stomach|Intestinal Adenocarcinoma of the Stomach|Mixed Adenocarcinoma of the Stomach|Recurrent Esophageal Cancer|Recurrent Gastric Cancer|Squamous Cell Carcinoma of the Esophagus|Stage IIIB Esophageal Cancer|Stage IIIB Gastric Cancer|Stage IIIC Esophageal Cancer|Stage IIIC Gastric Cancer|Stage IV Esophageal Cancer|Stage IV Gastric Cancer City of Hope Medical Center|National Cancer Institute (NCI) November 2012 --
NCT01202370 Completed Solid Malignancies University of Kentucky|Arno Therapeutics September 2010 Phase 1
NCT01124539 Active, not recruiting Glioblastoma Multiforme|GBM|Gliosarcoma Arno Therapeutics December 2009 Phase 2
NCT00956787 Recruiting Myelodysplastic Syndrome Arno Therapeutics June 2009 Phase 2

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Chemical Information

Download Camptothecin SDF
Molecular Weight (MW) 348.35


CAS No. 7689-03-4
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms NSC-100880
Solubility (25°C) * In vitro DMSO 3 mg/mL (8.61 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 30 mg/mL
* <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.
Chemical Name  (4S)​-4-​ethyl-​4-​hydroxy-1H-​pyrano[3',​4':6,​7]​indolizino[1,​2-​b]​quinoline-​3,​14(4H,​12H)​-​dione

Customer Product Validation(3)

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Source EMBO Rep 2010 11(12), 962-8. Camptothecin purchased from Selleck
Method Colony formation assays
Cell Lines U2OS cells
Concentrations 1 nM-1 Um
Incubation Time 1-24 h
Results We observed apartial, but statistically significant rescue of sensitivity at lowcamptothecin concentrations by simultaneous downregulationof CtIP and EXO1 (A,B). Consistent with this, we found asimilar increase in survival on chronic treatment with camptothecin (C).

Click to enlarge
Source EMBO Rep 2010 11(12), 962-8. Camptothecin purchased from Selleck
Method Western blot
Cell Lines U2OS cells
Concentrations 1 uM
Incubation Time 1 h
Results By analysing S2056 autophosphorylation, we observed increased DNA-PKcs activation particularly in doubly depleted cells, and the signal wasfurther amplified in response to camptothecin.

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Source PLoS One 2014 9(7), e101844. Camptothecin purchased from Selleck
Method Clonogenic assay
Cell Lines HEY cells
Concentrations 1.25 nM
Incubation Time
Results Treating the HEY cells with a Topoisomerase I inhibitor Camptothecin (CPT), further suppressed the cell survival of the UBE2M knockdown cells, compared to control cells.

Tech Support

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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