Camptothecin

Camptothecin is a specific inhibitor of DNA topoisomerase I (Topo I) with IC50 of 0.68 μM. Phase 2.

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Camptothecin Chemical Structure

Camptothecin Chemical Structure
Molecular Weight: 348.35

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Product Information

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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. Phase 2.
Targets DNA topoisomerase I (topo I)
IC50 0.68 μM [2]
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.
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]
Features

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
Dosages 0–8 mg/kg
Administration Administered via i.m. or i.v. injection
Solubility 30% PEG400/0.5% Tween80/5% propylene glycol, 30 mg/mL
1

References

Clinical Trial Information( data from http://clinicaltrials.gov)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT01803269 Recruiting Extensive Stage Small Cell Lung Cancer|Recurrent Small Cell Lung Cancer University of Chicago|National Cancer Institute (NCI) 2013-01 Phase 2
NCT01814501 Recruiting Mucinous Adenocarcinoma of the Colon|Mucinous Adenocarcinoma of the Rectum|Recurrent Colon Cancer|Recurrent Rectal Cancer|Signet Ring Adenocarcinoma of the Colon|Signet Ring Adenocarcinoma of the Rectum etc. Ohio State University Comprehensive Cancer Center|Christina Wu|Amgen 2013-02 Phase 2
NCT01767194 Not yet recruiting Neuroblastoma Children's Oncology Group|National Cancer Institute (NCI) 2013-03 Phase 2
NCT01835041 Recruiting Acinar Cell Adenocarcinoma of the Pancreas|Duct Cell Adenocarcinoma of the Pancreas|Recurrent Pancreatic Cancer|Stage IV Pancreatic Cancer Comprehensive Cancer Center of Wake Forest University|National Cancer Institute (NCI) 2013-04 Phase 1
NCT01821612 Recruiting Acinar Cell Adenocarcinoma of the Pancreas|Duct Cell Adenocarcinoma of the Pancreas|Recurrent Pancreatic Cancer|Stage II Pancreatic Cancer|Stage III Pancreatic Cancer Alliance for Clinical Oncology Trials|National Cancer Institute (NCI) 2013-05

Chemical Information

Download Camptothecin SDF
Molecular Weight (MW) 348.35
Formula

C20H16N2O4

CAS No. 7689-03-4
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Syonnyms N/A
Solubility (25°C) * In vitro DMSO 3 mg/mL (8 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.
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Customer Reviews (2)


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Rating
Source EMBO Rep. 2010 Dec;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 a partial, but statistically significant rescue of sensitivity at low camptothecin concentrations by simultaneous downregulation of CtIP and EXO1 (A,B). Consistent with this, we found a similar increase in survival on chronic treatment with camptothecin (C).

Click to enlarge
Rating
Source EMBO Rep. 2010 Dec;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 was further amplified in response to camptothecin .

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