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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Customer Reviews(2)

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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 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
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
Solubility 30% PEG400/0.5% Tween80/5% propylene glycol, , 30 mg/mL
* 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.
1

References

[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 http://clinicaltrials.gov)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02060955 Recruiting Glioblastoma Multiforme CytoVac A/S 2014-02 Phase 2
NCT02095132 Not yet recruiting Recurrent Childhood Medulloblastoma|Recurrent Childhood Supratentorial Primitive Neuroectodermal Tumor|Recurrent Neuroblastoma|Unspecified Childhood Solid Tumor, Protocol Specific National Cancer Institute (NCI) 2014-03 Phase 1|Phase 2
NCT01921751 Not yet recruiting Acinar Cell Adenocarcinoma of the Pancreas|Duct Cell Adenocarcinoma of the Pancreas|Stage III Pancreatic Cancer Radiation Therapy Oncology Group|National Cancer Institute (NCI) 2014-03 Phase 2
NCT02049593 Not yet recruiting Metastatic Cancer|Unspecified Adult Solid Tumor Jonsson Comprehensive Cancer Center|Translational Research in Oncology-US (TRIO-US) 2014-04 Phase 1
NCT02055196 Not yet recruiting Adult Anaplastic Astrocytoma|Adult Anaplastic Oligodendroglioma|Adult Giant Cell Glioblastoma|Adult Glioblastoma|Adult Gliosarcoma|Recurrent Adult Brain Tumor City of Hope Medical Center|National Cancer Institute (NCI) 2014-06 Phase 1

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
Synonyms NSC-100880
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.

Research Area

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 .

Product Citations (1)

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