Camptothecin

Catalog No.S1288 Synonyms: NSC-100880

Camptothecin Chemical Structure

Molecular Weight(MW): 348.35

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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3 Customer Reviews

  • CtIP and exonuclease 1 protect cells from chromosomal damage. (A) At 72 h after transfection with the indicated siRNA oligonucleotides, U2OS cells were treated with either DMSO or camptothecin (1 h, 1 μM; acute treatment) and survival was determined by colony formation. Data represent the mean±s.e.m. of five independent experiments. (B) Cell survival at low doses of camptothecin from the data shown in (A). Data represent the mean±s.e.m. of five independent experiments. (C) Cells transfected as in (A) were treated with either DMSO or camptothecin for 24 h (chronic treatment) and survival was determined by colony formation. Data represent the mean±s.e.m. of three independent experiments. (D) Metaphase spreads from cells transfected and treated as described in (A) were analysed for chromosomal aberrations. A total of 50 metaphase spreads was analysed for each sample. The percentages of metaphase spreads displaying the indicated numbers of radial chromosomes are shown. CNTL, control; DMSO, dimethyl sulphoxide; EXO1, exonuclease 1; siRNA, small interfering RNA.

    EMBO Rep 2010 11(12), 962-8. Camptothecin purchased from Selleck.

    U2OS cells transfected with siRNA oligonucleotides were treated with DMSO or camptothecin (1 μM, 1 h) and DNA-PKcs autophosphorylation at S2056 was monitored. Arrow indicates the hyperphosphorylated form of CtIP.

    EMBO Rep 2010 11(12), 962-8. Camptothecin purchased from Selleck.

  • Growth suppression by UBE2M silencing is enhanced by DNA damaging agents. Growth sensitivity of HEY cells in the presence of Camptothecin(CPT) was monitored using clonogenic assay.

    PLoS One 2014 9(7), e101844. Camptothecin purchased from Selleck.

Purity & Quality Control

Choose Selective Topoisomerase Inhibitors

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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)
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 Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SKOV3 NVvKflhR[3m2b4TvfIlkcXS7IHHzd4F6 Mo\GTWM2OD13MTDuUS=> NGixboc6ODB|NUKw
SKVLB M4nhUYN6fG:2b4jpZ4l1gSCjc4PhfS=> NFOwZZpKSzVyPUWzJI5O NYnqW3BTQTByM{WyNC=>
HT29 NYHQd252[3m2b4TvfIlkcXS7IHHzd4F6 M4DNSmlEPTB;OEeuPEBvVQ>? NFG4V4g6ODB|NUKw
KB NFzZ[VZkgXSxdH;4bYNqfHliYYPzZZk> MmDNTWM2OD16IH7N M{PpVFkxODN3MkC=
A427 NHfsXHVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2S0Op4yKM7:TR?= NGSzZYFFVVOR NIrONo1KSzVyPUK0JI5O NFOwO5M6QDd4MUGx
PC-3 NIPBdGZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWT+NUDPxE1? MY\EUXNQ MWHJR|UxRTV5IH7N M{DXRlk5PzZzMUG=
K562adr NHr2XoNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXLwc3VvhjFizszN NWjYeIQ2TE2VTx?= NG\QcXdKSzVyPUW3JI5O NXPYVm5vQTh5NkGxNS=>
MCF7mdr Ml7qS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NUL5R3NEhjFizszN MXzEUXNQ MojnTWM2OD1|LkGgcm0> MmnlPVg4PjFzMR?=
P388 M1y2VGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mo\BTWM2OD1|MjDuUS=> Mnr6NVA{PDZ7M{O=
P388CPT5 R NILqWWdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYDJR|UxRTJwODFOwG0> NVzHflRGOTB|NE[5N|M>
KBwt NV65R4I6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MkHxTWM2OD12MDDuUS=> MoDGNVA1OTF2N{[=
KBMDR M2\PZWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGLEcI1KSzVyPUewJI5O MkDVNVA1OTF2N{[=
KBV20C NF\T[m5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M{H4cGlEPTB;M{Cgcm0> NGfYTHAyODRzMUS3Oi=>
KB7D M2D3XWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NV3UVohOUUN3ME2zOUBvVQ>? Mke3NVA1OTF2N{[=
KBCamp MVjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYHXeHVTUUN3ME2xMlA1KM7:TR?= NEnZUI0yODRzMUS3Oi=>
HT29 MlKxZ5l1d3SxeHnjbZR6KGG|c3H5 MYrJR|UxRThyIH7N Mo[2NVA5PDF6MEi=
A549 NVvSSZRL[3m2b4TvfIlkcXS7IHHzd4F6 M{TYeGlEPTB;Nkegcm0> NVj5SFB2OTB6NEG4NFg>
T24 MVrjfZRwfG:6aXPpeJkh[XO|YYm= NUnzOmI5UUN3ME24PEBvVQ>? NHv0dZkyODh2MUiwPC=>
HOP-62 NYXye2M6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVXJR|UxRTFyIH7N Mle1NVExOjB{OEO=
HCT-116 NH\4UlNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXXJR|UxRTNyIH7N M1O1TlEyODJyMkiz
SF-539 NWfJXop6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NEPNSnlKSzVyPUGwJI5O MYOxNVAzODJ6Mx?=
UACC-62 M1;kU2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGjYfnNKSzVyPUGwJI5O MoPUNVExOjB{OEO=
OVCAR-3 NI\U[GFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NYfPcFltUUN3ME2yNlAhdk1? M{XUbVEyODJyMkiz
SN12C NFnPOVdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NEm3cHhKSzVyPUKwJI5O MnXLNVExOjB{OEO=
DU-145 Ml;5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MlW0TWM2OD1zMDDuUS=> Ml\vNVExOjB{OEO=
MDA-MB-435 NF;6PIFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NYW2Z|BEUUN3ME20NEBvVQ>? M2m3SVEyODJyMkiz
WiDr NYHEO4Rw[3m2b4TvfIlkcXS7IHHzd4F6 MVzEUXNQ NEPL[|lKSzVyPUG3JI5O MlrsNVE{OzR3Nkm=
A549 MXHjfZRwfG:6aXPpeJkh[XO|YYm= M3rxWmROW09? MmqzTWM2OD1zNDDuUS=> NVznWllxOTF|M{S1Olk>
MKN45 NWPnTFNM[3m2b4TvfIlkcXS7IHHzd4F6 MoT1SG1UVw>? Mlf4TWM2OD1zNzDuUS=> MVmxNVM{PDV4OR?=
SK-OV-3 NGjpVpFkgXSxdH;4bYNqfHliYYPzZZk> MnnRSG1UVw>? M3fHXGlEPTB;MkCgcm0> NED0O4wyOTN|NEW2PS=>
H128 MkPiZ5l1d3SxeHnjbZR6KGG|c3H5 MoHJSG1UVw>? NXvrOVZYUUN3ME2xPEBvVQ>? MkDONVE{OzR3Nkm=
SK-BR-3 NHfTXXVkgXSxdH;4bYNqfHliYYPzZZk> NIPJeoFFVVOR NH\SXVhKSzVyPUKwJI5O M3jLfVEyOzN2NU[5
LX-1 M4K4XoN6fG:2b4jpZ4l1gSCjc4PhfS=> NGjEWpdFVVOR MXLJR|UxRTF{MDDuUS=> NInpTlYyOTh3OEezOy=>
HCT116 NYqzeo85[3m2b4TvfIlkcXS7IHHzd4F6 NYnHZmpLTE2VTx?= MXjJR|UxRTlibl2= NGDCfHQyOTh3OEezOy=>
A2780 MonIZ5l1d3SxeHnjbZR6KGG|c3H5 MojuSG1UVw>? M2LpRmlEPTB;NDDuUS=> MWexNVg2QDd|Nx?=
IMR-32 MkDRZ5l1d3SxeHnjbZR6KGG|c3H5 Ml3TglExKM7:TR?= NXO0cHViTE2VTx?= NVLCcFNOUUN3ME2yMlIyKG6P M{\SW|EzPjF5OEm0
P388 NIL6dmpkgXSxdH;4bYNqfHliYYPzZZk> NHfYU3hKSzVyPUGzJI5O Mn3XNVI3OjByOEG=
Lewis NGT2PZRkgXSxdH;4bYNqfHliYYPzZZk> M2TuR2lEPTB;M{Ogcm0> MoXHNVI3OjByOEG=
JLC M3\vboN6fG:2b4jpZ4l1gSCjc4PhfS=> MYfJR|UxRTVwNjDuUS=> NETkdWIyOjZ{MEC4NS=>
HT-29 MYLjfZRwfG:6aXPpeJkh[XO|YYm= MY\JR|UxRTFwNDFOwG0> MWWxNlY{QTV2MR?=
Caki-2 NHfwSHBkgXSxdH;4bYNqfHliYYPzZZk> NYnXO5N[UUN3ME2zMlk3KM7:TR?= MX2xNlY{QTV2MR?=
A549 MUfjfZRwfG:6aXPpeJkh[XO|YYm= Mn3STWM2OD1{LkWzJO69VQ>? NFS0dIQyOjZ|OUW0NS=>
HEC-1-B MnTpZ5l1d3SxeHnjbZR6KGG|c3H5 NHzkV5FKSzVyPUiuOlQh|ryP NWjxdZloOTJ4M{m1OFE>
HL-60 M2C4dIN6fG:2b4jpZ4l1gSCjc4PhfS=> MYDJR|UxRTZ4IH7N MlXTNVI3Ozl3NEG=
Col2 M3rjb4N6fG:2b4jpZ4l1gSCjc4PhfS=> NGfWWHN,OSEQvF2= M1nF[2VFPTB;NUegcm0> Ml3HNVUxPDN2MEe=
HUVEC MXvjfZRwfG:6aXPpeJkh[XO|YYm= MUL+NUDPxE1? NYHaemZkTUR3ME2yOVghdk1? MXixOVA1OzRyNx?=
KB NF\3OoNkgXSxdH;4bYNqfHliYYPzZZk> MYX+NUDPxE1? NIHHUJdGTDVyPUKyJI5O NEjL[VgyPTB2M{SwOy=>
LCNaP M1nNNIN6fG:2b4jpZ4l1gSCjc4PhfS=> NXzrPGg{hjFizszN M1H3NGVFPTB;Mkigcm0> NEjsc2MyPTB2M{SwOy=>
Lu1 NX\xTmtp[3m2b4TvfIlkcXS7IHHzd4F6 M4jzTJ4yKM7:TR?= NFXWepBGTDVyPUK5JI5O MYexOVA1OzRyNx?=
RPMI8402 M3LWTIN6fG:2b4jpZ4l1gSCjc4PhfS=> NHzjbYJ,OTBizszN M3TzWmlEPTB;NjDuUS=> NUD2bpR5OTV2OEK5Nlk>
CPT-K5 MnHhZ5l1d3SxeHnjbZR6KGG|c3H5 MU\+NVAh|ryP NHnpc4lKSzVyPkGwJO69VQ>? M1nS[VE2PDh{OUK5
P388 M{TwWIN6fG:2b4jpZ4l1gSCjc4PhfS=> MXn+NVAh|ryP MnPyTWM2OD1zNDDuUS=> MW[xOVQ5Ojl{OR?=
P388/CPT45 NVr1RYFr[3m2b4TvfIlkcXS7IHHzd4F6 MlTmglExKM7:TR?= MojITWM2OD5zMDFOwG0> NYnXN5RsOTV2OEK5Nlk>
KB3-1 NWPk[Ihl[3m2b4TvfIlkcXS7IHHzd4F6 NImz[Zh,OTBizszN M2ntbWlEPTB;NECgcm0> NUnkfJgzOTV2OEK5Nlk>
KBV-1 + MDR1 NF\nUY5kgXSxdH;4bYNqfHliYYPzZZk> NGO0dG9,OTBizszN Mm\MTWM2OD12NECgcm0> M{jIVVE2PDh{OUK5
KBH M4\SWIN6fG:2b4jpZ4l1gSCjc4PhfS=> NVrzeYl[hjFyIN88US=> NWXpfZlRUUN3ME20OFAhdk1? MYCxOVQ5Ojl{OR?=
HOP-62 NXm1NY9b[3m2b4TvfIlkcXS7IHHzd4F6 M1rlRZ4yOCEQvF2= NGrEVoRIUTVyPUGwJI5O MWqxOVUxQTF4NB?=
HCT-116 M2D2UoN6fG:2b4jpZ4l1gSCjc4PhfS=> MVX+NVAh|ryP NGXmWYlIUTVyPUOwJI5O MkP4NVU2ODlzNkS=
F-539 NWTPemx3[3m2b4TvfIlkcXS7IHHzd4F6 NH7Pd5Z,OTBizszN M4LhdmdKPTB;MUCgcm0> MWqxOVUxQTF4NB?=
UACC-62 MoTqZ5l1d3SxeHnjbZR6KGG|c3H5 NWHoU4xphjFyIN88US=> MmrFS2k2OD1zMDDuUS=> NXXGUJFCOTV3MEmxOlQ>
OVCAR-3 MVXjfZRwfG:6aXPpeJkh[XO|YYm= NYXrNYlIhjFyIN88US=> MmTiS2k2OD1{MkCgcm0> NVLqeVVZOTV3MEmxOlQ>
SN12C M37tR4N6fG:2b4jpZ4l1gSCjc4PhfS=> NVf6RpRmhjFyIN88US=> MmHzS2k2OD1{MDDuUS=> M1XUV|E2PTB7MU[0
DU-145 Mme4Z5l1d3SxeHnjbZR6KGG|c3H5 Ml\jglExKM7:TR?= M13kVmdKPTB;MUCgcm0> MX2xOVUxQTF4NB?=
MDA-MB-435 NVzrfmdp[3m2b4TvfIlkcXS7IHHzd4F6 MWX+NVAh|ryP M4XPVGdKPTB;NECgcm0> NELSZYwyPTVyOUG2OC=>
MT-4 NXixXYFn[3m2b4TvfIlkcXS7IHHzd4F6 M1G3S2lEPTB;NDDuUS=> MVGxO|I2PDZ4OR?=
CCRF-CEMc NXWzUJRD[3m2b4TvfIlkcXS7IHHzd4F6 M4nnd2lEPTB;MzDuUS=> MY[xO|I2PDZ4OR?=
WIL-2NSd MV;jfZRwfG:6aXPpeJkh[XO|YYm= NYDQU25KUUN3ME21JI5O NXKwR2x2OTd{NUS2Olk>
CCRF-SB NXr4bocx[3m2b4TvfIlkcXS7IHHzd4F6 NITmW3FKSzVyPUOgcm0> MXGxO|I2PDZ4OR?=
CRL 7065 MVPjfZRwfG:6aXPpeJkh[XO|YYm= MnXtTWM2OD12MECgcm0> NWH4NplFOTd{NUS2Olk>
SK-MEL-28b MXrjfZRwfG:6aXPpeJkh[XO|YYm= M{f1fGlEPTB;NECgcm0> MnvJNVczPTR4Nkm=
MCF-7 NUfEOlhT[3m2b4TvfIlkcXS7IHHzd4F6 Mn;jTWM2OD12MDDuUS=> MXOxO|I2PDZ4OR?=
SKMES-1 M4TONYN6fG:2b4jpZ4l1gSCjc4PhfS=> Ml70TWM2OD1zMDDuUS=> MYqxO|I2PDZ4OR?=
HepG2 MVfjfZRwfG:6aXPpeJkh[XO|YYm= NYPud3ZxUUN3ME2zNEBvVQ>? NGDEV3gyPzJ3NE[2PS=>
DU145 M4Tkd4N6fG:2b4jpZ4l1gSCjc4PhfS=> M4\HNGlEPTB;MUCgcm0> NEi5ZnkyPzJ3NE[2PS=>

... Click to View More Cell Line Experimental Data

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

Kinase Assay:[2]
+ Expand

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 Research:[2]
+ Expand
  • 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.
    (Only for Reference)
Animal Research:[3]
+ Expand
  • 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
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 3 mg/mL (8.61 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
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 Information

Molecular Weight 348.35
Formula

C20H16N2O4

CAS No. 7689-03-4
Storage powder
in solvent
Synonyms NSC-100880

Bio Calculators

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators 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 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 Unknown status Glioblastoma Multiforme|GBM|Gliosarcoma Arno Therapeutics December 2009 Phase 2
NCT00956787 Unknown status Myelodysplastic Syndrome Arno Therapeutics June 2009 Phase 2
NCT00947739 Completed Advanced Solid Tumors|Lymphomas New Mexico Cancer Care Alliance|Christus Stehlin Foundation for Cancer Research September 2008 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Topoisomerase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID