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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  • 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.

  • a. Effects of five concentrations of CXCL12 (0, 10, 50, 100, and 500 ng/ml) on apoptosis of NPC cells caused by 10 μM camptothecin were determined by the amount of cleaved PARP detected by Western blot.

    Tumour Biol, 2016, 37(6):8169-79. 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.

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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.
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 M3jmVoN6fG:2b4jpZ4l1gSCjc4PhfS=> NXPJbFEzUUN3ME21NUBvVQ>? MYK5NFA{PTJy
HT29 NU\qeHBI[3m2b4TvfIlkcXS7IHHzd4F6 M1zwNGlEPTB;OEeuPEBvVQ>? M{nBe|kxODN3MkC=
KB M2C4S4N6fG:2b4jpZ4l1gSCjc4PhfS=> NVi1bFloUUN3ME24JI5O MYe5NFA{PTJy
A427 NGTEUoZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NYXlfGZkhjFizszN NWDacIFmTE2VTx?= NIfWbnlKSzVyPUK0JI5O Ml\jPVg4PjFzMR?=
K562adr MV3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXL+NUDPxE1? NWTUepQzTE2VTx?= M1PNPWlEPTB;NUegcm0> NH76cYc6QDd4MUGx
MCF7mdr MYPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M{TsSp4yKM7:TR?= MYrEUXNQ MkTHTWM2OD1|LkGgcm0> MXm5PFc3OTFz
P388 MlXXS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYLseXI5UUN3ME2zNkBvVQ>? MYWxNFM1Pjl|Mx?=
P388CPT5 R NHGxZYdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXzoTHlTUUN3ME2yMlgh|ryP MUexNFM1Pjl|Mx?=
KBwt MXzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2HHNmlEPTB;NECgcm0> M2DFblExPDFzNEe2
KBMDR M3HEcGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHzpTmpKSzVyPUewJI5O MnPrNVA1OTF2N{[=
KBV20C MkPiS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3jB[mlEPTB;M{Cgcm0> NW\lU4FkOTB2MUG0O|Y>
KB7D MljhS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFrQN4pKSzVyPUO1JI5O MV:xNFQyOTR5Nh?=
KBCamp MmHXS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1LqfGlEPTB;MT6wOEDPxE1? Ml3BNVA1OTF2N{[=
A549 MlzEZ5l1d3SxeHnjbZR6KGG|c3H5 NGrFRplKSzVyPU[3JI5O NEP1doYyODh2MUiwPC=>
T24 MlX0Z5l1d3SxeHnjbZR6KGG|c3H5 NVTaXHM1UUN3ME24PEBvVQ>? NGj6XmgyODh2MUiwPC=>
HOP-62 M{DxOWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MoS5TWM2OD1zMDDuUS=> NFnScJAyOTB{MEK4Ny=>
HCT-116 M4\U[mdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXzyRpBbUUN3ME2zNEBvVQ>? NF;yUGsyOTB{MEK4Ny=>
SF-539 NXX4UolST3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWDJR|UxRTFyIH7N M1:zO|EyODJyMkiz
UACC-62 M4LyWWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYjJR|UxRTFyIH7N NWfjPGF{OTFyMkCyPFM>
OVCAR-3 Ml\nS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVrjWlY6UUN3ME2yNlAhdk1? M1rFXVEyODJyMkiz
SN12C NYfEbWd{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NUe2TIM5UUN3ME2yNEBvVQ>? MnfGNVExOjB{OEO=
DU-145 NXHtSG43T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mlz5TWM2OD1zMDDuUS=> NUO1c|Q4OTFyMkCyPFM>
MDA-MB-435 M2[2TGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGHqTXRKSzVyPUSwJI5O M2[4VlEyODJyMkiz
WiDr NXn4PFdj[3m2b4TvfIlkcXS7IHHzd4F6 M1;3emROW09? M4fwTmlEPTB;MUegcm0> MX6xNVM{PDV4OR?=
A549 MnX0Z5l1d3SxeHnjbZR6KGG|c3H5 NGXuR3FFVVOR NELj[|NKSzVyPUG0JI5O MnyxNVE{OzR3Nkm=
MKN45 M3r0R4N6fG:2b4jpZ4l1gSCjc4PhfS=> NIPCXVJFVVOR Mny3TWM2OD1zNzDuUS=> MnX3NVE{OzR3Nkm=
H128 M2PXUYN6fG:2b4jpZ4l1gSCjc4PhfS=> NUf4NINITE2VTx?= MUPJR|UxRTF6IH7N NWe1[5NqOTF|M{S1Olk>
SK-BR-3 Ml;0Z5l1d3SxeHnjbZR6KGG|c3H5 MULEUXNQ M4T2TmlEPTB;MkCgcm0> M{\KN|EyOzN2NU[5
HCT116 MUXjfZRwfG:6aXPpeJkh[XO|YYm= NWr3NlhOTE2VTx?= MmniTWM2OD17IH7N M4HhZVEyQDV6N{O3
IMR-32 MlTGZ5l1d3SxeHnjbZR6KGG|c3H5 NGPOfJp,OTBizszN NV\1[lBrTE2VTx?= MnHOTWM2OD1{LkKxJI5O M2C0e|EzPjF5OEm0
Lewis Mnv0Z5l1d3SxeHnjbZR6KGG|c3H5 NX;WUGJmUUN3ME2zN{BvVQ>? NILZbVcyOjZ{MEC4NS=>
HT-29 MkS4Z5l1d3SxeHnjbZR6KGG|c3H5 MkXXTWM2OD1zLkSg{txO NV\3OVBPOTJ4M{m1OFE>
Caki-2 NVPNcHZV[3m2b4TvfIlkcXS7IHHzd4F6 NXXHdpRrUUN3ME2zMlk3KM7:TR?= M3zD[lEzPjN7NUSx
A549 M4nadIN6fG:2b4jpZ4l1gSCjc4PhfS=> M{[4NmlEPTB;Mj61N{DPxE1? MXixNlY{QTV2MR?=
HEC-1-B NV\xb3ds[3m2b4TvfIlkcXS7IHHzd4F6 NUjXNpZIUUN3ME24MlY1KM7:TR?= NF\ROGoyOjZ|OUW0NS=>
Col2 MnLwZ5l1d3SxeHnjbZR6KGG|c3H5 MoPYglEh|ryP NVnHOXZZTUR3ME21O{BvVQ>? NYjRVnhQOTVyNEO0NFc>
HUVEC MoC5Z5l1d3SxeHnjbZR6KGG|c3H5 NG\xfnh,OSEQvF2= NYL5OYw3TUR3ME2yOVghdk1? Ml36NVUxPDN2MEe=
LCNaP M3q4R4N6fG:2b4jpZ4l1gSCjc4PhfS=> M1HwdZ4yKM7:TR?= M1jSR2VFPTB;Mkigcm0> NXLPdnRkOTVyNEO0NFc>
Lu1 NUHHTZpw[3m2b4TvfIlkcXS7IHHzd4F6 M1rxd54yKM7:TR?= NEmxVnpGTDVyPUK5JI5O MYSxOVA1OzRyNx?=
CPT-K5 M{C4d4N6fG:2b4jpZ4l1gSCjc4PhfS=> M4LtSZ4yOCEQvF2= M3jOfGlEPTB-MUCg{txO M1HCbFE2PDh{OUK5
P388 NEjrdmZkgXSxdH;4bYNqfHliYYPzZZk> NV\1OmhvhjFyIN88US=> MUHJR|UxRTF2IH7N NXPtO2hNOTV2OEK5Nlk>
P388/CPT45 NU\ReoM6[3m2b4TvfIlkcXS7IHHzd4F6 MnjJglExKM7:TR?= NVnBcXVbUUN3ME6xNEDPxE1? NFLjSmUyPTR6MkmyPS=>
KB3-1 M3y4[YN6fG:2b4jpZ4l1gSCjc4PhfS=> M3zhRp4yOCEQvF2= MVPJR|UxRTRyIH7N NED6V3YyPTR6MkmyPS=>
KBV-1 + MDR1 MnH2Z5l1d3SxeHnjbZR6KGG|c3H5 MWP+NVAh|ryP Mn\0TWM2OD12NECgcm0> MWGxOVQ5Ojl{OR?=
KBH NXm0bYw1[3m2b4TvfIlkcXS7IHHzd4F6 Mon6glExKM7:TR?= MoXYTWM2OD12NECgcm0> NVnve25YOTV2OEK5Nlk>
HOP-62 MWnjfZRwfG:6aXPpeJkh[XO|YYm= MkPjglExKM7:TR?= M1\tbGdKPTB;MUCgcm0> NFrWXHkyPTVyOUG2OC=>
HCT-116 NFf4SYJkgXSxdH;4bYNqfHliYYPzZZk> MlL1glExKM7:TR?= M2jxVmdKPTB;M{Cgcm0> M2rZdFE2PTB7MU[0
UACC-62 NHzoXlNkgXSxdH;4bYNqfHliYYPzZZk> MVf+NVAh|ryP M1X3O2dKPTB;MUCgcm0> MmnKNVU2ODlzNkS=
OVCAR-3 M3n2[YN6fG:2b4jpZ4l1gSCjc4PhfS=> MYL+NVAh|ryP NVLVWmpkT0l3ME2yNlAhdk1? NVvUSHFwOTV3MEmxOlQ>
MDA-MB-435 MVTjfZRwfG:6aXPpeJkh[XO|YYm= NHn1clh,OTBizszN NFjqfGtIUTVyPUSwJI5O NX\M[JZ6OTV3MEmxOlQ>
MT-4 M1\LTIN6fG:2b4jpZ4l1gSCjc4PhfS=> NEXo[nRKSzVyPUSgcm0> MmG3NVczPTR4Nkm=
CCRF-CEMc NGTm[mpkgXSxdH;4bYNqfHliYYPzZZk> NX3GTmxrUUN3ME2zJI5O NXfwfFcxOTd{NUS2Olk>
WIL-2NSd NVrTeHpl[3m2b4TvfIlkcXS7IHHzd4F6 MnXGTWM2OD13IH7N NXjxdW9MOTd{NUS2Olk>
CCRF-SB M{mwT4N6fG:2b4jpZ4l1gSCjc4PhfS=> NFrMc|VKSzVyPUOgcm0> M4HMdFE4OjV2Nk[5
CRL 7065 NVW4XHdI[3m2b4TvfIlkcXS7IHHzd4F6 NI[xfodKSzVyPUSwNEBvVQ>? MWKxO|I2PDZ4OR?=
SK-MEL-28b M2Pm[oN6fG:2b4jpZ4l1gSCjc4PhfS=> NELJOnZKSzVyPUSwJI5O NEHrRWkyPzJ3NE[2PS=>
MCF-7 Mn22Z5l1d3SxeHnjbZR6KGG|c3H5 M1HJUWlEPTB;NECgcm0> MU[xO|I2PDZ4OR?=
SKMES-1 Mki3Z5l1d3SxeHnjbZR6KGG|c3H5 MkLkTWM2OD1zMDDuUS=> NFPFbWsyPzJ3NE[2PS=>
HepG2 M3zLN4N6fG:2b4jpZ4l1gSCjc4PhfS=> MnvITWM2OD1|MDDuUS=> MYCxO|I2PDZ4OR?=

... 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]


Kinase Assay:[2]
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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]
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  • 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 Insoluble
Ethanol 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


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

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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID