Camptothecin

For research use only. Not for use in humans.

Catalog No.S1288 Synonyms: NSC-100880

44 publications

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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Selleck's Camptothecin has been cited by 44 publications

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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.
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 MV;jfZRwfG:6aXPpeJkh[XO|YYm= NXf0ZXNvUUN3ME21NUBvVQ>? MY[5NFA{PTJy
SKVLB NIfWeFRkgXSxdH;4bYNqfHliYYPzZZk> NETlfFRKSzVyPUWzJI5O MYK5NFA{PTJy
HT29 NEPmNJNkgXSxdH;4bYNqfHliYYPzZZk> M1vobmlEPTB;OEeuPEBvVQ>? MlzyPVAxOzV{MB?=
KB NHvrUnVkgXSxdH;4bYNqfHliYYPzZZk> MYDJR|UxRThibl2= MV[5NFA{PTJy
A427 MX7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NEnZO3l,OSEQvF2= NYOw[IxnTE2VTx?= NULmN2VJUUN3ME2yOEBvVQ>? NILZOHk6QDd4MUGx
PC-3 M2Xy[mdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXv+NUDPxE1? MlTCSG1UVw>? NILOToNKSzVyPUW3JI5O M3PNVFk5PzZzMUG=
K562adr M3fSU2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NIracVV,OSEQvF2= NYjsSHN6TE2VTx?= NGrIOXdKSzVyPUW3JI5O M1nqdlk5PzZzMUG=
MCF7mdr NFzrZ3FIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NH\PSG9,OSEQvF2= M1m0WGROW09? NIThRWFKSzVyPUOuNUBvVQ>? NIPsd2M6QDd4MUGx
P388 NXjhXWZKT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MY\JR|UxRTN{IH7N MVGxNFM1Pjl|Mx?=
P388CPT5 R MV7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NE[2XGpKSzVyPUKuPEDPxE1? NHi3R|AyODN2NkmzNy=>
KBwt NFnKZ2JIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NIW2emhKSzVyPUSwJI5O MVSxNFQyOTR5Nh?=
KBMDR NY\YfoRST3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFzLSIlKSzVyPUewJI5O NUe5WpVQOTB2MUG0O|Y>
KBV20C MUPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MV3JR|UxRTNyIH7N MXOxNFQyOTR5Nh?=
KB7D M2m3V2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mmq4TWM2OD1|NTDuUS=> MYWxNFQyOTR5Nh?=
KBCamp NUjqcYlLT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWnJR|UxRTFwMESg{txO M2nMS|ExPDFzNEe2
HT29 NUK3dXA3[3m2b4TvfIlkcXS7IHHzd4F6 MX7JR|UxRThyIH7N MknwNVA5PDF6MEi=
A549 NUjmXGFS[3m2b4TvfIlkcXS7IHHzd4F6 NXfVb21qUUN3ME22O{BvVQ>? MUKxNFg1OThyOB?=
T24 NIe0XVRkgXSxdH;4bYNqfHliYYPzZZk> NYTyVWk4UUN3ME24PEBvVQ>? M4PucVExQDRzOEC4
HOP-62 Ml7tS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NUDQeWNMUUN3ME2xNEBvVQ>? MmXwNVExOjB{OEO=
HCT-116 Mm\JS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVXEOVNTUUN3ME2zNEBvVQ>? MnnmNVExOjB{OEO=
SF-539 MYDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2TBeWlEPTB;MUCgcm0> NXHveW1IOTFyMkCyPFM>
UACC-62 NV\BU|EzT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MlHkTWM2OD1zMDDuUS=> MnjONVExOjB{OEO=
OVCAR-3 M2O3[Gdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MoHoTWM2OD1{MkCgcm0> NV7MZnBDOTFyMkCyPFM>
SN12C NHmwb3hIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVzJR|UxRTJyIH7N MVOxNVAzODJ6Mx?=
DU-145 NEXGeWdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MljFTWM2OD1zMDDuUS=> NHLHdGoyOTB{MEK4Ny=>
MDA-MB-435 M3Th[2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3XJdWlEPTB;NECgcm0> NHrzWVMyOTB{MEK4Ny=>
WiDr MVHjfZRwfG:6aXPpeJkh[XO|YYm= MlvhSG1UVw>? MVvJR|UxRTF5IH7N NY\nW5lqOTF|M{S1Olk>
A549 M3;BSIN6fG:2b4jpZ4l1gSCjc4PhfS=> MnXsSG1UVw>? Mn3qTWM2OD1zNDDuUS=> M{jZ[|EyOzN2NU[5
MKN45 M1vWbIN6fG:2b4jpZ4l1gSCjc4PhfS=> NXv5VZhqTE2VTx?= NYTt[lJXUUN3ME2xO{BvVQ>? M2T3elEyOzN2NU[5
SK-OV-3 M1TpV4N6fG:2b4jpZ4l1gSCjc4PhfS=> Mn7FSG1UVw>? NF6xPWFKSzVyPUKwJI5O NFLlSnkyOTN|NEW2PS=>
H128 MljLZ5l1d3SxeHnjbZR6KGG|c3H5 MkjOSG1UVw>? MlPyTWM2OD1zODDuUS=> NH\i[Y8yOTN|NEW2PS=>
SK-BR-3 MnvOZ5l1d3SxeHnjbZR6KGG|c3H5 NIGzdZdFVVOR NF;OdWRKSzVyPUKwJI5O MoXUNVE{OzR3Nkm=
LX-1 MWjjfZRwfG:6aXPpeJkh[XO|YYm= M3TmO2ROW09? MYnJR|UxRTF{MDDuUS=> MUOxNVg2QDd|Nx?=
HCT116 NVWzSo5b[3m2b4TvfIlkcXS7IHHzd4F6 M1LqfWROW09? NUfacmh[UUN3ME25JI5O MVmxNVg2QDd|Nx?=
A2780 NFmyXXJkgXSxdH;4bYNqfHliYYPzZZk> MUjEUXNQ M2\KZWlEPTB;NDDuUS=> NWHxNXR5OTF6NUi3N|c>
IMR-32 NHLKRWVkgXSxdH;4bYNqfHliYYPzZZk> MnKwglExKM7:TR?= NF3IboZFVVOR NIPQXo9KSzVyPUKuNlEhdk1? M2\PZlEzPjF5OEm0
P388 M1HhZYN6fG:2b4jpZ4l1gSCjc4PhfS=> NVG0XGZsUUN3ME2xN{BvVQ>? M2jPN|EzPjJyMEix
Lewis Mkn4Z5l1d3SxeHnjbZR6KGG|c3H5 NI\qd3hKSzVyPUOzJI5O NUHLcJJVOTJ4MkCwPFE>
JLC MmPZZ5l1d3SxeHnjbZR6KGG|c3H5 MUXJR|UxRTVwNjDuUS=> NWGyWVV6OTJ4MkCwPFE>
HT-29 NFjBdGVkgXSxdH;4bYNqfHliYYPzZZk> NYDjNYFOUUN3ME2xMlQh|ryP MnzkNVI3Ozl3NEG=
Caki-2 NEjodohkgXSxdH;4bYNqfHliYYPzZZk> NWDT[YFMUUN3ME2zMlk3KM7:TR?= NFzyfI0yOjZ|OUW0NS=>
A549 M3;MS4N6fG:2b4jpZ4l1gSCjc4PhfS=> MVfJR|UxRTJwNUOg{txO MoL0NVI3Ozl3NEG=
HEC-1-B NVjURmJJ[3m2b4TvfIlkcXS7IHHzd4F6 NYDoeGkzUUN3ME24MlY1KM7:TR?= MnfBNVI3Ozl3NEG=
HL-60 NFjKTGRkgXSxdH;4bYNqfHliYYPzZZk> NHHxUpVKSzVyPU[2JI5O MYOxNlY{QTV2MR?=
Col2 MmHyZ5l1d3SxeHnjbZR6KGG|c3H5 M3jIcp4yKM7:TR?= MYDFSFUxRTV5IH7N M17BUVE2ODR|NEC3
HUVEC MUfjfZRwfG:6aXPpeJkh[XO|YYm= MVf+NUDPxE1? M4KzV2VFPTB;MkW4JI5O NXLvXXoyOTVyNEO0NFc>
KB MWjjfZRwfG:6aXPpeJkh[XO|YYm= MoPvglEh|ryP MUHFSFUxRTJ{IH7N NVjWW3F7OTVyNEO0NFc>
LCNaP MmLiZ5l1d3SxeHnjbZR6KGG|c3H5 NGnqNmV,OSEQvF2= MWPFSFUxRTJ6IH7N NUm5N|M5OTVyNEO0NFc>
Lu1 NF3ySmFkgXSxdH;4bYNqfHliYYPzZZk> M1e1Op4yKM7:TR?= M1q4NmVFPTB;Mkmgcm0> M2XJNVE2ODR|NEC3
RPMI8402 NFmxXGRkgXSxdH;4bYNqfHliYYPzZZk> M2P3OJ4yOCEQvF2= NHzUUmxKSzVyPU[gcm0> MkXWNVU1QDJ7Mkm=
CPT-K5 NWqyOHNV[3m2b4TvfIlkcXS7IHHzd4F6 MljtglExKM7:TR?= NYH3fppiUUN3ME6xNEDPxE1? M2DCWVE2PDh{OUK5
P388 MkLIZ5l1d3SxeHnjbZR6KGG|c3H5 MlzXglExKM7:TR?= MULJR|UxRTF2IH7N M{nZOFE2PDh{OUK5
P388/CPT45 NFHMVW9kgXSxdH;4bYNqfHliYYPzZZk> NY\MOII5hjFyIN88US=> MoTrTWM2OD5zMDFOwG0> M2i5PVE2PDh{OUK5
KB3-1 M3vKNIN6fG:2b4jpZ4l1gSCjc4PhfS=> NGLLbXB,OTBizszN NIe3bY1KSzVyPUSwJI5O MXGxOVQ5Ojl{OR?=
KBV-1 + MDR1 MXXjfZRwfG:6aXPpeJkh[XO|YYm= M2jtWJ4yOCEQvF2= M1vUOmlEPTB;NESwJI5O M4fRflE2PDh{OUK5
KBH MlXaZ5l1d3SxeHnjbZR6KGG|c3H5 NX;6N5NOhjFyIN88US=> M3rkSGlEPTB;NESwJI5O NVHjeVE{OTV2OEK5Nlk>
HOP-62 M1;Jc4N6fG:2b4jpZ4l1gSCjc4PhfS=> NFHTZ2x,OTBizszN NU\kXmx1T0l3ME2xNEBvVQ>? NGq0d4YyPTVyOUG2OC=>
HCT-116 NUXjVlJz[3m2b4TvfIlkcXS7IHHzd4F6 NULHPJB{hjFyIN88US=> NG\tTotIUTVyPUOwJI5O M{fZblE2PTB7MU[0
F-539 MWfjfZRwfG:6aXPpeJkh[XO|YYm= MV;+NVAh|ryP M{LnVWdKPTB;MUCgcm0> NEi0OI0yPTVyOUG2OC=>
UACC-62 NF2zc4pkgXSxdH;4bYNqfHliYYPzZZk> NYG2XYF6hjFyIN88US=> MWPHTVUxRTFyIH7N NUOxZnJUOTV3MEmxOlQ>
OVCAR-3 M1XEVYN6fG:2b4jpZ4l1gSCjc4PhfS=> Mn[2glExKM7:TR?= MnfiS2k2OD1{MkCgcm0> NFLVcZEyPTVyOUG2OC=>
SN12C M3LW[oN6fG:2b4jpZ4l1gSCjc4PhfS=> NVfrT|ZXhjFyIN88US=> NHrFbJhIUTVyPUKwJI5O MV[xOVUxQTF4NB?=
DU-145 M3nMdYN6fG:2b4jpZ4l1gSCjc4PhfS=> NH7Gb5Z,OTBizszN MYHHTVUxRTFyIH7N MYWxOVUxQTF4NB?=
MDA-MB-435 MmDYZ5l1d3SxeHnjbZR6KGG|c3H5 MYP+NVAh|ryP M3G0dWdKPTB;NECgcm0> M{f0WlE2PTB7MU[0
MT-4 MUXjfZRwfG:6aXPpeJkh[XO|YYm= Ml2yTWM2OD12IH7N NVW1eWlvOTd{NUS2Olk>
CCRF-CEMc Mon6Z5l1d3SxeHnjbZR6KGG|c3H5 NInyb3hKSzVyPUOgcm0> MorzNVczPTR4Nkm=
WIL-2NSd NIfzco5kgXSxdH;4bYNqfHliYYPzZZk> NWXnXJA6UUN3ME21JI5O MmPUNVczPTR4Nkm=
CCRF-SB MVXjfZRwfG:6aXPpeJkh[XO|YYm= MkXTTWM2OD1|IH7N MX[xO|I2PDZ4OR?=
CRL 7065 MYrjfZRwfG:6aXPpeJkh[XO|YYm= MYLJR|UxRTRyMDDuUS=> MUixO|I2PDZ4OR?=
SK-MEL-28b MVnjfZRwfG:6aXPpeJkh[XO|YYm= MmDuTWM2OD12MDDuUS=> MmnCNVczPTR4Nkm=
MCF-7 MV3jfZRwfG:6aXPpeJkh[XO|YYm= NIPPNINKSzVyPUSwJI5O MYqxO|I2PDZ4OR?=
SKMES-1 M1S2ZoN6fG:2b4jpZ4l1gSCjc4PhfS=> MkLLTWM2OD1zMDDuUS=> MoXINVczPTR4Nkm=
HepG2 NUG3O|lV[3m2b4TvfIlkcXS7IHHzd4F6 MVLJR|UxRTNyIH7N MUmxO|I2PDZ4OR?=
DU145 MUXjfZRwfG:6aXPpeJkh[XO|YYm= NEjoOXNKSzVyPUGwJI5O MXqxO|I2PDZ4OR?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
Cyclin1 / CDK1 / CDK2 ; 

PubMed: 29963130     


Western blot analysis indicated that camptothecin (6 µM) downregulates the expression of cell-cycle-associated proteins, cyclin 1, CDK1 and CDK2 in NPC cells. β-actin was used as a loading control.

Vimentin / Fibronectin / E-cadherin ; 

PubMed: 29963130     


Western blot analysis revealed that camptothecin (6 µM) treatment downregulates the expression of vimentin and fibronectin, and upregulates the expression of E-cadherin in NPC cells. β-actin was used as a loading control. NPC, nasopharyngeal carcinoma.

TGF-β / PI3K / pPI3K / AKT / pAKT ; 

PubMed: 29963130     


Western blot analysis revealed that camptothecin (6 µM) treatment inhibits the expression of TGF-β, PI3K and AKT in NPC cells. 

p53 / Cleaved caspase-3 / Cleaved PARP ; 

PubMed: 17548347     


NPCs in trophic factor-containing media were treated with 10 μM camptothecin for 0, 2, 4, 6, or 8 h, and extracts were immunoblotted for p53, active cleaved caspase-3, cleaved PARP, and total GSK3α/β as a loading control.

29963130 17548347
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]
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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]
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  • 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
Formula

C20H16N2O4

CAS No. 7689-03-4
Storage powder
in solvent
Synonyms NSC-100880
Smiles CCC1(O)C(=O)OCC2=C1C=C3N(CC4=C3N=C5C=CC=CC5=C4)C2=O

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID