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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Cited by 24 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 NEXMb29kgXSxdH;4bYNqfHliYYPzZZk> NEnJV|dKSzVyPUWxJI5O NXO1fXNIQTByM{WyNC=>
SKVLB MlLpZ5l1d3SxeHnjbZR6KGG|c3H5 MUfJR|UxRTV|IH7N M1y4[|kxODN3MkC=
HT29 NGnRb3lkgXSxdH;4bYNqfHliYYPzZZk> NGTuZ|hKSzVyPUi3Mlghdk1? NVXPU5hyQTByM{WyNC=>
KB MlW4Z5l1d3SxeHnjbZR6KGG|c3H5 Ml24TWM2OD16IH7N NEXRRnA6ODB|NUKw
A427 NUjuTotkT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NH;zO2V,OSEQvF2= NVfjOWFsTE2VTx?= M2rQ[WlEPTB;MkSgcm0> NYfBOWxQQTh5NkGxNS=>
PC-3 M3SxV2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmTRglEh|ryP MofvSG1UVw>? MlTQTWM2OD13NzDuUS=> MljNPVg4PjFzMR?=
K562adr M4fPcmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2Dte54yKM7:TR?= M3H1RmROW09? NIr6VW5KSzVyPUW3JI5O M2W1V|k5PzZzMUG=
MCF7mdr MkXFS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MY\+NUDPxE1? M3i1bGROW09? M{HBVGlEPTB;Mz6xJI5O MWe5PFc3OTFz
P388 NIrLZ2pIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NWHQR2liUUN3ME2zNkBvVQ>? M2G0OVExOzR4OUOz
P388CPT5 R NX3F[HNGT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mlv1TWM2OD1{Lkig{txO MlqwNVA{PDZ7M{O=
KBwt NF7TW3NIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NUnyTnJyUUN3ME20NEBvVQ>? MkfaNVA1OTF2N{[=
KBMDR MWTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MYrJR|UxRTdyIH7N MX:xNFQyOTR5Nh?=
KBV20C NXXwNVI1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFfR[ZZKSzVyPUOwJI5O M2P5TFExPDFzNEe2
KB7D MXTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NF7ZdXVKSzVyPUO1JI5O MkO2NVA1OTF2N{[=
KBCamp NYf0blFqT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MlPKTWM2OD1zLkC0JO69VQ>? NWHjWIN4OTB2MUG0O|Y>
HT29 MY\jfZRwfG:6aXPpeJkh[XO|YYm= M1nYW2lEPTB;OECgcm0> NHrrUpkyODh2MUiwPC=>
A549 M4PqUoN6fG:2b4jpZ4l1gSCjc4PhfS=> MYrJR|UxRTZ5IH7N MYOxNFg1OThyOB?=
T24 MWLjfZRwfG:6aXPpeJkh[XO|YYm= M2TURWlEPTB;OEigcm0> MWGxNFg1OThyOB?=
HOP-62 MXfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnzxTWM2OD1zMDDuUS=> Mo[2NVExOjB{OEO=
HCT-116 NISxfHlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MorSTWM2OD1|MDDuUS=> M1izWVEyODJyMkiz
SF-539 NU\idoJkT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mo\XTWM2OD1zMDDuUS=> NIXrOHoyOTB{MEK4Ny=>
UACC-62 MVHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3rNcmlEPTB;MUCgcm0> NVPOeol3OTFyMkCyPFM>
OVCAR-3 MV3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4jZT2lEPTB;MkKwJI5O NVn2UGNMOTFyMkCyPFM>
SN12C NVnCO2ozT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Ml3nTWM2OD1{MDDuUS=> NYPlV4pTOTFyMkCyPFM>
DU-145 MlzGS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVPJR|UxRTFyIH7N M1:xb|EyODJyMkiz
MDA-MB-435 NHLiR2VIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWHJR|UxRTRyIH7N MUmxNVAzODJ6Mx?=
WiDr MlPBZ5l1d3SxeHnjbZR6KGG|c3H5 NHLsVVRFVVOR NW[5d3RHUUN3ME2xO{BvVQ>? MVOxNVM{PDV4OR?=
A549 NHjze3ZkgXSxdH;4bYNqfHliYYPzZZk> MmTXSG1UVw>? MU\JR|UxRTF2IH7N NEjT[ZoyOTN|NEW2PS=>
MKN45 MWTjfZRwfG:6aXPpeJkh[XO|YYm= NF\Z[21FVVOR NHnqU5pKSzVyPUG3JI5O M4PqXlEyOzN2NU[5
SK-OV-3 MX3jfZRwfG:6aXPpeJkh[XO|YYm= MVrEUXNQ MWXJR|UxRTJyIH7N NFzrPGwyOTN|NEW2PS=>
H128 MnPXZ5l1d3SxeHnjbZR6KGG|c3H5 NYTjeXB4TE2VTx?= M4PqO2lEPTB;MUigcm0> M1PRNlEyOzN2NU[5
SK-BR-3 NHvrOmpkgXSxdH;4bYNqfHliYYPzZZk> NVTad4h5TE2VTx?= NXSzPZNsUUN3ME2yNEBvVQ>? NXPkZ2VHOTF|M{S1Olk>
LX-1 NUju[GNx[3m2b4TvfIlkcXS7IHHzd4F6 NXjYW2tvTE2VTx?= M13MSGlEPTB;MUKwJI5O MX:xNVg2QDd|Nx?=
HCT116 M1PP[YN6fG:2b4jpZ4l1gSCjc4PhfS=> MnTSSG1UVw>? MWPJR|UxRTlibl2= MlX0NVE5PTh5M{e=
A2780 NWm5WFJ7[3m2b4TvfIlkcXS7IHHzd4F6 M3ftOGROW09? MUDJR|UxRTRibl2= M1L5fVEyQDV6N{O3
IMR-32 NWLJbmNJ[3m2b4TvfIlkcXS7IHHzd4F6 NFXrcWd,OTBizszN M1WxcGROW09? M374NGlEPTB;Mj6yNUBvVQ>? MojXNVI3OTd6OUS=
P388 MUDjfZRwfG:6aXPpeJkh[XO|YYm= NGnGeWlKSzVyPUGzJI5O NGLJT2UyOjZ{MEC4NS=>
Lewis M1nzVoN6fG:2b4jpZ4l1gSCjc4PhfS=> NWPuXXMxUUN3ME2zN{BvVQ>? NXztWlUyOTJ4MkCwPFE>
JLC NHvaeY9kgXSxdH;4bYNqfHliYYPzZZk> M1jCNGlEPTB;NT62JI5O MY[xNlYzODB6MR?=
HT-29 M2TBSYN6fG:2b4jpZ4l1gSCjc4PhfS=> MlXkTWM2OD1zLkSg{txO MUGxNlY{QTV2MR?=
Caki-2 NVrMXIRr[3m2b4TvfIlkcXS7IHHzd4F6 NELicGNKSzVyPUOuPVYh|ryP MVGxNlY{QTV2MR?=
A549 NXjoPWhr[3m2b4TvfIlkcXS7IHHzd4F6 MljGTWM2OD1{LkWzJO69VQ>? Ml;PNVI3Ozl3NEG=
HEC-1-B M2C2fYN6fG:2b4jpZ4l1gSCjc4PhfS=> M1;CWWlEPTB;OD62OEDPxE1? MlmzNVI3Ozl3NEG=
HL-60 M1XUWYN6fG:2b4jpZ4l1gSCjc4PhfS=> MX7JR|UxRTZ4IH7N M33jO|EzPjN7NUSx
Col2 MmT2Z5l1d3SxeHnjbZR6KGG|c3H5 NHnSZod,OSEQvF2= NF3aNI5GTDVyPUW3JI5O NX3tOJhkOTVyNEO0NFc>
HUVEC NX2yPJNt[3m2b4TvfIlkcXS7IHHzd4F6 NYLpbnBNhjFizszN Ml7wSWQ2OD1{NUigcm0> MknUNVUxPDN2MEe=
KB MUTjfZRwfG:6aXPpeJkh[XO|YYm= NFjHW|J,OSEQvF2= NV3ySnE3TUR3ME2yNkBvVQ>? M{S2XlE2ODR|NEC3
LCNaP NIXQU3VkgXSxdH;4bYNqfHliYYPzZZk> NHThXoR,OSEQvF2= MXzFSFUxRTJ6IH7N MoXGNVUxPDN2MEe=
Lu1 M1rjXoN6fG:2b4jpZ4l1gSCjc4PhfS=> MnzyglEh|ryP NF7ST2lGTDVyPUK5JI5O MWGxOVA1OzRyNx?=
RPMI8402 MmrzZ5l1d3SxeHnjbZR6KGG|c3H5 NGLubFN,OTBizszN M2rPeWlEPTB;NjDuUS=> NF3NRnIyPTR6MkmyPS=>
CPT-K5 NHSyRVhkgXSxdH;4bYNqfHliYYPzZZk> MXL+NVAh|ryP MXfJR|UxRjFyIN88US=> MmLFNVU1QDJ7Mkm=
P388 Ml;FZ5l1d3SxeHnjbZR6KGG|c3H5 NYjXNIhshjFyIN88US=> NFnYfGRKSzVyPUG0JI5O NWrjS3R3OTV2OEK5Nlk>
P388/CPT45 M33sO4N6fG:2b4jpZ4l1gSCjc4PhfS=> NHzVN2p,OTBizszN MV\JR|UxRjFyIN88US=> NVHuW2NoOTV2OEK5Nlk>
KB3-1 NWnmcmtL[3m2b4TvfIlkcXS7IHHzd4F6 NHvh[YN,OTBizszN Mni2TWM2OD12MDDuUS=> NHTO[JEyPTR6MkmyPS=>
KBV-1 + MDR1 MXPjfZRwfG:6aXPpeJkh[XO|YYm= NFTQRmp,OTBizszN M4D3TWlEPTB;NESwJI5O NGDaXXgyPTR6MkmyPS=>
KBH MX;jfZRwfG:6aXPpeJkh[XO|YYm= NWLXWYtKhjFyIN88US=> MVjJR|UxRTR2MDDuUS=> M1XOeVE2PDh{OUK5
HOP-62 Mo\4Z5l1d3SxeHnjbZR6KGG|c3H5 MlnlglExKM7:TR?= NYC0fGQzT0l3ME2xNEBvVQ>? NEWxdYQyPTVyOUG2OC=>
HCT-116 M1;0foN6fG:2b4jpZ4l1gSCjc4PhfS=> MkfxglExKM7:TR?= MX3HTVUxRTNyIH7N M4\FNVE2PTB7MU[0
F-539 MWrjfZRwfG:6aXPpeJkh[XO|YYm= MkDrglExKM7:TR?= M4\h[mdKPTB;MUCgcm0> NH;VO3YyPTVyOUG2OC=>
UACC-62 NELLdm1kgXSxdH;4bYNqfHliYYPzZZk> NUXN[Jc5hjFyIN88US=> MmrBS2k2OD1zMDDuUS=> Mm\INVU2ODlzNkS=
OVCAR-3 NX;lZ4FW[3m2b4TvfIlkcXS7IHHzd4F6 MmfrglExKM7:TR?= NGniRXpIUTVyPUKyNEBvVQ>? M3zBTVE2PTB7MU[0
SN12C Ml\KZ5l1d3SxeHnjbZR6KGG|c3H5 NYTKXG5{hjFyIN88US=> NG\ZXItIUTVyPUKwJI5O NI[3fo8yPTVyOUG2OC=>
DU-145 MW\jfZRwfG:6aXPpeJkh[XO|YYm= MV;+NVAh|ryP NGrBNJlIUTVyPUGwJI5O M4rYRlE2PTB7MU[0
MDA-MB-435 MWLjfZRwfG:6aXPpeJkh[XO|YYm= MVr+NVAh|ryP Ml[zS2k2OD12MDDuUS=> NWjkenQ2OTV3MEmxOlQ>
MT-4 NXXHZ4dR[3m2b4TvfIlkcXS7IHHzd4F6 M17QXmlEPTB;NDDuUS=> NITxXHgyPzJ3NE[2PS=>
CCRF-CEMc NFjxdJJkgXSxdH;4bYNqfHliYYPzZZk> NH7rPGNKSzVyPUOgcm0> M4\5WFE4OjV2Nk[5
WIL-2NSd M{Xs[IN6fG:2b4jpZ4l1gSCjc4PhfS=> MYrJR|UxRTVibl2= MmLnNVczPTR4Nkm=
CCRF-SB M3rRPIN6fG:2b4jpZ4l1gSCjc4PhfS=> MlzKTWM2OD1|IH7N MW[xO|I2PDZ4OR?=
CRL 7065 MYHjfZRwfG:6aXPpeJkh[XO|YYm= M{DlfGlEPTB;NECwJI5O NFXGWWEyPzJ3NE[2PS=>
SK-MEL-28b NYnkeGVP[3m2b4TvfIlkcXS7IHHzd4F6 NYLmSoFvUUN3ME20NEBvVQ>? M2DjW|E4OjV2Nk[5
MCF-7 MXPjfZRwfG:6aXPpeJkh[XO|YYm= M3yweWlEPTB;NECgcm0> MYCxO|I2PDZ4OR?=
SKMES-1 Mmf3Z5l1d3SxeHnjbZR6KGG|c3H5 M13VVGlEPTB;MUCgcm0> M2HPZ|E4OjV2Nk[5
HepG2 MkCxZ5l1d3SxeHnjbZR6KGG|c3H5 Mk\JTWM2OD1|MDDuUS=> NH;qRlEyPzJ3NE[2PS=>
DU145 MUTjfZRwfG:6aXPpeJkh[XO|YYm= NXrQXG8zUUN3ME2xNEBvVQ>? NEHn[lYyPzJ3NE[2PS=>

... 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]
+ 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 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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID