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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  • 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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Choose Selective Topoisomerase Inhibitors

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 M2TzfIN6fG:2b4jpZ4l1gSCjc4PhfS=> MWjJR|UxRTVzIH7N MWO5NFA{PTJy
SKVLB MXXjfZRwfG:6aXPpeJkh[XO|YYm= NXfGXJBVUUN3ME21N{BvVQ>? NH2yZpU6ODB|NUKw
HT29 NHfJTHZkgXSxdH;4bYNqfHliYYPzZZk> NInSTYhKSzVyPUi3Mlghdk1? NUPDbHpJQTByM{WyNC=>
KB Mn3lZ5l1d3SxeHnjbZR6KGG|c3H5 MoHKTWM2OD16IH7N M3;mblkxODN3MkC=
A427 NVXi[G53T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXL+NUDPxE1? NYXHcHIxTE2VTx?= NEC2c5RKSzVyPUK0JI5O M1jYZ|k5PzZzMUG=
PC-3 M1TRbGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M{nqRZ4yKM7:TR?= NHr6VZVFVVOR MV\JR|UxRTV5IH7N MUe5PFc3OTFz
K562adr NFG3XVZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUH+NUDPxE1? MYnEUXNQ M2TFeWlEPTB;NUegcm0> MVS5PFc3OTFz
MCF7mdr Mlr6S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MkDMglEh|ryP NH\RfGZFVVOR MV;JR|UxRTNwMTDuUS=> M{[3bFk5PzZzMUG=
P388 NFHQPZlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NUHINJpMUUN3ME2zNkBvVQ>? MXOxNFM1Pjl|Mx?=
P388CPT5 R NHzJSVZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MlXUTWM2OD1{Lkig{txO MnftNVA{PDZ7M{O=
KBwt NVjteYEzT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MlzHTWM2OD12MDDuUS=> MofDNVA1OTF2N{[=
KBMDR NIfxdYRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2TXcGlEPTB;N{Cgcm0> M4e1WlExPDFzNEe2
KBV20C NYmzdIRnT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGf3cY5KSzVyPUOwJI5O NGrOemsyODRzMUS3Oi=>
KB7D NGToSXJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVnIdWcxUUN3ME2zOUBvVQ>? MXqxNFQyOTR5Nh?=
KBCamp Mn7rS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVrlU3IyUUN3ME2xMlA1KM7:TR?= MVixNFQyOTR5Nh?=
HT29 MYXjfZRwfG:6aXPpeJkh[XO|YYm= MVTJR|UxRThyIH7N NIrhTZYyODh2MUiwPC=>
A549 NH7ZV3NkgXSxdH;4bYNqfHliYYPzZZk> MofCTWM2OD14NzDuUS=> M37H[VExQDRzOEC4
T24 Mk\TZ5l1d3SxeHnjbZR6KGG|c3H5 Mn\sTWM2OD16ODDuUS=> M2nYNVExQDRzOEC4
HOP-62 M3\obGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MnvlTWM2OD1zMDDuUS=> NFr3cpQyOTB{MEK4Ny=>
HCT-116 MWTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MmLHTWM2OD1|MDDuUS=> NHzr[G0yOTB{MEK4Ny=>
SF-539 MmPTS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3;6WmlEPTB;MUCgcm0> MkjTNVExOjB{OEO=
UACC-62 NUW3TpZjT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mny2TWM2OD1zMDDuUS=> NYjOdXNROTFyMkCyPFM>
OVCAR-3 NY\BZnhlT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1z2fWlEPTB;MkKwJI5O Mk\UNVExOjB{OEO=
SN12C NVe2NXNXT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWHJR|UxRTJyIH7N NX3BeW05OTFyMkCyPFM>
DU-145 M4XVdGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MnH5TWM2OD1zMDDuUS=> MoXtNVExOjB{OEO=
MDA-MB-435 NF;JUW5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFjRWnpKSzVyPUSwJI5O M2T2dFEyODJyMkiz
WiDr NGr6dJlkgXSxdH;4bYNqfHliYYPzZZk> MVHEUXNQ MnvnTWM2OD1zNzDuUS=> NG[1XXIyOTN|NEW2PS=>
A549 NIHLTmlkgXSxdH;4bYNqfHliYYPzZZk> NEWxXGhFVVOR NHnMTpNKSzVyPUG0JI5O MlzRNVE{OzR3Nkm=
MKN45 Ml3uZ5l1d3SxeHnjbZR6KGG|c3H5 NWLXeHJDTE2VTx?= MlnlTWM2OD1zNzDuUS=> NFfrOnEyOTN|NEW2PS=>
SK-OV-3 MmOyZ5l1d3SxeHnjbZR6KGG|c3H5 NYjBWFZWTE2VTx?= M2PzOmlEPTB;MkCgcm0> NYHRWHhJOTF|M{S1Olk>
H128 Mk\FZ5l1d3SxeHnjbZR6KGG|c3H5 NV;Be454TE2VTx?= NHXzc4hKSzVyPUG4JI5O NXTyPGQ3OTF|M{S1Olk>
SK-BR-3 M3zvSoN6fG:2b4jpZ4l1gSCjc4PhfS=> M3XwXWROW09? MUTJR|UxRTJyIH7N NU[3bXdiOTF|M{S1Olk>
LX-1 MlXOZ5l1d3SxeHnjbZR6KGG|c3H5 MknMSG1UVw>? M1;QTmlEPTB;MUKwJI5O NGPVT4IyOTh3OEezOy=>
HCT116 MYTjfZRwfG:6aXPpeJkh[XO|YYm= Ml3WSG1UVw>? M1O0dGlEPTB;OTDuUS=> MmDTNVE5PTh5M{e=
A2780 NUKwO2ty[3m2b4TvfIlkcXS7IHHzd4F6 M1G3dmROW09? NFjQV4pKSzVyPUSgcm0> NV3GS4xWOTF6NUi3N|c>
IMR-32 MV7jfZRwfG:6aXPpeJkh[XO|YYm= NFP6S5Z,OTBizszN MXHEUXNQ NUnmSXJWUUN3ME2yMlIyKG6P MYqxNlYyPzh7NB?=
P388 MXjjfZRwfG:6aXPpeJkh[XO|YYm= NVXHVm1EUUN3ME2xN{BvVQ>? NHHF[ZoyOjZ{MEC4NS=>
Lewis M1jPW4N6fG:2b4jpZ4l1gSCjc4PhfS=> NXvZRoNyUUN3ME2zN{BvVQ>? NVPPd2JQOTJ4MkCwPFE>
JLC NXj4OoVK[3m2b4TvfIlkcXS7IHHzd4F6 Ml7QTWM2OD13Lk[gcm0> M13GR|EzPjJyMEix
HT-29 MU\jfZRwfG:6aXPpeJkh[XO|YYm= MYLJR|UxRTFwNDFOwG0> NULNNGdmOTJ4M{m1OFE>
Caki-2 NYq5S3FH[3m2b4TvfIlkcXS7IHHzd4F6 MYfJR|UxRTNwOU[g{txO NHOzPHMyOjZ|OUW0NS=>
A549 NW[4XIJ4[3m2b4TvfIlkcXS7IHHzd4F6 NEKzO21KSzVyPUKuOVMh|ryP NGrW[HIyOjZ|OUW0NS=>
HEC-1-B MoXaZ5l1d3SxeHnjbZR6KGG|c3H5 NGn6dnpKSzVyPUiuOlQh|ryP NF3HRWcyOjZ|OUW0NS=>
HL-60 M2[2VoN6fG:2b4jpZ4l1gSCjc4PhfS=> NXXrT2szUUN3ME22OkBvVQ>? MY[xNlY{QTV2MR?=
Col2 MVLjfZRwfG:6aXPpeJkh[XO|YYm= NWSzNIpqhjFizszN NHXme3lGTDVyPUW3JI5O M4\yUFE2ODR|NEC3
HUVEC MXzjfZRwfG:6aXPpeJkh[XO|YYm= MljQglEh|ryP M3;1S2VFPTB;MkW4JI5O MYSxOVA1OzRyNx?=
KB NGCwPG1kgXSxdH;4bYNqfHliYYPzZZk> MlnNglEh|ryP MXnFSFUxRTJ{IH7N NF3TNY0yPTB2M{SwOy=>
LCNaP NXfIZlhQ[3m2b4TvfIlkcXS7IHHzd4F6 NEOzcYt,OSEQvF2= M4XGR2VFPTB;Mkigcm0> MnH2NVUxPDN2MEe=
Lu1 MXnjfZRwfG:6aXPpeJkh[XO|YYm= NU\VeI9zhjFizszN MnTrSWQ2OD1{OTDuUS=> MXOxOVA1OzRyNx?=
RPMI8402 NVewcFBD[3m2b4TvfIlkcXS7IHHzd4F6 NEOzcGF,OTBizszN NFXCc|BKSzVyPU[gcm0> M4ixOFE2PDh{OUK5
CPT-K5 NVLLZmlD[3m2b4TvfIlkcXS7IHHzd4F6 NH7I[op,OTBizszN MV7JR|UxRjFyIN88US=> MUOxOVQ5Ojl{OR?=
P388 MnfRZ5l1d3SxeHnjbZR6KGG|c3H5 Mn65glExKM7:TR?= NV\meFhTUUN3ME2xOEBvVQ>? NIC2eIgyPTR6MkmyPS=>
P388/CPT45 MVzjfZRwfG:6aXPpeJkh[XO|YYm= M2S3Rp4yOCEQvF2= NF;4bnVKSzVyPkGwJO69VQ>? NF;QbnkyPTR6MkmyPS=>
KB3-1 M{HtVYN6fG:2b4jpZ4l1gSCjc4PhfS=> M{\3PZ4yOCEQvF2= NXjufGtyUUN3ME20NEBvVQ>? NHn3U|IyPTR6MkmyPS=>
KBV-1 + MDR1 NHrFTmZkgXSxdH;4bYNqfHliYYPzZZk> MkfhglExKM7:TR?= MWPJR|UxRTR2MDDuUS=> M3qyUFE2PDh{OUK5
KBH MoTSZ5l1d3SxeHnjbZR6KGG|c3H5 NFXUSlZ,OTBizszN MoqwTWM2OD12NECgcm0> NHfkNZoyPTR6MkmyPS=>
HOP-62 MlHQZ5l1d3SxeHnjbZR6KGG|c3H5 M4LSTJ4yOCEQvF2= NYPpSHNVT0l3ME2xNEBvVQ>? NWXRb|hkOTV3MEmxOlQ>
HCT-116 NHXORVVkgXSxdH;4bYNqfHliYYPzZZk> MYj+NVAh|ryP NGTVTVJIUTVyPUOwJI5O NEXwU5AyPTVyOUG2OC=>
F-539 MmTIZ5l1d3SxeHnjbZR6KGG|c3H5 Mo\aglExKM7:TR?= MWPHTVUxRTFyIH7N MkTmNVU2ODlzNkS=
UACC-62 MXTjfZRwfG:6aXPpeJkh[XO|YYm= MW\+NVAh|ryP M{LGd2dKPTB;MUCgcm0> NIjVO4QyPTVyOUG2OC=>
OVCAR-3 M2jhRYN6fG:2b4jpZ4l1gSCjc4PhfS=> MYL+NVAh|ryP NV3rTnF5T0l3ME2yNlAhdk1? M3jrS|E2PTB7MU[0
SN12C MUfjfZRwfG:6aXPpeJkh[XO|YYm= MX3+NVAh|ryP M1T5T2dKPTB;MkCgcm0> MVuxOVUxQTF4NB?=
DU-145 NGLBS5ZkgXSxdH;4bYNqfHliYYPzZZk> MnPiglExKM7:TR?= NVXkbItVT0l3ME2xNEBvVQ>? MU[xOVUxQTF4NB?=
MDA-MB-435 MY\jfZRwfG:6aXPpeJkh[XO|YYm= M1fNTJ4yOCEQvF2= MVLHTVUxRTRyIH7N M{npN|E2PTB7MU[0
MT-4 MWHjfZRwfG:6aXPpeJkh[XO|YYm= NIn2OWxKSzVyPUSgcm0> NXTFR|VxOTd{NUS2Olk>
CCRF-CEMc NGK3b5lkgXSxdH;4bYNqfHliYYPzZZk> MX3JR|UxRTNibl2= NXzWXmhsOTd{NUS2Olk>
WIL-2NSd MlnqZ5l1d3SxeHnjbZR6KGG|c3H5 M3vjWmlEPTB;NTDuUS=> NVrFXoVQOTd{NUS2Olk>
CCRF-SB NFru[XZkgXSxdH;4bYNqfHliYYPzZZk> Mn\aTWM2OD1|IH7N NH7CPZUyPzJ3NE[2PS=>
CRL 7065 M2DXPIN6fG:2b4jpZ4l1gSCjc4PhfS=> MWnJR|UxRTRyMDDuUS=> NYHXenRKOTd{NUS2Olk>
SK-MEL-28b MmDoZ5l1d3SxeHnjbZR6KGG|c3H5 NE[1NlhKSzVyPUSwJI5O NUTqeW9YOTd{NUS2Olk>
MCF-7 NGnzeGlkgXSxdH;4bYNqfHliYYPzZZk> NH7PRVlKSzVyPUSwJI5O NH3HTYwyPzJ3NE[2PS=>
SKMES-1 MYPjfZRwfG:6aXPpeJkh[XO|YYm= M37h[2lEPTB;MUCgcm0> NH:3dnMyPzJ3NE[2PS=>
HepG2 NFP4TFVkgXSxdH;4bYNqfHliYYPzZZk> NF\qVnRKSzVyPUOwJI5O M1HqclE4OjV2Nk[5
DU145 NHPyTGFkgXSxdH;4bYNqfHliYYPzZZk> NF6yZmZKSzVyPUGwJI5O MlP1NVczPTR4Nkm=

... 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 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
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

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.

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Topoisomerase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID