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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4 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.

  • 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.

Purity & Quality Control

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 NETHUFFkgXSxdH;4bYNqfHliYYPzZZk> MU\JR|UxRTVzIH7N M17aVVkxODN3MkC=
SKVLB MonWZ5l1d3SxeHnjbZR6KGG|c3H5 MlXNTWM2OD13MzDuUS=> M{jtNVkxODN3MkC=
HT29 NX\XZZVl[3m2b4TvfIlkcXS7IHHzd4F6 NGDxSIVKSzVyPUi3Mlghdk1? M4PNOlkxODN3MkC=
KB M2\ScoN6fG:2b4jpZ4l1gSCjc4PhfS=> NHP1[pRKSzVyPUigcm0> MUC5NFA{PTJy
A427 MnTmS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXWySlFjhjFizszN M1ezeWROW09? M1iy[WlEPTB;MkSgcm0> NHPQT|I6QDd4MUGx
PC-3 MUHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NH22TYd,OSEQvF2= MYnEUXNQ MXXJR|UxRTV5IH7N NGjYOmU6QDd4MUGx
K562adr MnX4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MmjzglEh|ryP NH[5N|dFVVOR NWHjNWJ7UUN3ME21O{BvVQ>? MXG5PFc3OTFz
MCF7mdr MVLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M{HERZ4yKM7:TR?= MWrEUXNQ M2rHW2lEPTB;Mz6xJI5O NX\p[3VrQTh5NkGxNS=>
P388 M{Ti[mdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYjvN29UUUN3ME2zNkBvVQ>? NXfHSWs6OTB|NE[5N|M>
P388CPT5 R MnXaS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NETzWGJKSzVyPUKuPEDPxE1? NYD3OWdTOTB|NE[5N|M>
KBwt M2O0bWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MX7JR|UxRTRyIH7N MVGxNFQyOTR5Nh?=
KBMDR MYjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NV;ET5lFUUN3ME23NEBvVQ>? NYL1Z|Q6OTB2MUG0O|Y>
KBV20C NWDJeolYT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MV7JR|UxRTNyIH7N NYCxbY1YOTB2MUG0O|Y>
KB7D NWLrWYttT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWjhdYV6UUN3ME2zOUBvVQ>? NIPpUY0yODRzMUS3Oi=>
KBCamp M4nN[2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NW\MUHdZUUN3ME2xMlA1KM7:TR?= NXjnN|Y6OTB2MUG0O|Y>
HT29 M1PNT4N6fG:2b4jpZ4l1gSCjc4PhfS=> MWTJR|UxRThyIH7N MVuxNFg1OThyOB?=
A549 MX7jfZRwfG:6aXPpeJkh[XO|YYm= M1nxc2lEPTB;Nkegcm0> NVSyOGZFOTB6NEG4NFg>
T24 MUHjfZRwfG:6aXPpeJkh[XO|YYm= NH\PS2xKSzVyPUi4JI5O NECyTXAyODh2MUiwPC=>
HOP-62 M1LNfGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2PlUGlEPTB;MUCgcm0> MmG0NVExOjB{OEO=
HCT-116 NGjITpNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NX;Dd3VIUUN3ME2zNEBvVQ>? NYTMR4RsOTFyMkCyPFM>
SF-539 M1\0RWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVfJR|UxRTFyIH7N M3XDZlEyODJyMkiz
UACC-62 NX;6bJVDT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NF7ZRWlKSzVyPUGwJI5O M4rmdVEyODJyMkiz
OVCAR-3 M3G5dmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHnrZnRKSzVyPUKyNEBvVQ>? M2CxNVEyODJyMkiz
SN12C NVriOWhXT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWHJR|UxRTJyIH7N M2HtW|EyODJyMkiz
DU-145 MV\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M{HFUmlEPTB;MUCgcm0> MYqxNVAzODJ6Mx?=
MDA-MB-435 NHXwN2VIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M37HPWlEPTB;NECgcm0> MkfQNVExOjB{OEO=
WiDr NWDQWIJH[3m2b4TvfIlkcXS7IHHzd4F6 NInmdFJFVVOR NEixTGNKSzVyPUG3JI5O NVPId20yOTF|M{S1Olk>
A549 M2HlSoN6fG:2b4jpZ4l1gSCjc4PhfS=> NYL2bY1jTE2VTx?= MXzJR|UxRTF2IH7N NYfiUWVnOTF|M{S1Olk>
MKN45 M{L2N4N6fG:2b4jpZ4l1gSCjc4PhfS=> NFTwZVdFVVOR NYTvfHBEUUN3ME2xO{BvVQ>? MlzPNVE{OzR3Nkm=
SK-OV-3 NWnEfG9K[3m2b4TvfIlkcXS7IHHzd4F6 M3nMZ2ROW09? NVXmN5BjUUN3ME2yNEBvVQ>? MVqxNVM{PDV4OR?=
H128 M322dYN6fG:2b4jpZ4l1gSCjc4PhfS=> MkfJSG1UVw>? M1;PUGlEPTB;MUigcm0> NUi1XGlGOTF|M{S1Olk>
SK-BR-3 M3vhSoN6fG:2b4jpZ4l1gSCjc4PhfS=> MX;EUXNQ M3:1SWlEPTB;MkCgcm0> MnO1NVE{OzR3Nkm=
LX-1 MVjjfZRwfG:6aXPpeJkh[XO|YYm= MkDpSG1UVw>? M2jVV2lEPTB;MUKwJI5O M{PUTFEyQDV6N{O3
HCT116 MXzjfZRwfG:6aXPpeJkh[XO|YYm= NFjtWnFFVVOR Mon5TWM2OD17IH7N MorXNVE5PTh5M{e=
A2780 MWrjfZRwfG:6aXPpeJkh[XO|YYm= NIrCOIZFVVOR MUHJR|UxRTRibl2= NWLadGJ{OTF6NUi3N|c>
IMR-32 NUPxcow6[3m2b4TvfIlkcXS7IHHzd4F6 NGDFRnZ,OTBizszN MWDEUXNQ MWTJR|UxRTJwMkGgcm0> M3vkV|EzPjF5OEm0
P388 M2iyOYN6fG:2b4jpZ4l1gSCjc4PhfS=> NEnKOXdKSzVyPUGzJI5O NXz2R4h[OTJ4MkCwPFE>
Lewis NXfWcZhR[3m2b4TvfIlkcXS7IHHzd4F6 NWDaXo5vUUN3ME2zN{BvVQ>? M2fEblEzPjJyMEix
JLC MkLrZ5l1d3SxeHnjbZR6KGG|c3H5 NV:3NJlbUUN3ME21MlYhdk1? NG\l[GIyOjZ{MEC4NS=>
HT-29 MnnMZ5l1d3SxeHnjbZR6KGG|c3H5 M{n2fmlEPTB;MT60JO69VQ>? M1TtNlEzPjN7NUSx
Caki-2 MlT1Z5l1d3SxeHnjbZR6KGG|c3H5 M1TJemlEPTB;Mz65OkDPxE1? M3\lZ|EzPjN7NUSx
A549 M3\YbYN6fG:2b4jpZ4l1gSCjc4PhfS=> MoHpTWM2OD1{LkWzJO69VQ>? NXXSdVZkOTJ4M{m1OFE>
HEC-1-B NUTYXFc1[3m2b4TvfIlkcXS7IHHzd4F6 NWHFW2ppUUN3ME24MlY1KM7:TR?= M1TEb|EzPjN7NUSx
HL-60 NUjnXpAz[3m2b4TvfIlkcXS7IHHzd4F6 NYnyVXNEUUN3ME22OkBvVQ>? Mof3NVI3Ozl3NEG=
Col2 Mn;sZ5l1d3SxeHnjbZR6KGG|c3H5 NXLvSVZThjFizszN NGnHUGZGTDVyPUW3JI5O Mn7ONVUxPDN2MEe=
HUVEC MmnvZ5l1d3SxeHnjbZR6KGG|c3H5 MVH+NUDPxE1? MWfFSFUxRTJ3ODDuUS=> M2TCOVE2ODR|NEC3
KB Moe0Z5l1d3SxeHnjbZR6KGG|c3H5 NXG5b4g3hjFizszN NIjFdXJGTDVyPUKyJI5O MVOxOVA1OzRyNx?=
LCNaP Mn:zZ5l1d3SxeHnjbZR6KGG|c3H5 M4L0ep4yKM7:TR?= NFXUVZFGTDVyPUK4JI5O M3jldlE2ODR|NEC3
Lu1 MnTyZ5l1d3SxeHnjbZR6KGG|c3H5 NG[xeZB,OSEQvF2= NITPWZlGTDVyPUK5JI5O Mnn2NVUxPDN2MEe=
RPMI8402 MXfjfZRwfG:6aXPpeJkh[XO|YYm= NEfEcZV,OTBizszN MVnJR|UxRTZibl2= M1\IeFE2PDh{OUK5
CPT-K5 NWT4VIl3[3m2b4TvfIlkcXS7IHHzd4F6 MV;+NVAh|ryP MXPJR|UxRjFyIN88US=> MmDjNVU1QDJ7Mkm=
P388 NHLUUm1kgXSxdH;4bYNqfHliYYPzZZk> MlyyglExKM7:TR?= M1vQbmlEPTB;MUSgcm0> NV\IcoNFOTV2OEK5Nlk>
P388/CPT45 NHjIVZhkgXSxdH;4bYNqfHliYYPzZZk> MVL+NVAh|ryP NHfIfWJKSzVyPkGwJO69VQ>? NHzlN3cyPTR6MkmyPS=>
KB3-1 Mk\aZ5l1d3SxeHnjbZR6KGG|c3H5 M4jxZ54yOCEQvF2= M3LwXmlEPTB;NECgcm0> M4LLW|E2PDh{OUK5
KBV-1 + MDR1 NF:wS3BkgXSxdH;4bYNqfHliYYPzZZk> M1\Wd54yOCEQvF2= NYXR[ItjUUN3ME20OFAhdk1? MYWxOVQ5Ojl{OR?=
KBH MV7jfZRwfG:6aXPpeJkh[XO|YYm= NX60U2lJhjFyIN88US=> M1nBWmlEPTB;NESwJI5O Mn7aNVU1QDJ7Mkm=
HOP-62 MWrjfZRwfG:6aXPpeJkh[XO|YYm= MmHDglExKM7:TR?= NXvU[nFlT0l3ME2xNEBvVQ>? NFezUG8yPTVyOUG2OC=>
HCT-116 M4H1bIN6fG:2b4jpZ4l1gSCjc4PhfS=> NFS1cVN,OTBizszN MV;HTVUxRTNyIH7N NHGweGcyPTVyOUG2OC=>
F-539 M1HGNoN6fG:2b4jpZ4l1gSCjc4PhfS=> Mkn6glExKM7:TR?= MX\HTVUxRTFyIH7N NHPJSnUyPTVyOUG2OC=>
UACC-62 NHXsR3VkgXSxdH;4bYNqfHliYYPzZZk> MXz+NVAh|ryP MnjpS2k2OD1zMDDuUS=> M4rrO|E2PTB7MU[0
OVCAR-3 NHXtR4pkgXSxdH;4bYNqfHliYYPzZZk> NF2xNVZ,OTBizszN M1\MdmdKPTB;MkKwJI5O NIe0d5cyPTVyOUG2OC=>
SN12C M3vMN4N6fG:2b4jpZ4l1gSCjc4PhfS=> M4L2R54yOCEQvF2= MUXHTVUxRTJyIH7N NVnRcWtPOTV3MEmxOlQ>
DU-145 M3jIO4N6fG:2b4jpZ4l1gSCjc4PhfS=> MYj+NVAh|ryP NXGzd2t7T0l3ME2xNEBvVQ>? MUSxOVUxQTF4NB?=
MDA-MB-435 MYnjfZRwfG:6aXPpeJkh[XO|YYm= NGPYZ2d,OTBizszN MojaS2k2OD12MDDuUS=> M1W4OlE2PTB7MU[0
MT-4 NInndoZkgXSxdH;4bYNqfHliYYPzZZk> MWTJR|UxRTRibl2= NWHWfmd2OTd{NUS2Olk>
CCRF-CEMc NH\6TGRkgXSxdH;4bYNqfHliYYPzZZk> M4DHd2lEPTB;MzDuUS=> NHriOYIyPzJ3NE[2PS=>
WIL-2NSd M1zzV4N6fG:2b4jpZ4l1gSCjc4PhfS=> M4LwSGlEPTB;NTDuUS=> MnvRNVczPTR4Nkm=
CCRF-SB MWXjfZRwfG:6aXPpeJkh[XO|YYm= MmfUTWM2OD1|IH7N MoS5NVczPTR4Nkm=
CRL 7065 MoLCZ5l1d3SxeHnjbZR6KGG|c3H5 M3jINGlEPTB;NECwJI5O MnrBNVczPTR4Nkm=
SK-MEL-28b M{fpTYN6fG:2b4jpZ4l1gSCjc4PhfS=> MVTJR|UxRTRyIH7N MV:xO|I2PDZ4OR?=
MCF-7 MVjjfZRwfG:6aXPpeJkh[XO|YYm= MXPJR|UxRTRyIH7N M1jVblE4OjV2Nk[5
SKMES-1 NUTHZnpo[3m2b4TvfIlkcXS7IHHzd4F6 MX\JR|UxRTFyIH7N M1K1dlE4OjV2Nk[5
HepG2 MYHjfZRwfG:6aXPpeJkh[XO|YYm= NXXY[4o4UUN3ME2zNEBvVQ>? MV:xO|I2PDZ4OR?=
DU145 NFrhXXBkgXSxdH;4bYNqfHliYYPzZZk> MWPJR|UxRTFyIH7N NXP5c5BzOTd{NUS2Olk>

... 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

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