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 NV7ifoFK[3m2b4TvfIlkcXS7IHHzd4F6 MYPJR|UxRTVzIH7N NU\PT4llQTByM{WyNC=>
SKVLB MVrjfZRwfG:6aXPpeJkh[XO|YYm= M{Pk[2lEPTB;NUOgcm0> MYG5NFA{PTJy
HT29 NV7OSIgx[3m2b4TvfIlkcXS7IHHzd4F6 MojtTWM2OD16Nz64JI5O M17HTFkxODN3MkC=
KB NUfzdmJw[3m2b4TvfIlkcXS7IHHzd4F6 MYXJR|UxRThibl2= MYK5NFA{PTJy
A427 NXi2PYp3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1;abp4yKM7:TR?= NFnzbIZFVVOR MUTJR|UxRTJ2IH7N NFTtUm06QDd4MUGx
PC-3 NXf0SnMzT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXz+NUDPxE1? MWrEUXNQ M4Tw[GlEPTB;NUegcm0> MkPvPVg4PjFzMR?=
K562adr NHHV[3VIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUT+NUDPxE1? NXy5bItTTE2VTx?= NUHYdWx{UUN3ME21O{BvVQ>? M1zU[Vk5PzZzMUG=
MCF7mdr M2fyNGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NWnYb3Z2hjFizszN MlGySG1UVw>? M{HuXmlEPTB;Mz6xJI5O MoXRPVg4PjFzMR?=
P388 MXTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFL5bnFKSzVyPUOyJI5O M2jDe|ExOzR4OUOz
P388CPT5 R MYrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NIXDS2FKSzVyPUKuPEDPxE1? MVqxNFM1Pjl|Mx?=
KBwt MYnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWLQR4RDUUN3ME20NEBvVQ>? Mo\JNVA1OTF2N{[=
KBMDR M1fzZ2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MUPJR|UxRTdyIH7N NEH0RlMyODRzMUS3Oi=>
KBV20C NGPMOVRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXPJR|UxRTNyIH7N NXzTZ3FCOTB2MUG0O|Y>
KB7D M{fWcmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVXtSXVqUUN3ME2zOUBvVQ>? Mn\2NVA1OTF2N{[=
KBCamp M3r3XWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NWH3SWVkUUN3ME2xMlA1KM7:TR?= M1j4NlExPDFzNEe2
HT29 M{XpVIN6fG:2b4jpZ4l1gSCjc4PhfS=> NVXqbXRPUUN3ME24NEBvVQ>? M2HxVlExQDRzOEC4
A549 MnG4Z5l1d3SxeHnjbZR6KGG|c3H5 MoDPTWM2OD14NzDuUS=> MljlNVA5PDF6MEi=
T24 NWfUVJI2[3m2b4TvfIlkcXS7IHHzd4F6 M33PTWlEPTB;OEigcm0> NWHzdHBFOTB6NEG4NFg>
HOP-62 NWrwe4Z3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUjJR|UxRTFyIH7N NY[wUGt[OTFyMkCyPFM>
HCT-116 MkG1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NEDUW|lKSzVyPUOwJI5O NGfJTHQyOTB{MEK4Ny=>
SF-539 NE\rfoZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXHHSGN[UUN3ME2xNEBvVQ>? MnLPNVExOjB{OEO=
UACC-62 NFnyOWNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NUXDbY46UUN3ME2xNEBvVQ>? NH;IemEyOTB{MEK4Ny=>
OVCAR-3 MlPuS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1nwfmlEPTB;MkKwJI5O M3f0[lEyODJyMkiz
SN12C NXGzRlJ2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MoC4TWM2OD1{MDDuUS=> MmfWNVExOjB{OEO=
DU-145 MYrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWTuWIxUUUN3ME2xNEBvVQ>? NWn3[Go3OTFyMkCyPFM>
MDA-MB-435 NXnNSZNlT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXrVdItsUUN3ME20NEBvVQ>? M4rid|EyODJyMkiz
WiDr MUTjfZRwfG:6aXPpeJkh[XO|YYm= NVH5bXZnTE2VTx?= NEHPU5BKSzVyPUG3JI5O MlvZNVE{OzR3Nkm=
A549 NI\sVHZkgXSxdH;4bYNqfHliYYPzZZk> NHzVc|hFVVOR MVLJR|UxRTF2IH7N M4DjdFEyOzN2NU[5
MKN45 NUf6fGVb[3m2b4TvfIlkcXS7IHHzd4F6 NFvSVJBFVVOR NVe0T2xEUUN3ME2xO{BvVQ>? MlLJNVE{OzR3Nkm=
SK-OV-3 M2nYUIN6fG:2b4jpZ4l1gSCjc4PhfS=> M4PkN2ROW09? NX;6cYZGUUN3ME2yNEBvVQ>? Mn3VNVE{OzR3Nkm=
H128 MWPjfZRwfG:6aXPpeJkh[XO|YYm= MVHEUXNQ MU\JR|UxRTF6IH7N NXzmNJU1OTF|M{S1Olk>
SK-BR-3 MnrNZ5l1d3SxeHnjbZR6KGG|c3H5 MljDSG1UVw>? MmnQTWM2OD1{MDDuUS=> MYexNVM{PDV4OR?=
LX-1 NIfpdnZkgXSxdH;4bYNqfHliYYPzZZk> NETFPJRFVVOR M325OGlEPTB;MUKwJI5O NVXBbJlmOTF6NUi3N|c>
HCT116 MXnjfZRwfG:6aXPpeJkh[XO|YYm= MUjEUXNQ NWLzfXlnUUN3ME25JI5O M1TZZ|EyQDV6N{O3
A2780 MmDZZ5l1d3SxeHnjbZR6KGG|c3H5 MXLEUXNQ MlPETWM2OD12IH7N MV:xNVg2QDd|Nx?=
IMR-32 NF3hfWVkgXSxdH;4bYNqfHliYYPzZZk> MXL+NVAh|ryP NXe3elFnTE2VTx?= MlK0TWM2OD1{LkKxJI5O NUHBNHRDOTJ4MUe4PVQ>
P388 NXnObnUy[3m2b4TvfIlkcXS7IHHzd4F6 NU\4[3FEUUN3ME2xN{BvVQ>? NWDPZ3BDOTJ4MkCwPFE>
Lewis NVzFVVBG[3m2b4TvfIlkcXS7IHHzd4F6 M2DpUmlEPTB;M{Ogcm0> NID5b3AyOjZ{MEC4NS=>
JLC NW\LW4ZJ[3m2b4TvfIlkcXS7IHHzd4F6 MmXvTWM2OD13Lk[gcm0> M3TsfFEzPjJyMEix
HT-29 MmPEZ5l1d3SxeHnjbZR6KGG|c3H5 M4DJcWlEPTB;MT60JO69VQ>? NVLCNHVvOTJ4M{m1OFE>
Caki-2 NXnLdGQ4[3m2b4TvfIlkcXS7IHHzd4F6 MnLyTWM2OD1|Lkm2JO69VQ>? NVTmbYpROTJ4M{m1OFE>
A549 MV;jfZRwfG:6aXPpeJkh[XO|YYm= NYXYZ5k5UUN3ME2yMlU{KM7:TR?= MkfaNVI3Ozl3NEG=
HEC-1-B NFLMVZJkgXSxdH;4bYNqfHliYYPzZZk> NVrpXmF1UUN3ME24MlY1KM7:TR?= MWqxNlY{QTV2MR?=
HL-60 NH;1T4ZkgXSxdH;4bYNqfHliYYPzZZk> MUXJR|UxRTZ4IH7N MVmxNlY{QTV2MR?=
Col2 M4D2O4N6fG:2b4jpZ4l1gSCjc4PhfS=> NX7pNIlyhjFizszN M2SyR2VFPTB;NUegcm0> MlfVNVUxPDN2MEe=
HUVEC NXf0WYR[[3m2b4TvfIlkcXS7IHHzd4F6 MYj+NUDPxE1? NGPwTWRGTDVyPUK1PEBvVQ>? MlrnNVUxPDN2MEe=
KB MWLjfZRwfG:6aXPpeJkh[XO|YYm= NYnCTHFjhjFizszN MYXFSFUxRTJ{IH7N MXmxOVA1OzRyNx?=
LCNaP NEP2OmxkgXSxdH;4bYNqfHliYYPzZZk> M1iyUZ4yKM7:TR?= Mn7ESWQ2OD1{ODDuUS=> MlTmNVUxPDN2MEe=
Lu1 MoLKZ5l1d3SxeHnjbZR6KGG|c3H5 M4nhbp4yKM7:TR?= M1ztbmVFPTB;Mkmgcm0> Mn7wNVUxPDN2MEe=
RPMI8402 NYL6W3N2[3m2b4TvfIlkcXS7IHHzd4F6 MUf+NVAh|ryP MUHJR|UxRTZibl2= MYixOVQ5Ojl{OR?=
CPT-K5 M4rPSYN6fG:2b4jpZ4l1gSCjc4PhfS=> NYfEblI3hjFyIN88US=> MX7JR|UxRjFyIN88US=> M{P6SVE2PDh{OUK5
P388 M3fZV4N6fG:2b4jpZ4l1gSCjc4PhfS=> MlHMglExKM7:TR?= NGTnNJhKSzVyPUG0JI5O M3X1blE2PDh{OUK5
P388/CPT45 NHjzPYZkgXSxdH;4bYNqfHliYYPzZZk> NYD3RXZqhjFyIN88US=> MlnITWM2OD5zMDFOwG0> M3PyclE2PDh{OUK5
KB3-1 M3HQRYN6fG:2b4jpZ4l1gSCjc4PhfS=> MVL+NVAh|ryP NHznSW1KSzVyPUSwJI5O NH:0VXQyPTR6MkmyPS=>
KBV-1 + MDR1 MkDEZ5l1d3SxeHnjbZR6KGG|c3H5 MkTyglExKM7:TR?= M3W4WmlEPTB;NESwJI5O NEnPbmUyPTR6MkmyPS=>
KBH NXzhdph[[3m2b4TvfIlkcXS7IHHzd4F6 MXT+NVAh|ryP Mn\6TWM2OD12NECgcm0> MlrZNVU1QDJ7Mkm=
HOP-62 MYfjfZRwfG:6aXPpeJkh[XO|YYm= Mm\wglExKM7:TR?= MnfoS2k2OD1zMDDuUS=> MlntNVU2ODlzNkS=
HCT-116 M3u4O4N6fG:2b4jpZ4l1gSCjc4PhfS=> NY[wZVQyhjFyIN88US=> MkP4S2k2OD1|MDDuUS=> M1v2b|E2PTB7MU[0
F-539 M{OzSIN6fG:2b4jpZ4l1gSCjc4PhfS=> M13UNp4yOCEQvF2= NETQSZlIUTVyPUGwJI5O M3rCO|E2PTB7MU[0
UACC-62 NYTXb3V3[3m2b4TvfIlkcXS7IHHzd4F6 NUm0PGxxhjFyIN88US=> NVjFb|E4T0l3ME2xNEBvVQ>? MonONVU2ODlzNkS=
OVCAR-3 M{jJ[oN6fG:2b4jpZ4l1gSCjc4PhfS=> NUTYbItbhjFyIN88US=> MoLJS2k2OD1{MkCgcm0> M4nzRVE2PTB7MU[0
SN12C M1nVXIN6fG:2b4jpZ4l1gSCjc4PhfS=> NXPNRWhLhjFyIN88US=> MUPHTVUxRTJyIH7N NHrSW|gyPTVyOUG2OC=>
DU-145 NXLFOJBr[3m2b4TvfIlkcXS7IHHzd4F6 M3zxdJ4yOCEQvF2= Ml;SS2k2OD1zMDDuUS=> NVfRZXdDOTV3MEmxOlQ>
MDA-MB-435 NWn6U4R6[3m2b4TvfIlkcXS7IHHzd4F6 MnvaglExKM7:TR?= M4LBRWdKPTB;NECgcm0> MmnXNVU2ODlzNkS=
MT-4 NG\JXphkgXSxdH;4bYNqfHliYYPzZZk> NXvu[WViUUN3ME20JI5O NVe5fZJ[OTd{NUS2Olk>
CCRF-CEMc NEPmWJdkgXSxdH;4bYNqfHliYYPzZZk> NHPVdoNKSzVyPUOgcm0> M3\LU|E4OjV2Nk[5
WIL-2NSd NV7hZnU1[3m2b4TvfIlkcXS7IHHzd4F6 NIPMUINKSzVyPUWgcm0> NWLsenV5OTd{NUS2Olk>
CCRF-SB M37KTYN6fG:2b4jpZ4l1gSCjc4PhfS=> NF\nZXJKSzVyPUOgcm0> M3fwO|E4OjV2Nk[5
CRL 7065 MmTkZ5l1d3SxeHnjbZR6KGG|c3H5 NVWzV|dJUUN3ME20NFAhdk1? NGPPZpoyPzJ3NE[2PS=>
SK-MEL-28b M4HLVYN6fG:2b4jpZ4l1gSCjc4PhfS=> MnTSTWM2OD12MDDuUS=> NWrSU3I4OTd{NUS2Olk>
MCF-7 MnzDZ5l1d3SxeHnjbZR6KGG|c3H5 NV3QXVBjUUN3ME20NEBvVQ>? M1v5RVE4OjV2Nk[5
SKMES-1 NGTLVHpkgXSxdH;4bYNqfHliYYPzZZk> MoP1TWM2OD1zMDDuUS=> MVixO|I2PDZ4OR?=
HepG2 M{LrUIN6fG:2b4jpZ4l1gSCjc4PhfS=> M{LWRmlEPTB;M{Cgcm0> MXexO|I2PDZ4OR?=
DU145 M1\X[IN6fG:2b4jpZ4l1gSCjc4PhfS=> M2DwZWlEPTB;MUCgcm0> MljzNVczPTR4Nkm=

... 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