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.

  • 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 MoD6Z5l1d3SxeHnjbZR6KGG|c3H5 NYHXS|ZiUUN3ME21NUBvVQ>? MYS5NFA{PTJy
SKVLB Mn7IZ5l1d3SxeHnjbZR6KGG|c3H5 MUTJR|UxRTV|IH7N MV[5NFA{PTJy
HT29 NFzIU2hkgXSxdH;4bYNqfHliYYPzZZk> M{PBUGlEPTB;OEeuPEBvVQ>? NVzifJZ4QTByM{WyNC=>
KB MkfVZ5l1d3SxeHnjbZR6KGG|c3H5 Mm\aTWM2OD16IH7N NF2wZms6ODB|NUKw
A427 MknvS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mly0glEh|ryP MlfKSG1UVw>? MXrJR|UxRTJ2IH7N MnWzPVg4PjFzMR?=
PC-3 NIXPb3FIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHPJOXN,OSEQvF2= NInJWYNFVVOR NVrrSIl2UUN3ME21O{BvVQ>? NVfCOHNbQTh5NkGxNS=>
K562adr MkP6S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NWLxVldQhjFizszN MlvUSG1UVw>? MULJR|UxRTV5IH7N NIThbVY6QDd4MUGx
MCF7mdr M4CxeGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXTjdmR4hjFizszN M{jLTWROW09? NVG5UZZzUUN3ME2zMlEhdk1? NFzOboI6QDd4MUGx
P388 Mlz3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M{\jXWlEPTB;M{Kgcm0> MVuxNFM1Pjl|Mx?=
P388CPT5 R MV7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4fsPWlEPTB;Mj64JO69VQ>? M37melExOzR4OUOz
KBwt NGDqfolIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NF\aTWJKSzVyPUSwJI5O NX\BNWxVOTB2MUG0O|Y>
KBMDR NVe4dIhuT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVX3[lVzUUN3ME23NEBvVQ>? MX:xNFQyOTR5Nh?=
KBV20C MlvHS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NUC2Z4VCUUN3ME2zNEBvVQ>? MmD0NVA1OTF2N{[=
KB7D MnnUS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXjaTZc{UUN3ME2zOUBvVQ>? Ml7tNVA1OTF2N{[=
KBCamp NUP5[WI4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGXzUnRKSzVyPUGuNFQh|ryP MXexNFQyOTR5Nh?=
HT29 Mn7GZ5l1d3SxeHnjbZR6KGG|c3H5 NX\iTollUUN3ME24NEBvVQ>? NGDleI0yODh2MUiwPC=>
A549 NH3OR2dkgXSxdH;4bYNqfHliYYPzZZk> NY[yXFNmUUN3ME22O{BvVQ>? MnvFNVA5PDF6MEi=
T24 MYXjfZRwfG:6aXPpeJkh[XO|YYm= MVXJR|UxRTh6IH7N NWHrO41LOTB6NEG4NFg>
HOP-62 M2Due2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MnzWTWM2OD1zMDDuUS=> MUOxNVAzODJ6Mx?=
HCT-116 MoLFS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWrJR|UxRTNyIH7N M{D5WFEyODJyMkiz
SF-539 MWPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MmHrTWM2OD1zMDDuUS=> MmHxNVExOjB{OEO=
UACC-62 M2HuU2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MlG2TWM2OD1zMDDuUS=> NIn0ZYQyOTB{MEK4Ny=>
OVCAR-3 NGXLPJVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MmDITWM2OD1{MkCgcm0> MYqxNVAzODJ6Mx?=
SN12C M{fvXmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1j1dWlEPTB;MkCgcm0> MV6xNVAzODJ6Mx?=
DU-145 Mk\wS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2XYSGlEPTB;MUCgcm0> NV24PG1LOTFyMkCyPFM>
MDA-MB-435 MnT1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnLOTWM2OD12MDDuUS=> NHHZbJEyOTB{MEK4Ny=>
WiDr MVTjfZRwfG:6aXPpeJkh[XO|YYm= MYTEUXNQ M17PbGlEPTB;MUegcm0> MlPBNVE{OzR3Nkm=
A549 NIXpVItkgXSxdH;4bYNqfHliYYPzZZk> NITD[JpFVVOR NHrpNWdKSzVyPUG0JI5O MkLzNVE{OzR3Nkm=
MKN45 NVvtT4l[[3m2b4TvfIlkcXS7IHHzd4F6 M13jbmROW09? M3LhdmlEPTB;MUegcm0> MYKxNVM{PDV4OR?=
SK-OV-3 MnrRZ5l1d3SxeHnjbZR6KGG|c3H5 NGHsOJlFVVOR NYmyRXFJUUN3ME2yNEBvVQ>? NVzIOXB[OTF|M{S1Olk>
H128 NX\J[WRP[3m2b4TvfIlkcXS7IHHzd4F6 MWXEUXNQ M1fHW2lEPTB;MUigcm0> NXWxbHpIOTF|M{S1Olk>
SK-BR-3 NHzkeGpkgXSxdH;4bYNqfHliYYPzZZk> MkXGSG1UVw>? NVXOeppzUUN3ME2yNEBvVQ>? NVzEdnBFOTF|M{S1Olk>
LX-1 MoXIZ5l1d3SxeHnjbZR6KGG|c3H5 MYXEUXNQ NFvsR4JKSzVyPUGyNEBvVQ>? NIOzdY4yOTh3OEezOy=>
HCT116 NX\mT3Rb[3m2b4TvfIlkcXS7IHHzd4F6 M3v0XWROW09? MkPZTWM2OD17IH7N MVGxNVg2QDd|Nx?=
A2780 MYfjfZRwfG:6aXPpeJkh[XO|YYm= NXvGUXJtTE2VTx?= NGjzUJNKSzVyPUSgcm0> NEHybFUyOTh3OEezOy=>
IMR-32 NXKxZWdx[3m2b4TvfIlkcXS7IHHzd4F6 NHPJ[49,OTBizszN MXLEUXNQ NHTLZ|hKSzVyPUKuNlEhdk1? MkXUNVI3OTd6OUS=
P388 M37ZO4N6fG:2b4jpZ4l1gSCjc4PhfS=> NVTJ[FlCUUN3ME2xN{BvVQ>? MmP2NVI3OjByOEG=
Lewis MVzjfZRwfG:6aXPpeJkh[XO|YYm= M12wZWlEPTB;M{Ogcm0> M4f5VVEzPjJyMEix
JLC M4L1RYN6fG:2b4jpZ4l1gSCjc4PhfS=> M3jHRmlEPTB;NT62JI5O NEHvTXoyOjZ{MEC4NS=>
HT-29 NGW1eIFkgXSxdH;4bYNqfHliYYPzZZk> NIDNXWNKSzVyPUGuOEDPxE1? MmHvNVI3Ozl3NEG=
Caki-2 MofOZ5l1d3SxeHnjbZR6KGG|c3H5 NV\qNYNVUUN3ME2zMlk3KM7:TR?= Mn\aNVI3Ozl3NEG=
A549 M4e4doN6fG:2b4jpZ4l1gSCjc4PhfS=> NH7WbZZKSzVyPUKuOVMh|ryP MUOxNlY{QTV2MR?=
HEC-1-B MnHXZ5l1d3SxeHnjbZR6KGG|c3H5 M{LTS2lEPTB;OD62OEDPxE1? NYLvfWlIOTJ4M{m1OFE>
HL-60 M{HIboN6fG:2b4jpZ4l1gSCjc4PhfS=> NWH6PFhMUUN3ME22OkBvVQ>? M2LHOVEzPjN7NUSx
Col2 M2nIfoN6fG:2b4jpZ4l1gSCjc4PhfS=> MU\+NUDPxE1? Mlz1SWQ2OD13NzDuUS=> MXOxOVA1OzRyNx?=
HUVEC NHfqPFFkgXSxdH;4bYNqfHliYYPzZZk> NXXiNY43hjFizszN MorBSWQ2OD1{NUigcm0> NWOwZYhpOTVyNEO0NFc>
KB M1\0boN6fG:2b4jpZ4l1gSCjc4PhfS=> NUPtblQyhjFizszN M{\pOmVFPTB;MkKgcm0> M1PBe|E2ODR|NEC3
LCNaP MXLjfZRwfG:6aXPpeJkh[XO|YYm= M1;WT54yKM7:TR?= NHzNenVGTDVyPUK4JI5O NHXoPFQyPTB2M{SwOy=>
Lu1 NHqzd2hkgXSxdH;4bYNqfHliYYPzZZk> MXj+NUDPxE1? NULx[XFvTUR3ME2yPUBvVQ>? NWPvS|N3OTVyNEO0NFc>
RPMI8402 MVfjfZRwfG:6aXPpeJkh[XO|YYm= MV3+NVAh|ryP MWnJR|UxRTZibl2= MWixOVQ5Ojl{OR?=
CPT-K5 MUTjfZRwfG:6aXPpeJkh[XO|YYm= NIPz[nJ,OTBizszN M1;x[GlEPTB-MUCg{txO NWDtOm1MOTV2OEK5Nlk>
P388 NYTtZ246[3m2b4TvfIlkcXS7IHHzd4F6 NGHZZ2p,OTBizszN M3rwe2lEPTB;MUSgcm0> MW[xOVQ5Ojl{OR?=
P388/CPT45 MV;jfZRwfG:6aXPpeJkh[XO|YYm= M4fvfJ4yOCEQvF2= MYfJR|UxRjFyIN88US=> MV[xOVQ5Ojl{OR?=
KB3-1 NFzkTFNkgXSxdH;4bYNqfHliYYPzZZk> NVv5[nhVhjFyIN88US=> NYDZSohpUUN3ME20NEBvVQ>? MVWxOVQ5Ojl{OR?=
KBV-1 + MDR1 NVnyNlE6[3m2b4TvfIlkcXS7IHHzd4F6 MVv+NVAh|ryP MnPKTWM2OD12NECgcm0> NVm2ZZJtOTV2OEK5Nlk>
KBH M2nWU4N6fG:2b4jpZ4l1gSCjc4PhfS=> NG[xUGt,OTBizszN NIPEOGxKSzVyPUS0NEBvVQ>? NYnhVXhCOTV2OEK5Nlk>
HOP-62 MWjjfZRwfG:6aXPpeJkh[XO|YYm= NXHGXoFWhjFyIN88US=> M{XWWGdKPTB;MUCgcm0> NHXRXngyPTVyOUG2OC=>
HCT-116 MXnjfZRwfG:6aXPpeJkh[XO|YYm= MXH+NVAh|ryP M{HZbmdKPTB;M{Cgcm0> M{TGfFE2PTB7MU[0
F-539 M{TwU4N6fG:2b4jpZ4l1gSCjc4PhfS=> MoLHglExKM7:TR?= MXfHTVUxRTFyIH7N MnXwNVU2ODlzNkS=
UACC-62 MWfjfZRwfG:6aXPpeJkh[XO|YYm= NXPCSW5UhjFyIN88US=> MlXlS2k2OD1zMDDuUS=> Mk\jNVU2ODlzNkS=
OVCAR-3 NH:ze4FkgXSxdH;4bYNqfHliYYPzZZk> NVu2RYNQhjFyIN88US=> M1Xlb2dKPTB;MkKwJI5O MnTqNVU2ODlzNkS=
SN12C M37RNYN6fG:2b4jpZ4l1gSCjc4PhfS=> MoXUglExKM7:TR?= NGjBfVhIUTVyPUKwJI5O NIHxXo0yPTVyOUG2OC=>
DU-145 NFu5NWFkgXSxdH;4bYNqfHliYYPzZZk> MYX+NVAh|ryP MVLHTVUxRTFyIH7N NGPNWYQyPTVyOUG2OC=>
MDA-MB-435 Mnj0Z5l1d3SxeHnjbZR6KGG|c3H5 NHSwVHp,OTBizszN NFfSXZJIUTVyPUSwJI5O NUTjWpI5OTV3MEmxOlQ>
MT-4 M3n2UoN6fG:2b4jpZ4l1gSCjc4PhfS=> NED4fnlKSzVyPUSgcm0> NGezenIyPzJ3NE[2PS=>
CCRF-CEMc NILlNJlkgXSxdH;4bYNqfHliYYPzZZk> NHHiWG9KSzVyPUOgcm0> MVyxO|I2PDZ4OR?=
WIL-2NSd MliyZ5l1d3SxeHnjbZR6KGG|c3H5 MVLJR|UxRTVibl2= Mn\JNVczPTR4Nkm=
CCRF-SB M1nRdoN6fG:2b4jpZ4l1gSCjc4PhfS=> NV2wUmV6UUN3ME2zJI5O NUHUUW1LOTd{NUS2Olk>
CRL 7065 NULpR3h1[3m2b4TvfIlkcXS7IHHzd4F6 MWPJR|UxRTRyMDDuUS=> NILoeFcyPzJ3NE[2PS=>
SK-MEL-28b NGfhTGFkgXSxdH;4bYNqfHliYYPzZZk> MWXJR|UxRTRyIH7N MYmxO|I2PDZ4OR?=
MCF-7 MXfjfZRwfG:6aXPpeJkh[XO|YYm= NHi2SlZKSzVyPUSwJI5O M3myeVE4OjV2Nk[5
SKMES-1 M17CXYN6fG:2b4jpZ4l1gSCjc4PhfS=> NWqxVVRNUUN3ME2xNEBvVQ>? NGHxeFkyPzJ3NE[2PS=>
HepG2 NUewblMx[3m2b4TvfIlkcXS7IHHzd4F6 NUn0XJhmUUN3ME2zNEBvVQ>? NUDWcG5yOTd{NUS2Olk>
DU145 MnrpZ5l1d3SxeHnjbZR6KGG|c3H5 NUXZ[otqUUN3ME2xNEBvVQ>? M3TTS|E4OjV2Nk[5

... 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 <1 mg/mL
Ethanol <1 mg/mL
In vivo

* 1 mg/ml means slightly soluble or 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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Molecular Weight Calculator

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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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