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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3 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.

  • 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

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 NXXae5dw[3m2b4TvfIlkcXS7IHHzd4F6 MV3JR|UxRTVzIH7N NVHsfYFxQTByM{WyNC=>
SKVLB MoHSZ5l1d3SxeHnjbZR6KGG|c3H5 MVjJR|UxRTV|IH7N MYC5NFA{PTJy
HT29 M{H2NYN6fG:2b4jpZ4l1gSCjc4PhfS=> MUPJR|UxRTh5Lkigcm0> M4XuPVkxODN3MkC=
KB MYfjfZRwfG:6aXPpeJkh[XO|YYm= NXO4RmhJUUN3ME24JI5O NHy1So86ODB|NUKw
A427 M{O2Omdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1y4S54yKM7:TR?= NGqyUnVFVVOR NHG4U4lKSzVyPUK0JI5O MXG5PFc3OTFz
PC-3 NEHBcZhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mo\oglEh|ryP NYPhfFJlTE2VTx?= Mn\yTWM2OD13NzDuUS=> NULmVY9SQTh5NkGxNS=>
K562adr MXjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFHKbmR,OSEQvF2= NVPxOZFUTE2VTx?= MkHjTWM2OD13NzDuUS=> M1y4ZVk5PzZzMUG=
MCF7mdr NI\BVFFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWn+NUDPxE1? NHO5WmxFVVOR M3T5T2lEPTB;Mz6xJI5O NFL4ZYE6QDd4MUGx
P388 MXrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYPQOlRpUUN3ME2zNkBvVQ>? NGPSTWoyODN2NkmzNy=>
P388CPT5 R M4r1emdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYLJR|UxRTJwODFOwG0> NYe3eJF7OTB|NE[5N|M>
KBwt MVXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1PCR2lEPTB;NECgcm0> NVT1[4ROOTB2MUG0O|Y>
KBMDR M3TNWGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYnJR|UxRTdyIH7N M1HCeFExPDFzNEe2
KBV20C NHPMeINIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NETZRpVKSzVyPUOwJI5O M1LsOFExPDFzNEe2
KB7D M4m0Smdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NV34[45oUUN3ME2zOUBvVQ>? M1vXRlExPDFzNEe2
KBCamp M2XtPGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXjxdo5WUUN3ME2xMlA1KM7:TR?= MXixNFQyOTR5Nh?=
HT29 NXLTbZp7[3m2b4TvfIlkcXS7IHHzd4F6 NX\idXlXUUN3ME24NEBvVQ>? NYfqUpkxOTB6NEG4NFg>
A549 NVfxWpBR[3m2b4TvfIlkcXS7IHHzd4F6 MWLJR|UxRTZ5IH7N MmDHNVA5PDF6MEi=
T24 M4jFWIN6fG:2b4jpZ4l1gSCjc4PhfS=> MkLWTWM2OD16ODDuUS=> NYf0SlduOTB6NEG4NFg>
HOP-62 MW\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHTMRYpKSzVyPUGwJI5O MUOxNVAzODJ6Mx?=
HCT-116 MW\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnK0TWM2OD1|MDDuUS=> M1jYWlEyODJyMkiz
SF-539 MoDlS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1m0RmlEPTB;MUCgcm0> MWWxNVAzODJ6Mx?=
UACC-62 NGHw[45Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWTJR|UxRTFyIH7N NF\RSFAyOTB{MEK4Ny=>
OVCAR-3 Mk\lS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NILMdWhKSzVyPUKyNEBvVQ>? Mm\BNVExOjB{OEO=
SN12C NH3YWYxIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4nMb2lEPTB;MkCgcm0> MnjxNVExOjB{OEO=
DU-145 M2XWWWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NULvT|RwUUN3ME2xNEBvVQ>? NGnHeZUyOTB{MEK4Ny=>
MDA-MB-435 NI\LbVdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NYLSNJpkUUN3ME20NEBvVQ>? NFe3dGgyOTB{MEK4Ny=>
WiDr M1TKeYN6fG:2b4jpZ4l1gSCjc4PhfS=> Mo\LSG1UVw>? NYnIfGdjUUN3ME2xO{BvVQ>? NI[4d2oyOTN|NEW2PS=>
A549 NITMUVRkgXSxdH;4bYNqfHliYYPzZZk> MVfEUXNQ NHfhRVZKSzVyPUG0JI5O NXS2VplzOTF|M{S1Olk>
MKN45 MnzMZ5l1d3SxeHnjbZR6KGG|c3H5 M2frVmROW09? NEDmRZRKSzVyPUG3JI5O MmfTNVE{OzR3Nkm=
SK-OV-3 MWHjfZRwfG:6aXPpeJkh[XO|YYm= MmDESG1UVw>? NWnWeoR[UUN3ME2yNEBvVQ>? M4nRXVEyOzN2NU[5
H128 NHvxfGZkgXSxdH;4bYNqfHliYYPzZZk> M4HXNmROW09? NGDZPYhKSzVyPUG4JI5O NVLhNGRDOTF|M{S1Olk>
SK-BR-3 M2DicIN6fG:2b4jpZ4l1gSCjc4PhfS=> MnrrSG1UVw>? MVLJR|UxRTJyIH7N NXrxW5BkOTF|M{S1Olk>
LX-1 MV7jfZRwfG:6aXPpeJkh[XO|YYm= MoXBSG1UVw>? NYXt[IVHUUN3ME2xNlAhdk1? Mlf2NVE5PTh5M{e=
HCT116 M4Doc4N6fG:2b4jpZ4l1gSCjc4PhfS=> NUnPVWpqTE2VTx?= MVXJR|UxRTlibl2= M4jqVlEyQDV6N{O3
A2780 NV3hV4hZ[3m2b4TvfIlkcXS7IHHzd4F6 NVK2UVJvTE2VTx?= NEDKbGpKSzVyPUSgcm0> MYmxNVg2QDd|Nx?=
IMR-32 MmXYZ5l1d3SxeHnjbZR6KGG|c3H5 M1TmO54yOCEQvF2= MXLEUXNQ M4TzcGlEPTB;Mj6yNUBvVQ>? MlvjNVI3OTd6OUS=
P388 MYDjfZRwfG:6aXPpeJkh[XO|YYm= MoO1TWM2OD1zMzDuUS=> NGDCbpMyOjZ{MEC4NS=>
Lewis MUnjfZRwfG:6aXPpeJkh[XO|YYm= MV3JR|UxRTN|IH7N MnLONVI3OjByOEG=
JLC Mlu4Z5l1d3SxeHnjbZR6KGG|c3H5 MmX4TWM2OD13Lk[gcm0> MnvjNVI3OjByOEG=
HT-29 M1ztW4N6fG:2b4jpZ4l1gSCjc4PhfS=> Mmm1TWM2OD1zLkSg{txO NV;qSVdlOTJ4M{m1OFE>
Caki-2 NU\YXmhT[3m2b4TvfIlkcXS7IHHzd4F6 NUC1fJZuUUN3ME2zMlk3KM7:TR?= NFO3WpgyOjZ|OUW0NS=>
A549 MnXlZ5l1d3SxeHnjbZR6KGG|c3H5 NULIenZGUUN3ME2yMlU{KM7:TR?= NFvrU28yOjZ|OUW0NS=>
HEC-1-B MnnBZ5l1d3SxeHnjbZR6KGG|c3H5 MkfGTWM2OD16Lk[0JO69VQ>? NYK5XlZoOTJ4M{m1OFE>
HL-60 NVLPVppP[3m2b4TvfIlkcXS7IHHzd4F6 NWfsfpdLUUN3ME22OkBvVQ>? NG\DWYgyOjZ|OUW0NS=>
Col2 M3zQZ4N6fG:2b4jpZ4l1gSCjc4PhfS=> MkC3glEh|ryP MkDJSWQ2OD13NzDuUS=> M2n2RVE2ODR|NEC3
HUVEC NVfiSoYz[3m2b4TvfIlkcXS7IHHzd4F6 M2\qb54yKM7:TR?= M1fvU2VFPTB;MkW4JI5O M1nMPFE2ODR|NEC3
KB MYTjfZRwfG:6aXPpeJkh[XO|YYm= M4LaUp4yKM7:TR?= M37sPWVFPTB;MkKgcm0> MWqxOVA1OzRyNx?=
LCNaP NVPqU|R{[3m2b4TvfIlkcXS7IHHzd4F6 NWD6TIg3hjFizszN NXnhWHdDTUR3ME2yPEBvVQ>? MXGxOVA1OzRyNx?=
Lu1 NVv1[ZRD[3m2b4TvfIlkcXS7IHHzd4F6 NETOe2F,OSEQvF2= MlrISWQ2OD1{OTDuUS=> NHfI[28yPTB2M{SwOy=>
RPMI8402 MX;jfZRwfG:6aXPpeJkh[XO|YYm= MlfiglExKM7:TR?= NFfYeGJKSzVyPU[gcm0> MoDFNVU1QDJ7Mkm=
CPT-K5 M2nHc4N6fG:2b4jpZ4l1gSCjc4PhfS=> M13NXJ4yOCEQvF2= NFL2fHZKSzVyPkGwJO69VQ>? M2HadVE2PDh{OUK5
P388 M370foN6fG:2b4jpZ4l1gSCjc4PhfS=> NWLzZ245hjFyIN88US=> M2fjd2lEPTB;MUSgcm0> NWrsboViOTV2OEK5Nlk>
P388/CPT45 Mm\yZ5l1d3SxeHnjbZR6KGG|c3H5 MXL+NVAh|ryP MlS1TWM2OD5zMDFOwG0> NV:0Z5ZkOTV2OEK5Nlk>
KB3-1 Ml7CZ5l1d3SxeHnjbZR6KGG|c3H5 MXH+NVAh|ryP M1LPd2lEPTB;NECgcm0> NHzke44yPTR6MkmyPS=>
KBV-1 + MDR1 MlW2Z5l1d3SxeHnjbZR6KGG|c3H5 Mlr2glExKM7:TR?= Ml[1TWM2OD12NECgcm0> M3LIWlE2PDh{OUK5
KBH NWjNW4tJ[3m2b4TvfIlkcXS7IHHzd4F6 M2nIb54yOCEQvF2= MVzJR|UxRTR2MDDuUS=> M2HtUVE2PDh{OUK5
HOP-62 NVnwdoEz[3m2b4TvfIlkcXS7IHHzd4F6 NW\3VVVnhjFyIN88US=> M{XiPWdKPTB;MUCgcm0> M13LdFE2PTB7MU[0
HCT-116 MYLjfZRwfG:6aXPpeJkh[XO|YYm= NHzSdYV,OTBizszN NEnMPFVIUTVyPUOwJI5O MWSxOVUxQTF4NB?=
F-539 NHzHd21kgXSxdH;4bYNqfHliYYPzZZk> MoDjglExKM7:TR?= NUHLRVRRT0l3ME2xNEBvVQ>? MUmxOVUxQTF4NB?=
UACC-62 MXHjfZRwfG:6aXPpeJkh[XO|YYm= MYD+NVAh|ryP M1HDTWdKPTB;MUCgcm0> MWSxOVUxQTF4NB?=
OVCAR-3 MVzjfZRwfG:6aXPpeJkh[XO|YYm= MYH+NVAh|ryP M4rB[GdKPTB;MkKwJI5O NIC3XFUyPTVyOUG2OC=>
SN12C M1fMe4N6fG:2b4jpZ4l1gSCjc4PhfS=> NVLjU|Y5hjFyIN88US=> MUHHTVUxRTJyIH7N MVGxOVUxQTF4NB?=
DU-145 M1TydIN6fG:2b4jpZ4l1gSCjc4PhfS=> NUG1TXRIhjFyIN88US=> NFS1[3FIUTVyPUGwJI5O MXmxOVUxQTF4NB?=
MDA-MB-435 MkjiZ5l1d3SxeHnjbZR6KGG|c3H5 M2rHVZ4yOCEQvF2= NYL1SGJET0l3ME20NEBvVQ>? MlzpNVU2ODlzNkS=
MT-4 MX7jfZRwfG:6aXPpeJkh[XO|YYm= M2f5dGlEPTB;NDDuUS=> NV;qZ21pOTd{NUS2Olk>
CCRF-CEMc NEflNI5kgXSxdH;4bYNqfHliYYPzZZk> NFzOWFJKSzVyPUOgcm0> NI\jO24yPzJ3NE[2PS=>
WIL-2NSd MYrjfZRwfG:6aXPpeJkh[XO|YYm= MlvjTWM2OD13IH7N MmjrNVczPTR4Nkm=
CCRF-SB NIi1elhkgXSxdH;4bYNqfHliYYPzZZk> MVLJR|UxRTNibl2= MoHTNVczPTR4Nkm=
CRL 7065 M{\uXoN6fG:2b4jpZ4l1gSCjc4PhfS=> NX\VVnZLUUN3ME20NFAhdk1? M4K3NVE4OjV2Nk[5
SK-MEL-28b NYjVeplx[3m2b4TvfIlkcXS7IHHzd4F6 NHjOfJNKSzVyPUSwJI5O NGX2cYEyPzJ3NE[2PS=>
MCF-7 MnrTZ5l1d3SxeHnjbZR6KGG|c3H5 NGfBZlVKSzVyPUSwJI5O NVnxVJVkOTd{NUS2Olk>
SKMES-1 M{m4ToN6fG:2b4jpZ4l1gSCjc4PhfS=> NETMe3dKSzVyPUGwJI5O M4nP[FE4OjV2Nk[5
HepG2 M4L3coN6fG:2b4jpZ4l1gSCjc4PhfS=> M33rcGlEPTB;M{Cgcm0> NXSwWWw1OTd{NUS2Olk>
DU145 NGm1OolkgXSxdH;4bYNqfHliYYPzZZk> MWXJR|UxRTFyIH7N M3fiSlE4OjV2Nk[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
+ 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
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  • 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
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  • 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 30% PEG400+0.5% Tween80+5% propylene glycol 30 mg/mL

* 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

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 Active, not recruiting Glioblastoma Multiforme|GBM|Gliosarcoma Arno Therapeutics December 2009 Phase 2
NCT00956787 Recruiting 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