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.

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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 M2Tzc4N6fG:2b4jpZ4l1gSCjc4PhfS=> MUDJR|UxRTVzIH7N Ml32PVAxOzV{MB?=
SKVLB NEP0WmlkgXSxdH;4bYNqfHliYYPzZZk> MWHJR|UxRTV|IH7N NHjUXFE6ODB|NUKw
HT29 M4DCZYN6fG:2b4jpZ4l1gSCjc4PhfS=> MYrJR|UxRTh5Lkigcm0> NHzlPHg6ODB|NUKw
KB NW\B[ZpJ[3m2b4TvfIlkcXS7IHHzd4F6 MlnuTWM2OD16IH7N Mn\kPVAxOzV{MB?=
A427 MnniS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWD+NUDPxE1? M2naSGROW09? NGDNbWFKSzVyPUK0JI5O M4\ibVk5PzZzMUG=
PC-3 NHTqdIRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXr+NUDPxE1? MkTmSG1UVw>? M1qwUWlEPTB;NUegcm0> MV:5PFc3OTFz
K562adr NXPiU5ZqT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NV7rd40{hjFizszN NH22fpFFVVOR MmHCTWM2OD13NzDuUS=> MmHUPVg4PjFzMR?=
MCF7mdr NE\HfIVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MV7+NUDPxE1? MnzXSG1UVw>? NG\hNo9KSzVyPUOuNUBvVQ>? M4OzbFk5PzZzMUG=
P388 MkS0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NEjNPJRKSzVyPUOyJI5O NYqwfJNHOTB|NE[5N|M>
P388CPT5 R M4iw[Gdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Ml\KTWM2OD1{Lkig{txO M{HSd|ExOzR4OUOz
KBwt M3rRSWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MkTTTWM2OD12MDDuUS=> MnLMNVA1OTF2N{[=
KBMDR Mle3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NIfocJRKSzVyPUewJI5O NVvDTGxrOTB2MUG0O|Y>
KBV20C NVPNfWdlT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mlv4TWM2OD1|MDDuUS=> M3fVbVExPDFzNEe2
KB7D MmG2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4j3RmlEPTB;M{Wgcm0> NV7qW4xkOTB2MUG0O|Y>
KBCamp MVvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NF33eldKSzVyPUGuNFQh|ryP MVGxNFQyOTR5Nh?=
HT29 NV:5OYlD[3m2b4TvfIlkcXS7IHHzd4F6 MljmTWM2OD16MDDuUS=> MVOxNFg1OThyOB?=
A549 NIDVb49kgXSxdH;4bYNqfHliYYPzZZk> MnjKTWM2OD14NzDuUS=> M2rkUVExQDRzOEC4
T24 NIixUVBkgXSxdH;4bYNqfHliYYPzZZk> MX3JR|UxRTh6IH7N MUSxNFg1OThyOB?=
HOP-62 MXjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MUjJR|UxRTFyIH7N NF3HfpEyOTB{MEK4Ny=>
HCT-116 MV7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M{DWcGlEPTB;M{Cgcm0> MWGxNVAzODJ6Mx?=
SF-539 NY\5bYdDT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4juNGlEPTB;MUCgcm0> M3L6UFEyODJyMkiz
UACC-62 MX\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVTJR|UxRTFyIH7N M17aNVEyODJyMkiz
OVCAR-3 M333Tmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NE\CN3ZKSzVyPUKyNEBvVQ>? M{fve|EyODJyMkiz
SN12C NFrhfZBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MX\JR|UxRTJyIH7N MXixNVAzODJ6Mx?=
DU-145 NVnqWZNZT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUnJR|UxRTFyIH7N NFzXengyOTB{MEK4Ny=>
MDA-MB-435 NUPZTZkzT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NHfTXpFKSzVyPUSwJI5O MY[xNVAzODJ6Mx?=
WiDr NFPuc5NkgXSxdH;4bYNqfHliYYPzZZk> NWTFU2o{TE2VTx?= M324NGlEPTB;MUegcm0> MoTKNVE{OzR3Nkm=
A549 M4TYVIN6fG:2b4jpZ4l1gSCjc4PhfS=> MnLhSG1UVw>? NX3SfIt[UUN3ME2xOEBvVQ>? NXyxe5pbOTF|M{S1Olk>
MKN45 NVLLRW9R[3m2b4TvfIlkcXS7IHHzd4F6 M363[2ROW09? NVHqSm0yUUN3ME2xO{BvVQ>? MWOxNVM{PDV4OR?=
SK-OV-3 MW\jfZRwfG:6aXPpeJkh[XO|YYm= MmXISG1UVw>? NGW3NJRKSzVyPUKwJI5O M3HpN|EyOzN2NU[5
H128 NHLkPGtkgXSxdH;4bYNqfHliYYPzZZk> MV3EUXNQ MXPJR|UxRTF6IH7N M2XMbVEyOzN2NU[5
SK-BR-3 MYjjfZRwfG:6aXPpeJkh[XO|YYm= MnTZSG1UVw>? M2Tu[2lEPTB;MkCgcm0> MXqxNVM{PDV4OR?=
LX-1 MY\jfZRwfG:6aXPpeJkh[XO|YYm= NHuzOHVFVVOR MnTuTWM2OD1zMkCgcm0> M4KzRVEyQDV6N{O3
HCT116 MlrrZ5l1d3SxeHnjbZR6KGG|c3H5 M2\BdWROW09? NUTpVYNyUUN3ME25JI5O NHSyNIsyOTh3OEezOy=>
A2780 MXHjfZRwfG:6aXPpeJkh[XO|YYm= MVvEUXNQ NY\SV3VTUUN3ME20JI5O MXSxNVg2QDd|Nx?=
IMR-32 Mnf1Z5l1d3SxeHnjbZR6KGG|c3H5 M1izVp4yOCEQvF2= NWK3NlRlTE2VTx?= MUjJR|UxRTJwMkGgcm0> MUCxNlYyPzh7NB?=
P388 M4\PVoN6fG:2b4jpZ4l1gSCjc4PhfS=> MlnoTWM2OD1zMzDuUS=> NETGOHEyOjZ{MEC4NS=>
Lewis MnPiZ5l1d3SxeHnjbZR6KGG|c3H5 MVnJR|UxRTN|IH7N M{C5[VEzPjJyMEix
JLC NWfi[4FI[3m2b4TvfIlkcXS7IHHzd4F6 M1HBOGlEPTB;NT62JI5O MUmxNlYzODB6MR?=
HT-29 Mn30Z5l1d3SxeHnjbZR6KGG|c3H5 NHfndJZKSzVyPUGuOEDPxE1? Ml3aNVI3Ozl3NEG=
Caki-2 MmLuZ5l1d3SxeHnjbZR6KGG|c3H5 NUTVXo5TUUN3ME2zMlk3KM7:TR?= NULaN3p[OTJ4M{m1OFE>
A549 MnnnZ5l1d3SxeHnjbZR6KGG|c3H5 MUDJR|UxRTJwNUOg{txO NFXWOnAyOjZ|OUW0NS=>
HEC-1-B MmqwZ5l1d3SxeHnjbZR6KGG|c3H5 NEXlfldKSzVyPUiuOlQh|ryP MXGxNlY{QTV2MR?=
HL-60 Mmq2Z5l1d3SxeHnjbZR6KGG|c3H5 M2rIVWlEPTB;Nk[gcm0> MnPFNVI3Ozl3NEG=
Col2 NIDucW5kgXSxdH;4bYNqfHliYYPzZZk> M{\MVJ4yKM7:TR?= NIm1SGxGTDVyPUW3JI5O Moj3NVUxPDN2MEe=
HUVEC Mm\tZ5l1d3SxeHnjbZR6KGG|c3H5 NF[4NFJ,OSEQvF2= NVLOcpRXTUR3ME2yOVghdk1? NX\tUo5pOTVyNEO0NFc>
KB NF22SGxkgXSxdH;4bYNqfHliYYPzZZk> MUP+NUDPxE1? MYrFSFUxRTJ{IH7N NVjRepZjOTVyNEO0NFc>
LCNaP NHvnd2FkgXSxdH;4bYNqfHliYYPzZZk> NXSzb2lJhjFizszN Ml2wSWQ2OD1{ODDuUS=> NWm4dFVuOTVyNEO0NFc>
Lu1 M{nBT4N6fG:2b4jpZ4l1gSCjc4PhfS=> M{nNU54yKM7:TR?= NHH1PZNGTDVyPUK5JI5O MWWxOVA1OzRyNx?=
RPMI8402 MUHjfZRwfG:6aXPpeJkh[XO|YYm= MkfhglExKM7:TR?= NHLzZ5dKSzVyPU[gcm0> NGi2dnAyPTR6MkmyPS=>
CPT-K5 MWDjfZRwfG:6aXPpeJkh[XO|YYm= MVH+NVAh|ryP NYnlUYhPUUN3ME6xNEDPxE1? NEDJUXMyPTR6MkmyPS=>
P388 MYfjfZRwfG:6aXPpeJkh[XO|YYm= MV3+NVAh|ryP Mo\uTWM2OD1zNDDuUS=> NYTVUFN3OTV2OEK5Nlk>
P388/CPT45 NYHseIZO[3m2b4TvfIlkcXS7IHHzd4F6 MXn+NVAh|ryP M33qPWlEPTB-MUCg{txO MX6xOVQ5Ojl{OR?=
KB3-1 MX;jfZRwfG:6aXPpeJkh[XO|YYm= MWP+NVAh|ryP M2fXUWlEPTB;NECgcm0> NFTOXYcyPTR6MkmyPS=>
KBV-1 + MDR1 NIfwNG9kgXSxdH;4bYNqfHliYYPzZZk> M2D3fZ4yOCEQvF2= M4DnT2lEPTB;NESwJI5O MYexOVQ5Ojl{OR?=
KBH Mn3IZ5l1d3SxeHnjbZR6KGG|c3H5 NHK2[nN,OTBizszN NEPaUoVKSzVyPUS0NEBvVQ>? NHnqW3AyPTR6MkmyPS=>
HOP-62 MnTJZ5l1d3SxeHnjbZR6KGG|c3H5 MXf+NVAh|ryP NWDsWVQxT0l3ME2xNEBvVQ>? MoXYNVU2ODlzNkS=
HCT-116 M{n6WoN6fG:2b4jpZ4l1gSCjc4PhfS=> Ml\KglExKM7:TR?= MoXlS2k2OD1|MDDuUS=> MXSxOVUxQTF4NB?=
F-539 NVHrTYRS[3m2b4TvfIlkcXS7IHHzd4F6 NETKe|N,OTBizszN MWPHTVUxRTFyIH7N M1TDT|E2PTB7MU[0
UACC-62 M{\mfIN6fG:2b4jpZ4l1gSCjc4PhfS=> MYj+NVAh|ryP NUXPdW5nT0l3ME2xNEBvVQ>? NV\JV5l7OTV3MEmxOlQ>
OVCAR-3 MXfjfZRwfG:6aXPpeJkh[XO|YYm= NGPDT2F,OTBizszN M2PEVmdKPTB;MkKwJI5O MnPDNVU2ODlzNkS=
SN12C MmTsZ5l1d3SxeHnjbZR6KGG|c3H5 MkjtglExKM7:TR?= MVvHTVUxRTJyIH7N M{TQcVE2PTB7MU[0
DU-145 NUjRfZBV[3m2b4TvfIlkcXS7IHHzd4F6 NVf5NWQzhjFyIN88US=> MWnHTVUxRTFyIH7N NWr3SXR[OTV3MEmxOlQ>
MDA-MB-435 NWf3W2ZQ[3m2b4TvfIlkcXS7IHHzd4F6 Mki4glExKM7:TR?= M2nJVWdKPTB;NECgcm0> M1\nb|E2PTB7MU[0
MT-4 NXHNcGxU[3m2b4TvfIlkcXS7IHHzd4F6 MWTJR|UxRTRibl2= MVOxO|I2PDZ4OR?=
CCRF-CEMc M3O3XYN6fG:2b4jpZ4l1gSCjc4PhfS=> NETiSJZKSzVyPUOgcm0> NF7hfpkyPzJ3NE[2PS=>
WIL-2NSd M3OxSYN6fG:2b4jpZ4l1gSCjc4PhfS=> NEXOUJBKSzVyPUWgcm0> MUCxO|I2PDZ4OR?=
CCRF-SB M3LVcoN6fG:2b4jpZ4l1gSCjc4PhfS=> NXL2TmZbUUN3ME2zJI5O Mn3tNVczPTR4Nkm=
CRL 7065 MmXzZ5l1d3SxeHnjbZR6KGG|c3H5 M1j2bGlEPTB;NECwJI5O M37wXlE4OjV2Nk[5
SK-MEL-28b MUXjfZRwfG:6aXPpeJkh[XO|YYm= M1\NcGlEPTB;NECgcm0> NHuyfo0yPzJ3NE[2PS=>
MCF-7 NWDHNWRb[3m2b4TvfIlkcXS7IHHzd4F6 NYWwUmxCUUN3ME20NEBvVQ>? M{fRfFE4OjV2Nk[5
SKMES-1 NFnqNVhkgXSxdH;4bYNqfHliYYPzZZk> MXzJR|UxRTFyIH7N MYqxO|I2PDZ4OR?=
HepG2 M33zWIN6fG:2b4jpZ4l1gSCjc4PhfS=> M3naTmlEPTB;M{Cgcm0> NGm3eW0yPzJ3NE[2PS=>
DU145 M4rxNoN6fG:2b4jpZ4l1gSCjc4PhfS=> M4radGlEPTB;MUCgcm0> M4LEUlE4OjV2Nk[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 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
in solvent
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