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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Cited by 11 Publications

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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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 NGnNRZRkgXSxdH;4bYNqfHliYYPzZZk> NUfueYFmUUN3ME21NUBvVQ>? MWC5NFA{PTJy
SKVLB NYHMbY1H[3m2b4TvfIlkcXS7IHHzd4F6 MnWyTWM2OD13MzDuUS=> NYrTc2RQQTByM{WyNC=>
HT29 M4\mU4N6fG:2b4jpZ4l1gSCjc4PhfS=> NYDzbY9SUUN3ME24O{45KG6P NGjIOXA6ODB|NUKw
KB MX3jfZRwfG:6aXPpeJkh[XO|YYm= MXrJR|UxRThibl2= Mn;WPVAxOzV{MB?=
A427 M3;t[2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFLJWWN,OSEQvF2= Mn7RSG1UVw>? MnTaTWM2OD1{NDDuUS=> M3HFUVk5PzZzMUG=
PC-3 NFLKeWhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVzQRoNMhjFizszN NIP5W5NFVVOR NGn4XGtKSzVyPUW3JI5O NWCzPZpiQTh5NkGxNS=>
K562adr M3H1RWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MoS1glEh|ryP NXnBNGtzTE2VTx?= MoHxTWM2OD13NzDuUS=> MVS5PFc3OTFz
MCF7mdr MVzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4jJc54yKM7:TR?= NVv3dolPTE2VTx?= MYXJR|UxRTNwMTDuUS=> NYPrOplWQTh5NkGxNS=>
P388 M3ntZWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MWnJR|UxRTN{IH7N NFL0fGoyODN2NkmzNy=>
P388CPT5 R NVTzZpJZT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4qxcGlEPTB;Mj64JO69VQ>? M2Wye|ExOzR4OUOz
KBwt MYTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2mxTWlEPTB;NECgcm0> M1XkUlExPDFzNEe2
KBMDR M4rFR2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NF\kV4FKSzVyPUewJI5O NWDwT45tOTB2MUG0O|Y>
KBV20C NFLsfllIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1jIPGlEPTB;M{Cgcm0> MmmzNVA1OTF2N{[=
KB7D NGqxd|JIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWDJR|UxRTN3IH7N MVmxNFQyOTR5Nh?=
KBCamp MWLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHHVVFNKSzVyPUGuNFQh|ryP NWHleIhJOTB2MUG0O|Y>
HT29 M{i3e4N6fG:2b4jpZ4l1gSCjc4PhfS=> NX24[FZuUUN3ME24NEBvVQ>? MWmxNFg1OThyOB?=
A549 M2CzdIN6fG:2b4jpZ4l1gSCjc4PhfS=> NWLMZ|MyUUN3ME22O{BvVQ>? MnPUNVA5PDF6MEi=
T24 NFLMNJZkgXSxdH;4bYNqfHliYYPzZZk> MofGTWM2OD16ODDuUS=> MUmxNFg1OThyOB?=
HOP-62 MYjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4HaOmlEPTB;MUCgcm0> MlniNVExOjB{OEO=
HCT-116 NX71SHE1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NEL6c4pKSzVyPUOwJI5O Ml3RNVExOjB{OEO=
SF-539 MVPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MoOwTWM2OD1zMDDuUS=> M{TxOFEyODJyMkiz
UACC-62 MoHoS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NGX2[mRKSzVyPUGwJI5O NF7yfpgyOTB{MEK4Ny=>
OVCAR-3 MkjmS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NITzcYJKSzVyPUKyNEBvVQ>? NGf0b3cyOTB{MEK4Ny=>
SN12C NILv[FJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVXJR|UxRTJyIH7N MWqxNVAzODJ6Mx?=
DU-145 NW\OV|RrT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmrSTWM2OD1zMDDuUS=> MV:xNVAzODJ6Mx?=
MDA-MB-435 NWHUe41lT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWfSV4NHUUN3ME20NEBvVQ>? NEnpXmsyOTB{MEK4Ny=>
WiDr MofCZ5l1d3SxeHnjbZR6KGG|c3H5 MlO1SG1UVw>? NEj6dIVKSzVyPUG3JI5O MnLKNVE{OzR3Nkm=
A549 NVHNOGJT[3m2b4TvfIlkcXS7IHHzd4F6 M2rBPGROW09? M17PW2lEPTB;MUSgcm0> NWf1dmZOOTF|M{S1Olk>
MKN45 NYLjZolP[3m2b4TvfIlkcXS7IHHzd4F6 MV7EUXNQ MWrJR|UxRTF5IH7N NYfpW5luOTF|M{S1Olk>
SK-OV-3 MkHkZ5l1d3SxeHnjbZR6KGG|c3H5 MlnXSG1UVw>? NGTFcYhKSzVyPUKwJI5O NFfiPVQyOTN|NEW2PS=>
H128 M2Th[YN6fG:2b4jpZ4l1gSCjc4PhfS=> MnmzSG1UVw>? NEX3dodKSzVyPUG4JI5O MoPmNVE{OzR3Nkm=
SK-BR-3 MV7jfZRwfG:6aXPpeJkh[XO|YYm= M4nyXWROW09? M3:1PWlEPTB;MkCgcm0> NVHiZXV7OTF|M{S1Olk>
LX-1 MVjjfZRwfG:6aXPpeJkh[XO|YYm= NULJfYVwTE2VTx?= NVPG[403UUN3ME2xNlAhdk1? NEHyWW8yOTh3OEezOy=>
HCT116 MVnjfZRwfG:6aXPpeJkh[XO|YYm= M2T1fGROW09? MX3JR|UxRTlibl2= M4fL[FEyQDV6N{O3
A2780 M4\jeYN6fG:2b4jpZ4l1gSCjc4PhfS=> M3LKSmROW09? M1SxRmlEPTB;NDDuUS=> NWG4XXY2OTF6NUi3N|c>
IMR-32 NVnYNnlT[3m2b4TvfIlkcXS7IHHzd4F6 M3H4ep4yOCEQvF2= M1LFNmROW09? M2\PbmlEPTB;Mj6yNUBvVQ>? NYHjOGF5OTJ4MUe4PVQ>
P388 M4jhR4N6fG:2b4jpZ4l1gSCjc4PhfS=> NUewbJZSUUN3ME2xN{BvVQ>? M{Xzb|EzPjJyMEix
Lewis NYH5NpVP[3m2b4TvfIlkcXS7IHHzd4F6 NI\qendKSzVyPUOzJI5O MUWxNlYzODB6MR?=
JLC MYDjfZRwfG:6aXPpeJkh[XO|YYm= MoHETWM2OD13Lk[gcm0> NWTqeW1jOTJ4MkCwPFE>
HT-29 MknwZ5l1d3SxeHnjbZR6KGG|c3H5 MWnJR|UxRTFwNDFOwG0> NXjwSoJSOTJ4M{m1OFE>
Caki-2 NWTsUppm[3m2b4TvfIlkcXS7IHHzd4F6 NX7tUHFkUUN3ME2zMlk3KM7:TR?= NGPGfIkyOjZ|OUW0NS=>
A549 MX;jfZRwfG:6aXPpeJkh[XO|YYm= NX\4TopWUUN3ME2yMlU{KM7:TR?= MoPlNVI3Ozl3NEG=
HEC-1-B MnnzZ5l1d3SxeHnjbZR6KGG|c3H5 MmPwTWM2OD16Lk[0JO69VQ>? NUXxO2VKOTJ4M{m1OFE>
HL-60 M3rmcoN6fG:2b4jpZ4l1gSCjc4PhfS=> NGHsOYVKSzVyPU[2JI5O NXWycGR2OTJ4M{m1OFE>
Col2 M2fBfoN6fG:2b4jpZ4l1gSCjc4PhfS=> MWH+NUDPxE1? NUfUWFlCTUR3ME21O{BvVQ>? MmjCNVUxPDN2MEe=
HUVEC NETqTVJkgXSxdH;4bYNqfHliYYPzZZk> MlzoglEh|ryP NVu1N5ZkTUR3ME2yOVghdk1? NXfEXJZ2OTVyNEO0NFc>
KB NF;OdnVkgXSxdH;4bYNqfHliYYPzZZk> MXn+NUDPxE1? NXHhc5FlTUR3ME2yNkBvVQ>? M1fpRlE2ODR|NEC3
LCNaP MoHtZ5l1d3SxeHnjbZR6KGG|c3H5 M1fTVZ4yKM7:TR?= NEPiXo1GTDVyPUK4JI5O MV[xOVA1OzRyNx?=
Lu1 NYH4PYp2[3m2b4TvfIlkcXS7IHHzd4F6 MlHPglEh|ryP NHzNPYtGTDVyPUK5JI5O NYPqOpN{OTVyNEO0NFc>
RPMI8402 M3HiUoN6fG:2b4jpZ4l1gSCjc4PhfS=> MUT+NVAh|ryP NHi5RWxKSzVyPU[gcm0> Ml3uNVU1QDJ7Mkm=
CPT-K5 NUi2dGtj[3m2b4TvfIlkcXS7IHHzd4F6 NXfYXXNChjFyIN88US=> NIrRcm1KSzVyPkGwJO69VQ>? M{n3TVE2PDh{OUK5
P388 MX;jfZRwfG:6aXPpeJkh[XO|YYm= MmrHglExKM7:TR?= MVrJR|UxRTF2IH7N NXvub|NyOTV2OEK5Nlk>
P388/CPT45 NGnpVZZkgXSxdH;4bYNqfHliYYPzZZk> MWX+NVAh|ryP MXLJR|UxRjFyIN88US=> M2nmZ|E2PDh{OUK5
KB3-1 NXm3eWtF[3m2b4TvfIlkcXS7IHHzd4F6 M{DaeZ4yOCEQvF2= Mn7hTWM2OD12MDDuUS=> MneyNVU1QDJ7Mkm=
KBV-1 + MDR1 NEf3O4hkgXSxdH;4bYNqfHliYYPzZZk> NInaWFJ,OTBizszN NUP2UppKUUN3ME20OFAhdk1? MYWxOVQ5Ojl{OR?=
KBH MkDjZ5l1d3SxeHnjbZR6KGG|c3H5 M4fxSp4yOCEQvF2= NGTXZWRKSzVyPUS0NEBvVQ>? MljDNVU1QDJ7Mkm=
HOP-62 MXzjfZRwfG:6aXPpeJkh[XO|YYm= MWH+NVAh|ryP M2rVU2dKPTB;MUCgcm0> MV6xOVUxQTF4NB?=
HCT-116 NV;rd3k3[3m2b4TvfIlkcXS7IHHzd4F6 MYf+NVAh|ryP Mn:wS2k2OD1|MDDuUS=> Ml\yNVU2ODlzNkS=
F-539 MVPjfZRwfG:6aXPpeJkh[XO|YYm= M3fPOZ4yOCEQvF2= Mlu3S2k2OD1zMDDuUS=> NIL1V4wyPTVyOUG2OC=>
UACC-62 M1TzfYN6fG:2b4jpZ4l1gSCjc4PhfS=> M{L3dJ4yOCEQvF2= NFfpW3RIUTVyPUGwJI5O M1ztSVE2PTB7MU[0
OVCAR-3 M2HnNoN6fG:2b4jpZ4l1gSCjc4PhfS=> MnjOglExKM7:TR?= MXPHTVUxRTJ{MDDuUS=> M1e1clE2PTB7MU[0
SN12C M330VYN6fG:2b4jpZ4l1gSCjc4PhfS=> NH7acY9,OTBizszN NYPKT4V4T0l3ME2yNEBvVQ>? MoLWNVU2ODlzNkS=
DU-145 MlPZZ5l1d3SxeHnjbZR6KGG|c3H5 NFX5bIV,OTBizszN Mn\5S2k2OD1zMDDuUS=> NFzj[HUyPTVyOUG2OC=>
MDA-MB-435 MnfQZ5l1d3SxeHnjbZR6KGG|c3H5 M4rmcp4yOCEQvF2= M3;HZmdKPTB;NECgcm0> NXjodm54OTV3MEmxOlQ>
MT-4 M3jHOYN6fG:2b4jpZ4l1gSCjc4PhfS=> NF[1eY1KSzVyPUSgcm0> MnrJNVczPTR4Nkm=
CCRF-CEMc MVHjfZRwfG:6aXPpeJkh[XO|YYm= MojqTWM2OD1|IH7N MVWxO|I2PDZ4OR?=
WIL-2NSd MnnzZ5l1d3SxeHnjbZR6KGG|c3H5 NUTlbWZqUUN3ME21JI5O M2nyWFE4OjV2Nk[5
CCRF-SB Mo\OZ5l1d3SxeHnjbZR6KGG|c3H5 MX7JR|UxRTNibl2= M3KwPVE4OjV2Nk[5
CRL 7065 MmfRZ5l1d3SxeHnjbZR6KGG|c3H5 M2HxcGlEPTB;NECwJI5O MmjKNVczPTR4Nkm=
SK-MEL-28b M17ieIN6fG:2b4jpZ4l1gSCjc4PhfS=> M3HGVWlEPTB;NECgcm0> MnjjNVczPTR4Nkm=
MCF-7 M1jDOoN6fG:2b4jpZ4l1gSCjc4PhfS=> NFnZNVZKSzVyPUSwJI5O Mkj1NVczPTR4Nkm=
SKMES-1 NITsV2FkgXSxdH;4bYNqfHliYYPzZZk> MUjJR|UxRTFyIH7N M{nKSFE4OjV2Nk[5
HepG2 NGrtW3hkgXSxdH;4bYNqfHliYYPzZZk> Mmm3TWM2OD1|MDDuUS=> Mo\nNVczPTR4Nkm=
DU145 NHLFTJBkgXSxdH;4bYNqfHliYYPzZZk> M2fJe2lEPTB;MUCgcm0> NGjLbnIyPzJ3NE[2PS=>

... 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
NCT02755311 Unknown status Hepatocellular Carcinoma Sun Yat-sen University March 2014 Phase 3
NCT02755311 Unknown status Hepatocellular Carcinoma Sun Yat-sen University March 2014 Phase 3
NCT01803269 Terminated Extensive Stage Small Cell Lung Cancer|Recurrent Small Cell Lung Cancer University of Chicago|National Cancer Institute (NCI) January 16 2013 Phase 2
NCT01803269 Terminated Extensive Stage Small Cell Lung Cancer|Recurrent Small Cell Lung Cancer University of Chicago|National Cancer Institute (NCI) January 16 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 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 Phase 2

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