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.

  • 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 NIjZV5ZkgXSxdH;4bYNqfHliYYPzZZk> NYXrcpJuUUN3ME21NUBvVQ>? MmrSPVAxOzV{MB?=
SKVLB NH\jNGdkgXSxdH;4bYNqfHliYYPzZZk> M4rVWGlEPTB;NUOgcm0> NF;aNJg6ODB|NUKw
HT29 NIXpbItkgXSxdH;4bYNqfHliYYPzZZk> NEDPTVhKSzVyPUi3Mlghdk1? NXzIbHVvQTByM{WyNC=>
KB MUXjfZRwfG:6aXPpeJkh[XO|YYm= MkHRTWM2OD16IH7N MVK5NFA{PTJy
A427 MWnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHPYT3R,OSEQvF2= MmrCSG1UVw>? MmfGTWM2OD1{NDDuUS=> MWm5PFc3OTFz
PC-3 NFPSfnVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mke4glEh|ryP NVTpSVM5TE2VTx?= NGTBZ5NKSzVyPUW3JI5O Ml;DPVg4PjFzMR?=
K562adr MY\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MmjsglEh|ryP MUTEUXNQ NUfRbI1EUUN3ME21O{BvVQ>? MUG5PFc3OTFz
MCF7mdr M4TiVWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MlXyglEh|ryP M{PmSWROW09? NF7FW49KSzVyPUOuNUBvVQ>? Mk\UPVg4PjFzMR?=
P388 MnzkS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYLJR|UxRTN{IH7N M1LzVlExOzR4OUOz
P388CPT5 R NIfiZoZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Ml36TWM2OD1{Lkig{txO Mn3MNVA{PDZ7M{O=
KBwt MmDxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MmLZTWM2OD12MDDuUS=> M{O3cFExPDFzNEe2
KBMDR NV;hUGVMT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MljXTWM2OD15MDDuUS=> NHT1NoQyODRzMUS3Oi=>
KBV20C NVmy[Gl{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NX\ib2Y{UUN3ME2zNEBvVQ>? MWOxNFQyOTR5Nh?=
KB7D NGLqVYpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHSxbnFKSzVyPUO1JI5O M4[4WFExPDFzNEe2
KBCamp NW\vbnlbT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmC1TWM2OD1zLkC0JO69VQ>? NGO0e5cyODRzMUS3Oi=>
HT29 M{fsbIN6fG:2b4jpZ4l1gSCjc4PhfS=> NWDXcmlxUUN3ME24NEBvVQ>? NFHUOmIyODh2MUiwPC=>
A549 NGjMdXBkgXSxdH;4bYNqfHliYYPzZZk> Mnm4TWM2OD14NzDuUS=> MX6xNFg1OThyOB?=
T24 M4Hx[IN6fG:2b4jpZ4l1gSCjc4PhfS=> NXvjZllxUUN3ME24PEBvVQ>? M4HNUVExQDRzOEC4
HOP-62 NInxOopIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MV;JR|UxRTFyIH7N M{HT[VEyODJyMkiz
HCT-116 NWmxNYtTT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NH:xO5dKSzVyPUOwJI5O M164ZlEyODJyMkiz
SF-539 NWTsbI9MT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NUCw[VhDUUN3ME2xNEBvVQ>? M2XnWFEyODJyMkiz
UACC-62 NV\1RVY5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NX7pWXFvUUN3ME2xNEBvVQ>? MVexNVAzODJ6Mx?=
OVCAR-3 MWfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MlzyTWM2OD1{MkCgcm0> M2rz[FEyODJyMkiz
SN12C MWjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MYrJR|UxRTJyIH7N NWKzZmZbOTFyMkCyPFM>
DU-145 NV\xZmZ4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MX7JR|UxRTFyIH7N NXfyPZIzOTFyMkCyPFM>
MDA-MB-435 NYHGWWJzT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWrJR|UxRTRyIH7N NHHwdlUyOTB{MEK4Ny=>
WiDr MXHjfZRwfG:6aXPpeJkh[XO|YYm= MknBSG1UVw>? MV\JR|UxRTF5IH7N NGfZSVIyOTN|NEW2PS=>
A549 MXnjfZRwfG:6aXPpeJkh[XO|YYm= NEDEZ2pFVVOR NXTTbGtTUUN3ME2xOEBvVQ>? M2fLWFEyOzN2NU[5
MKN45 M{TkWIN6fG:2b4jpZ4l1gSCjc4PhfS=> M4K2T2ROW09? NVPLWoNYUUN3ME2xO{BvVQ>? M3XIT|EyOzN2NU[5
SK-OV-3 NIrRZXZkgXSxdH;4bYNqfHliYYPzZZk> NVflV4R5TE2VTx?= NE\qcWRKSzVyPUKwJI5O MWexNVM{PDV4OR?=
H128 M3;qNIN6fG:2b4jpZ4l1gSCjc4PhfS=> NHPaSo1FVVOR NGmyemVKSzVyPUG4JI5O MoTrNVE{OzR3Nkm=
SK-BR-3 MXvjfZRwfG:6aXPpeJkh[XO|YYm= M4fKVGROW09? M3PwU2lEPTB;MkCgcm0> M3LqNVEyOzN2NU[5
LX-1 NEnYfmlkgXSxdH;4bYNqfHliYYPzZZk> Ml;0SG1UVw>? NHrT[W5KSzVyPUGyNEBvVQ>? NGrQOZMyOTh3OEezOy=>
HCT116 NVfq[mlM[3m2b4TvfIlkcXS7IHHzd4F6 NGPsUWxFVVOR MlO4TWM2OD17IH7N M3zXblEyQDV6N{O3
A2780 MW\jfZRwfG:6aXPpeJkh[XO|YYm= NETtdWVFVVOR MojyTWM2OD12IH7N NI\qR|AyOTh3OEezOy=>
IMR-32 NUfYbVlq[3m2b4TvfIlkcXS7IHHzd4F6 M2TQTp4yOCEQvF2= MXHEUXNQ MUfJR|UxRTJwMkGgcm0> M13FVVEzPjF5OEm0
P388 M4PZSoN6fG:2b4jpZ4l1gSCjc4PhfS=> NHXvUFlKSzVyPUGzJI5O MoD5NVI3OjByOEG=
Lewis NWTOU5N2[3m2b4TvfIlkcXS7IHHzd4F6 M37Xd2lEPTB;M{Ogcm0> MXGxNlYzODB6MR?=
JLC MnyyZ5l1d3SxeHnjbZR6KGG|c3H5 M2jxN2lEPTB;NT62JI5O M{DYflEzPjJyMEix
HT-29 MV7jfZRwfG:6aXPpeJkh[XO|YYm= MVrJR|UxRTFwNDFOwG0> NV;VUpliOTJ4M{m1OFE>
Caki-2 Mnj2Z5l1d3SxeHnjbZR6KGG|c3H5 NFTMU2FKSzVyPUOuPVYh|ryP NHnHb3MyOjZ|OUW0NS=>
A549 NEf5RnpkgXSxdH;4bYNqfHliYYPzZZk> NEPXWY1KSzVyPUKuOVMh|ryP MXuxNlY{QTV2MR?=
HEC-1-B NGrZVWZkgXSxdH;4bYNqfHliYYPzZZk> MXXJR|UxRThwNkSg{txO MYCxNlY{QTV2MR?=
HL-60 NVX4UI8y[3m2b4TvfIlkcXS7IHHzd4F6 M17sUmlEPTB;Nk[gcm0> MlXoNVI3Ozl3NEG=
Col2 NFewcVhkgXSxdH;4bYNqfHliYYPzZZk> NHL2coV,OSEQvF2= NWrTNo1ZTUR3ME21O{BvVQ>? MVixOVA1OzRyNx?=
HUVEC MVjjfZRwfG:6aXPpeJkh[XO|YYm= MYX+NUDPxE1? M2T1WGVFPTB;MkW4JI5O MV:xOVA1OzRyNx?=
KB NUK4bI4y[3m2b4TvfIlkcXS7IHHzd4F6 MlO4glEh|ryP NXLkbIxUTUR3ME2yNkBvVQ>? MkmyNVUxPDN2MEe=
LCNaP NW\JdWJP[3m2b4TvfIlkcXS7IHHzd4F6 Mo\6glEh|ryP MnzSSWQ2OD1{ODDuUS=> MVSxOVA1OzRyNx?=
Lu1 NFHS[IVkgXSxdH;4bYNqfHliYYPzZZk> MXn+NUDPxE1? NXPrN5hTTUR3ME2yPUBvVQ>? M1O2PFE2ODR|NEC3
RPMI8402 M1r5RoN6fG:2b4jpZ4l1gSCjc4PhfS=> MlfnglExKM7:TR?= Mnq3TWM2OD14IH7N NUn0cZVoOTV2OEK5Nlk>
CPT-K5 M3LQS4N6fG:2b4jpZ4l1gSCjc4PhfS=> MVz+NVAh|ryP M{KzW2lEPTB-MUCg{txO NXuycHg4OTV2OEK5Nlk>
P388 NHThcpdkgXSxdH;4bYNqfHliYYPzZZk> M2j6dp4yOCEQvF2= MkW4TWM2OD1zNDDuUS=> MoLMNVU1QDJ7Mkm=
P388/CPT45 M3;KZoN6fG:2b4jpZ4l1gSCjc4PhfS=> NX;Nb|B7hjFyIN88US=> NFu5OFFKSzVyPkGwJO69VQ>? M1jL[FE2PDh{OUK5
KB3-1 NVr6d2JC[3m2b4TvfIlkcXS7IHHzd4F6 MXT+NVAh|ryP M4r2XmlEPTB;NECgcm0> NXuyN|V7OTV2OEK5Nlk>
KBV-1 + MDR1 MXjjfZRwfG:6aXPpeJkh[XO|YYm= NV[wd3M2hjFyIN88US=> NGrC[mhKSzVyPUS0NEBvVQ>? MnS5NVU1QDJ7Mkm=
KBH MUTjfZRwfG:6aXPpeJkh[XO|YYm= Mk\iglExKM7:TR?= NGX5cplKSzVyPUS0NEBvVQ>? MX[xOVQ5Ojl{OR?=
HOP-62 MkHXZ5l1d3SxeHnjbZR6KGG|c3H5 MU\+NVAh|ryP NHLUSYtIUTVyPUGwJI5O NHvoSWIyPTVyOUG2OC=>
HCT-116 NIOyVZhkgXSxdH;4bYNqfHliYYPzZZk> NFPqb3F,OTBizszN MnLBS2k2OD1|MDDuUS=> MlTYNVU2ODlzNkS=
F-539 NWjxNmJW[3m2b4TvfIlkcXS7IHHzd4F6 NUHoRlRxhjFyIN88US=> NHPWbIlIUTVyPUGwJI5O MkPVNVU2ODlzNkS=
UACC-62 NUS0OVZX[3m2b4TvfIlkcXS7IHHzd4F6 NIXUdox,OTBizszN M3zIfWdKPTB;MUCgcm0> MlvjNVU2ODlzNkS=
OVCAR-3 MVLjfZRwfG:6aXPpeJkh[XO|YYm= M1q0N54yOCEQvF2= MnW5S2k2OD1{MkCgcm0> Ml;mNVU2ODlzNkS=
SN12C MWnjfZRwfG:6aXPpeJkh[XO|YYm= M4j4bJ4yOCEQvF2= MXPHTVUxRTJyIH7N NIHDe5oyPTVyOUG2OC=>
DU-145 MXjjfZRwfG:6aXPpeJkh[XO|YYm= MVv+NVAh|ryP NIX0NndIUTVyPUGwJI5O MW[xOVUxQTF4NB?=
MDA-MB-435 M2\COYN6fG:2b4jpZ4l1gSCjc4PhfS=> M4\a[54yOCEQvF2= MojmS2k2OD12MDDuUS=> M2HGTVE2PTB7MU[0
MT-4 Ml;JZ5l1d3SxeHnjbZR6KGG|c3H5 MX7JR|UxRTRibl2= NGDrSnYyPzJ3NE[2PS=>
CCRF-CEMc NX7VXHR6[3m2b4TvfIlkcXS7IHHzd4F6 NY\5bGFmUUN3ME2zJI5O NUnyWoJQOTd{NUS2Olk>
WIL-2NSd MoPVZ5l1d3SxeHnjbZR6KGG|c3H5 MUDJR|UxRTVibl2= MYmxO|I2PDZ4OR?=
CCRF-SB MkXkZ5l1d3SxeHnjbZR6KGG|c3H5 MYnJR|UxRTNibl2= MlS5NVczPTR4Nkm=
CRL 7065 MmT6Z5l1d3SxeHnjbZR6KGG|c3H5 NHvtRXlKSzVyPUSwNEBvVQ>? M3TrSVE4OjV2Nk[5
SK-MEL-28b MUTjfZRwfG:6aXPpeJkh[XO|YYm= NWL4[|A5UUN3ME20NEBvVQ>? MWKxO|I2PDZ4OR?=
MCF-7 NXrOTWsx[3m2b4TvfIlkcXS7IHHzd4F6 NVzuOJpWUUN3ME20NEBvVQ>? NH31[WQyPzJ3NE[2PS=>
SKMES-1 NVL6SlFK[3m2b4TvfIlkcXS7IHHzd4F6 NF71RmhKSzVyPUGwJI5O MmP1NVczPTR4Nkm=
HepG2 NVfGUoJJ[3m2b4TvfIlkcXS7IHHzd4F6 NUWxWWk2UUN3ME2zNEBvVQ>? M2fvbFE4OjV2Nk[5
DU145 MUnjfZRwfG:6aXPpeJkh[XO|YYm= MUHJR|UxRTFyIH7N NGnTVIwyPzJ3NE[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
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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID