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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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 M2LafoN6fG:2b4jpZ4l1gSCjc4PhfS=> NXHwd3U3UUN3ME21NUBvVQ>? NYn2WVZpQTByM{WyNC=>
SKVLB NW\TcW1R[3m2b4TvfIlkcXS7IHHzd4F6 M4nPNmlEPTB;NUOgcm0> MUi5NFA{PTJy
HT29 NVjLWY1v[3m2b4TvfIlkcXS7IHHzd4F6 M{nRTmlEPTB;OEeuPEBvVQ>? NWL3V491QTByM{WyNC=>
KB M{PGPYN6fG:2b4jpZ4l1gSCjc4PhfS=> NEXqTWRKSzVyPUigcm0> MmfpPVAxOzV{MB?=
A427 MWDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVjhUVV{hjFizszN MWfEUXNQ M1LQcmlEPTB;MkSgcm0> MWm5PFc3OTFz
PC-3 MWrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXz+NUDPxE1? M3H5XmROW09? M4PTRWlEPTB;NUegcm0> MXi5PFc3OTFz
K562adr M4TvRmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MUD+NUDPxE1? NFvLWFNFVVOR NGD2fmRKSzVyPUW3JI5O MorMPVg4PjFzMR?=
MCF7mdr MmfnS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MljKglEh|ryP MV\EUXNQ NXLFUZl5UUN3ME2zMlEhdk1? NIjCVo86QDd4MUGx
P388 MUDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NV7yVVFqUUN3ME2zNkBvVQ>? MknsNVA{PDZ7M{O=
P388CPT5 R M3T2b2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1rQfmlEPTB;Mj64JO69VQ>? M2G3fFExOzR4OUOz
KBwt Ml;mS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mk\CTWM2OD12MDDuUS=> MWWxNFQyOTR5Nh?=
KBMDR NX73PXlPT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MlfDTWM2OD15MDDuUS=> M3LxNlExPDFzNEe2
KBV20C MUTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NIX5WFZKSzVyPUOwJI5O MYCxNFQyOTR5Nh?=
KB7D NIX6Oo5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NWfWbXFOUUN3ME2zOUBvVQ>? NFWycJkyODRzMUS3Oi=>
KBCamp MlnwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MmrUTWM2OD1zLkC0JO69VQ>? MVyxNFQyOTR5Nh?=
HT29 NGPhdnFkgXSxdH;4bYNqfHliYYPzZZk> M2jC[GlEPTB;OECgcm0> NGjDWZYyODh2MUiwPC=>
A549 M1\kfIN6fG:2b4jpZ4l1gSCjc4PhfS=> MXvJR|UxRTZ5IH7N NVTiSIp7OTB6NEG4NFg>
T24 MUXjfZRwfG:6aXPpeJkh[XO|YYm= MoKzTWM2OD16ODDuUS=> Mn\MNVA5PDF6MEi=
HOP-62 NV;vOFNbT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1LRN2lEPTB;MUCgcm0> NVPlfVZMOTFyMkCyPFM>
HCT-116 NFjIPG5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NF:5N5ZKSzVyPUOwJI5O Mo[xNVExOjB{OEO=
SF-539 MX7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXfJR|UxRTFyIH7N NIrKcokyOTB{MEK4Ny=>
UACC-62 MX\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NIfUfYlKSzVyPUGwJI5O M1vVOlEyODJyMkiz
OVCAR-3 NFj1cGlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGrsRYNKSzVyPUKyNEBvVQ>? NH3FS2UyOTB{MEK4Ny=>
SN12C MYTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWLTcGFFUUN3ME2yNEBvVQ>? NHPEVm4yOTB{MEK4Ny=>
DU-145 Mln2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MULJR|UxRTFyIH7N NEn5Z|UyOTB{MEK4Ny=>
MDA-MB-435 M2K0WWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYjDWWRmUUN3ME20NEBvVQ>? M{LINVEyODJyMkiz
WiDr NXWyXZRH[3m2b4TvfIlkcXS7IHHzd4F6 MnLJSG1UVw>? Mm[xTWM2OD1zNzDuUS=> NW\yUpNCOTF|M{S1Olk>
A549 MkPPZ5l1d3SxeHnjbZR6KGG|c3H5 M1XiVmROW09? NXHuSGF[UUN3ME2xOEBvVQ>? NG\ZbWQyOTN|NEW2PS=>
MKN45 MYjjfZRwfG:6aXPpeJkh[XO|YYm= M2DRRWROW09? NUe4OlR1UUN3ME2xO{BvVQ>? M17iTVEyOzN2NU[5
SK-OV-3 MWXjfZRwfG:6aXPpeJkh[XO|YYm= NEDyfFlFVVOR M3f4fGlEPTB;MkCgcm0> MV[xNVM{PDV4OR?=
H128 M4D3V4N6fG:2b4jpZ4l1gSCjc4PhfS=> MXXEUXNQ M2jhPWlEPTB;MUigcm0> M2DsN|EyOzN2NU[5
SK-BR-3 MmfSZ5l1d3SxeHnjbZR6KGG|c3H5 NXT1UmI1TE2VTx?= NX\ibXlOUUN3ME2yNEBvVQ>? NGXpcXkyOTN|NEW2PS=>
LX-1 MWPjfZRwfG:6aXPpeJkh[XO|YYm= MYnEUXNQ MmXiTWM2OD1zMkCgcm0> NHnKdmwyOTh3OEezOy=>
HCT116 MWrjfZRwfG:6aXPpeJkh[XO|YYm= M2Xpe2ROW09? NYPj[YI5UUN3ME25JI5O NFG0PZkyOTh3OEezOy=>
A2780 NYCxZnE{[3m2b4TvfIlkcXS7IHHzd4F6 Mom0SG1UVw>? M37JNWlEPTB;NDDuUS=> NG\2PVUyOTh3OEezOy=>
IMR-32 NGPEPVdkgXSxdH;4bYNqfHliYYPzZZk> MY\+NVAh|ryP M2fRfWROW09? MlrMTWM2OD1{LkKxJI5O MoTiNVI3OTd6OUS=
P388 M4OxVYN6fG:2b4jpZ4l1gSCjc4PhfS=> MXfJR|UxRTF|IH7N Ml3tNVI3OjByOEG=
Lewis NXzRV|V6[3m2b4TvfIlkcXS7IHHzd4F6 MkmzTWM2OD1|MzDuUS=> M3rjSFEzPjJyMEix
JLC NF3TeldkgXSxdH;4bYNqfHliYYPzZZk> NY\pUlBYUUN3ME21MlYhdk1? M{nK[VEzPjJyMEix
HT-29 MoTMZ5l1d3SxeHnjbZR6KGG|c3H5 NEWyWnBKSzVyPUGuOEDPxE1? NG\HN4gyOjZ|OUW0NS=>
Caki-2 M3iwdoN6fG:2b4jpZ4l1gSCjc4PhfS=> NFnDe2hKSzVyPUOuPVYh|ryP M1fpflEzPjN7NUSx
A549 MmW5Z5l1d3SxeHnjbZR6KGG|c3H5 MWLJR|UxRTJwNUOg{txO M2W0flEzPjN7NUSx
HEC-1-B MVjjfZRwfG:6aXPpeJkh[XO|YYm= NHvTRmNKSzVyPUiuOlQh|ryP NVL2W4ZOOTJ4M{m1OFE>
HL-60 NXjOTGdu[3m2b4TvfIlkcXS7IHHzd4F6 MmPWTWM2OD14NjDuUS=> M2\sWFEzPjN7NUSx
Col2 MmLuZ5l1d3SxeHnjbZR6KGG|c3H5 MXT+NUDPxE1? NWe4[W1{TUR3ME21O{BvVQ>? NYLGeJBbOTVyNEO0NFc>
HUVEC Mn:2Z5l1d3SxeHnjbZR6KGG|c3H5 M4jEOp4yKM7:TR?= MmjhSWQ2OD1{NUigcm0> MX6xOVA1OzRyNx?=
KB M4\YeIN6fG:2b4jpZ4l1gSCjc4PhfS=> NYjUWFV3hjFizszN NGLqcmtGTDVyPUKyJI5O NVPPellZOTVyNEO0NFc>
LCNaP MUPjfZRwfG:6aXPpeJkh[XO|YYm= NYrOc25[hjFizszN NETM[5pGTDVyPUK4JI5O M3zyb|E2ODR|NEC3
Lu1 MkXtZ5l1d3SxeHnjbZR6KGG|c3H5 NVfLWZc6hjFizszN MlLwSWQ2OD1{OTDuUS=> MUmxOVA1OzRyNx?=
RPMI8402 NIjhUW1kgXSxdH;4bYNqfHliYYPzZZk> NIT6PGh,OTBizszN MnjSTWM2OD14IH7N Ml3WNVU1QDJ7Mkm=
CPT-K5 M3HXPIN6fG:2b4jpZ4l1gSCjc4PhfS=> NFW0blB,OTBizszN MlvrTWM2OD5zMDFOwG0> NI\YOZQyPTR6MkmyPS=>
P388 NUTRToVr[3m2b4TvfIlkcXS7IHHzd4F6 NV7aR3hNhjFyIN88US=> MUDJR|UxRTF2IH7N NVixe4ZSOTV2OEK5Nlk>
P388/CPT45 NVvSU5NZ[3m2b4TvfIlkcXS7IHHzd4F6 MmHsglExKM7:TR?= NWfJdYtvUUN3ME6xNEDPxE1? NIrRb|cyPTR6MkmyPS=>
KB3-1 NXTvXZlx[3m2b4TvfIlkcXS7IHHzd4F6 NFnPbYd,OTBizszN MVLJR|UxRTRyIH7N MYexOVQ5Ojl{OR?=
KBV-1 + MDR1 MoHQZ5l1d3SxeHnjbZR6KGG|c3H5 MnS5glExKM7:TR?= M4jsSGlEPTB;NESwJI5O MoqwNVU1QDJ7Mkm=
KBH NUDueY5j[3m2b4TvfIlkcXS7IHHzd4F6 M3\YTp4yOCEQvF2= NVzlS3lvUUN3ME20OFAhdk1? NXPC[nlROTV2OEK5Nlk>
HOP-62 M4f6TIN6fG:2b4jpZ4l1gSCjc4PhfS=> MmTiglExKM7:TR?= MljhS2k2OD1zMDDuUS=> Ml\tNVU2ODlzNkS=
HCT-116 M3i0b4N6fG:2b4jpZ4l1gSCjc4PhfS=> NG[z[Zp,OTBizszN NYjBZZd7T0l3ME2zNEBvVQ>? MkXPNVU2ODlzNkS=
F-539 M3TwOYN6fG:2b4jpZ4l1gSCjc4PhfS=> MmL0glExKM7:TR?= NH7IWZhIUTVyPUGwJI5O M1uwcVE2PTB7MU[0
UACC-62 NYDDXFhM[3m2b4TvfIlkcXS7IHHzd4F6 M3nSPJ4yOCEQvF2= NV:0e2xGT0l3ME2xNEBvVQ>? MXmxOVUxQTF4NB?=
OVCAR-3 NF\LWWxkgXSxdH;4bYNqfHliYYPzZZk> NVHsXZNThjFyIN88US=> M2H1R2dKPTB;MkKwJI5O MXixOVUxQTF4NB?=
SN12C NFfDfFdkgXSxdH;4bYNqfHliYYPzZZk> NHjHXHh,OTBizszN MXrHTVUxRTJyIH7N M1njdFE2PTB7MU[0
DU-145 NF3ibVFkgXSxdH;4bYNqfHliYYPzZZk> M4[2Up4yOCEQvF2= M3zITGdKPTB;MUCgcm0> MnK1NVU2ODlzNkS=
MDA-MB-435 MknKZ5l1d3SxeHnjbZR6KGG|c3H5 NG\4Uol,OTBizszN MVLHTVUxRTRyIH7N NYXMZZk5OTV3MEmxOlQ>
MT-4 MXvjfZRwfG:6aXPpeJkh[XO|YYm= NELTVJNKSzVyPUSgcm0> MlOyNVczPTR4Nkm=
CCRF-CEMc NHLEWoNkgXSxdH;4bYNqfHliYYPzZZk> MVrJR|UxRTNibl2= NYjIWGJNOTd{NUS2Olk>
WIL-2NSd NWP1bJdx[3m2b4TvfIlkcXS7IHHzd4F6 MmnMTWM2OD13IH7N MkWyNVczPTR4Nkm=
CCRF-SB MmfJZ5l1d3SxeHnjbZR6KGG|c3H5 MoK2TWM2OD1|IH7N MVOxO|I2PDZ4OR?=
CRL 7065 NX\3WVBM[3m2b4TvfIlkcXS7IHHzd4F6 MVXJR|UxRTRyMDDuUS=> NU\td5ZVOTd{NUS2Olk>
SK-MEL-28b MWPjfZRwfG:6aXPpeJkh[XO|YYm= MnnSTWM2OD12MDDuUS=> NE\GTJgyPzJ3NE[2PS=>
MCF-7 MXvjfZRwfG:6aXPpeJkh[XO|YYm= M4nmTmlEPTB;NECgcm0> NUT4VnFTOTd{NUS2Olk>
SKMES-1 NEjqR2NkgXSxdH;4bYNqfHliYYPzZZk> NF;Hd4dKSzVyPUGwJI5O MY[xO|I2PDZ4OR?=
HepG2 NE\YOJpkgXSxdH;4bYNqfHliYYPzZZk> MknzTWM2OD1|MDDuUS=> MlX0NVczPTR4Nkm=
DU145 NGL2T3NkgXSxdH;4bYNqfHliYYPzZZk> NYj3WWZoUUN3ME2xNEBvVQ>? MVuxO|I2PDZ4OR?=

... 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 slightly soluble or insoluble
Ethanol slightly soluble or insoluble
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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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