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 NHGwTpJkgXSxdH;4bYNqfHliYYPzZZk> NHvrXppKSzVyPUWxJI5O MWe5NFA{PTJy
SKVLB MWLjfZRwfG:6aXPpeJkh[XO|YYm= NVnQcYtGUUN3ME21N{BvVQ>? M{nzUVkxODN3MkC=
HT29 MUfjfZRwfG:6aXPpeJkh[XO|YYm= NXX3PG81UUN3ME24O{45KG6P NVTCVW1kQTByM{WyNC=>
KB Ml;jZ5l1d3SxeHnjbZR6KGG|c3H5 NHTIZW1KSzVyPUigcm0> NELCSVg6ODB|NUKw
A427 NETnOnlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVz+NUDPxE1? NI\OfI1FVVOR MniwTWM2OD1{NDDuUS=> NVfvbXczQTh5NkGxNS=>
PC-3 M2rFd2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1zjd54yKM7:TR?= M37yb2ROW09? MUjJR|UxRTV5IH7N MoDzPVg4PjFzMR?=
K562adr M1q0Tmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXPqfY9XhjFizszN MVXEUXNQ MlvDTWM2OD13NzDuUS=> MoL0PVg4PjFzMR?=
MCF7mdr NYLxOYlJT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFTncZF,OSEQvF2= NICxPIdFVVOR NX\NNnhzUUN3ME2zMlEhdk1? MXm5PFc3OTFz
P388 NXjyeWxWT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MojoTWM2OD1|MjDuUS=> NX7RbXJMOTB|NE[5N|M>
P388CPT5 R MnnXS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MorzTWM2OD1{Lkig{txO MX:xNFM1Pjl|Mx?=
KBwt MWjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3LBTGlEPTB;NECgcm0> NHHLN|QyODRzMUS3Oi=>
KBMDR MWjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnPrTWM2OD15MDDuUS=> MYmxNFQyOTR5Nh?=
KBV20C NXnK[VA6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXzJR|UxRTNyIH7N NWHXfpppOTB2MUG0O|Y>
KB7D MnK0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2jsbGlEPTB;M{Wgcm0> NEDFPJIyODRzMUS3Oi=>
KBCamp NV65Z5dbT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWXRbYN6UUN3ME2xMlA1KM7:TR?= M1rrdFExPDFzNEe2
HT29 NX\3S4Zu[3m2b4TvfIlkcXS7IHHzd4F6 NG\UeWhKSzVyPUiwJI5O MXixNFg1OThyOB?=
A549 M1fncIN6fG:2b4jpZ4l1gSCjc4PhfS=> MoLMTWM2OD14NzDuUS=> MW[xNFg1OThyOB?=
T24 NXP1Zplp[3m2b4TvfIlkcXS7IHHzd4F6 NHzk[pZKSzVyPUi4JI5O MXexNFg1OThyOB?=
HOP-62 NYfIe20zT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVLJR|UxRTFyIH7N MYqxNVAzODJ6Mx?=
HCT-116 NG\2ZWtIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXjvZlNQUUN3ME2zNEBvVQ>? NYKxN5NjOTFyMkCyPFM>
SF-539 M2nlWGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NV[3OGRpUUN3ME2xNEBvVQ>? NGXzPIEyOTB{MEK4Ny=>
UACC-62 NV:y[5F7T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4nwW2lEPTB;MUCgcm0> MUKxNVAzODJ6Mx?=
OVCAR-3 NXmwfmdrT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NUL5V2pxUUN3ME2yNlAhdk1? MkXVNVExOjB{OEO=
SN12C MVPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MlXsTWM2OD1{MDDuUS=> M{HNTlEyODJyMkiz
DU-145 MmXxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWXJR|UxRTFyIH7N NGDuSpIyOTB{MEK4Ny=>
MDA-MB-435 NVm3Z2VVT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYrJR|UxRTRyIH7N NWS5co9UOTFyMkCyPFM>
WiDr MmP4Z5l1d3SxeHnjbZR6KGG|c3H5 M1LnOGROW09? MmD3TWM2OD1zNzDuUS=> NHfocpEyOTN|NEW2PS=>
A549 M2ezVYN6fG:2b4jpZ4l1gSCjc4PhfS=> M4qxTGROW09? NUi4O4ZzUUN3ME2xOEBvVQ>? NVixeW1IOTF|M{S1Olk>
MKN45 NGrzT3FkgXSxdH;4bYNqfHliYYPzZZk> M2DkT2ROW09? M4Xq[WlEPTB;MUegcm0> M1uxNlEyOzN2NU[5
SK-OV-3 MormZ5l1d3SxeHnjbZR6KGG|c3H5 MXPEUXNQ M{fVcGlEPTB;MkCgcm0> MlvaNVE{OzR3Nkm=
H128 M2m3U4N6fG:2b4jpZ4l1gSCjc4PhfS=> M1fIXWROW09? MnfWTWM2OD1zODDuUS=> NYfVV2doOTF|M{S1Olk>
SK-BR-3 NG\oSZdkgXSxdH;4bYNqfHliYYPzZZk> NEHITo9FVVOR NYHmPYtRUUN3ME2yNEBvVQ>? MXSxNVM{PDV4OR?=
LX-1 MX;jfZRwfG:6aXPpeJkh[XO|YYm= NUDqWnd2TE2VTx?= MYnJR|UxRTF{MDDuUS=> NHHX[ZQyOTh3OEezOy=>
HCT116 M2jOfYN6fG:2b4jpZ4l1gSCjc4PhfS=> MYPEUXNQ M1zr[GlEPTB;OTDuUS=> M1vV[lEyQDV6N{O3
A2780 MX3jfZRwfG:6aXPpeJkh[XO|YYm= NF;sZnBFVVOR MWTJR|UxRTRibl2= NWCyU|VvOTF6NUi3N|c>
IMR-32 NIWzNGlkgXSxdH;4bYNqfHliYYPzZZk> NITZ[|Z,OTBizszN NFz4XJRFVVOR NY\Me2FMUUN3ME2yMlIyKG6P NXy0[VhMOTJ4MUe4PVQ>
P388 MWLjfZRwfG:6aXPpeJkh[XO|YYm= MoDYTWM2OD1zMzDuUS=> NHLHb3UyOjZ{MEC4NS=>
Lewis NV\UdHhv[3m2b4TvfIlkcXS7IHHzd4F6 NWjUN2RUUUN3ME2zN{BvVQ>? NIPDV2QyOjZ{MEC4NS=>
JLC M{DFVIN6fG:2b4jpZ4l1gSCjc4PhfS=> MV3JR|UxRTVwNjDuUS=> NF\Y[pYyOjZ{MEC4NS=>
HT-29 M2LlcYN6fG:2b4jpZ4l1gSCjc4PhfS=> NFvWN49KSzVyPUGuOEDPxE1? MV[xNlY{QTV2MR?=
Caki-2 MV7jfZRwfG:6aXPpeJkh[XO|YYm= NX2xN|NpUUN3ME2zMlk3KM7:TR?= NYGyUopxOTJ4M{m1OFE>
A549 MXPjfZRwfG:6aXPpeJkh[XO|YYm= MlrkTWM2OD1{LkWzJO69VQ>? NVHvNpIzOTJ4M{m1OFE>
HEC-1-B MUDjfZRwfG:6aXPpeJkh[XO|YYm= MkKzTWM2OD16Lk[0JO69VQ>? NXvKZnFKOTJ4M{m1OFE>
HL-60 M3HpNIN6fG:2b4jpZ4l1gSCjc4PhfS=> Mn32TWM2OD14NjDuUS=> M3m1WFEzPjN7NUSx
Col2 MkHxZ5l1d3SxeHnjbZR6KGG|c3H5 MoPkglEh|ryP M4nsXWVFPTB;NUegcm0> NWPQNWd1OTVyNEO0NFc>
HUVEC NX\ZfYtI[3m2b4TvfIlkcXS7IHHzd4F6 NWjPc3pMhjFizszN MlnKSWQ2OD1{NUigcm0> NIXUWmgyPTB2M{SwOy=>
KB MXzjfZRwfG:6aXPpeJkh[XO|YYm= M1fSd54yKM7:TR?= Mlf6SWQ2OD1{MjDuUS=> MUSxOVA1OzRyNx?=
LCNaP MoS2Z5l1d3SxeHnjbZR6KGG|c3H5 MoT3glEh|ryP M1fXXWVFPTB;Mkigcm0> NGnLZWMyPTB2M{SwOy=>
Lu1 NXrRWIpw[3m2b4TvfIlkcXS7IHHzd4F6 M{Pa[J4yKM7:TR?= NV6we3k3TUR3ME2yPUBvVQ>? NIj6TlEyPTB2M{SwOy=>
RPMI8402 MYXjfZRwfG:6aXPpeJkh[XO|YYm= NHuye2Z,OTBizszN MlTOTWM2OD14IH7N NEf4OIIyPTR6MkmyPS=>
CPT-K5 NIfnOlhkgXSxdH;4bYNqfHliYYPzZZk> MlPaglExKM7:TR?= MkHxTWM2OD5zMDFOwG0> MVKxOVQ5Ojl{OR?=
P388 NVu4bWtl[3m2b4TvfIlkcXS7IHHzd4F6 NF\NNIR,OTBizszN NUT0OY0zUUN3ME2xOEBvVQ>? MVSxOVQ5Ojl{OR?=
P388/CPT45 MV7jfZRwfG:6aXPpeJkh[XO|YYm= NE\zVXV,OTBizszN MlW5TWM2OD5zMDFOwG0> MlzmNVU1QDJ7Mkm=
KB3-1 MljhZ5l1d3SxeHnjbZR6KGG|c3H5 NUjEcJQ5hjFyIN88US=> MWrJR|UxRTRyIH7N M3vPd|E2PDh{OUK5
KBV-1 + MDR1 NYXkcmF3[3m2b4TvfIlkcXS7IHHzd4F6 MWH+NVAh|ryP M2rwWWlEPTB;NESwJI5O M{XONVE2PDh{OUK5
KBH MkDOZ5l1d3SxeHnjbZR6KGG|c3H5 MlfpglExKM7:TR?= M3ywe2lEPTB;NESwJI5O NF;sSo8yPTR6MkmyPS=>
HOP-62 NV3LdoJ6[3m2b4TvfIlkcXS7IHHzd4F6 MofFglExKM7:TR?= MmHUS2k2OD1zMDDuUS=> NVSzUINNOTV3MEmxOlQ>
HCT-116 NYHXZWd5[3m2b4TvfIlkcXS7IHHzd4F6 NHjjTJV,OTBizszN MlXSS2k2OD1|MDDuUS=> NF6xWVYyPTVyOUG2OC=>
F-539 M1L2dIN6fG:2b4jpZ4l1gSCjc4PhfS=> NUDNeZdnhjFyIN88US=> MUnHTVUxRTFyIH7N M{jFb|E2PTB7MU[0
UACC-62 MUDjfZRwfG:6aXPpeJkh[XO|YYm= MlX2glExKM7:TR?= NVzVbHhRT0l3ME2xNEBvVQ>? NUTs[4NVOTV3MEmxOlQ>
OVCAR-3 MUnjfZRwfG:6aXPpeJkh[XO|YYm= MnrsglExKM7:TR?= NHrIV3lIUTVyPUKyNEBvVQ>? MkjrNVU2ODlzNkS=
SN12C NVP0bFV2[3m2b4TvfIlkcXS7IHHzd4F6 NHniOXZ,OTBizszN NUPWNXdbT0l3ME2yNEBvVQ>? NXjIZW4zOTV3MEmxOlQ>
DU-145 NFXGTHBkgXSxdH;4bYNqfHliYYPzZZk> MlnjglExKM7:TR?= MoHiS2k2OD1zMDDuUS=> NYHyNoNzOTV3MEmxOlQ>
MDA-MB-435 NWHBdZJr[3m2b4TvfIlkcXS7IHHzd4F6 MlHVglExKM7:TR?= NVOwNYlIT0l3ME20NEBvVQ>? M3jUb|E2PTB7MU[0
MT-4 MnjzZ5l1d3SxeHnjbZR6KGG|c3H5 NEDzRnVKSzVyPUSgcm0> Ml2wNVczPTR4Nkm=
CCRF-CEMc M2nKTIN6fG:2b4jpZ4l1gSCjc4PhfS=> NGTm[ppKSzVyPUOgcm0> NF;ZSIQyPzJ3NE[2PS=>
WIL-2NSd NGDieXJkgXSxdH;4bYNqfHliYYPzZZk> MmLJTWM2OD13IH7N NX\mdnViOTd{NUS2Olk>
CCRF-SB NUPOeItl[3m2b4TvfIlkcXS7IHHzd4F6 NWjaVoJmUUN3ME2zJI5O M1GwXVE4OjV2Nk[5
CRL 7065 MYjjfZRwfG:6aXPpeJkh[XO|YYm= NHnrZW9KSzVyPUSwNEBvVQ>? MlHONVczPTR4Nkm=
SK-MEL-28b MmDnZ5l1d3SxeHnjbZR6KGG|c3H5 M1TLO2lEPTB;NECgcm0> NUKxVI1yOTd{NUS2Olk>
MCF-7 MUDjfZRwfG:6aXPpeJkh[XO|YYm= NHznfWxKSzVyPUSwJI5O NWD0PHR2OTd{NUS2Olk>
SKMES-1 NIPvTHNkgXSxdH;4bYNqfHliYYPzZZk> MWLJR|UxRTFyIH7N M1mwWlE4OjV2Nk[5
HepG2 MYnjfZRwfG:6aXPpeJkh[XO|YYm= MnvrTWM2OD1|MDDuUS=> NFrCUmsyPzJ3NE[2PS=>
DU145 Mo\ZZ5l1d3SxeHnjbZR6KGG|c3H5 MX7JR|UxRTFyIH7N M4XhcFE4OjV2Nk[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
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