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 NXnpWZFC[3m2b4TvfIlkcXS7IHHzd4F6 M3PZTWlEPTB;NUGgcm0> MnL6PVAxOzV{MB?=
SKVLB M2jmVIN6fG:2b4jpZ4l1gSCjc4PhfS=> NVu5c4tlUUN3ME21N{BvVQ>? Mn7DPVAxOzV{MB?=
HT29 NX7sNHRj[3m2b4TvfIlkcXS7IHHzd4F6 MVLJR|UxRTh5Lkigcm0> M{flUlkxODN3MkC=
KB MkPCZ5l1d3SxeHnjbZR6KGG|c3H5 M4nYVWlEPTB;ODDuUS=> MVq5NFA{PTJy
A427 NHy3bpJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MoL2glEh|ryP MX3EUXNQ MX;JR|UxRTJ2IH7N MmHTPVg4PjFzMR?=
PC-3 MVHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NELn[pR,OSEQvF2= NHXCSFVFVVOR NV;GRnpJUUN3ME21O{BvVQ>? Ml7CPVg4PjFzMR?=
K562adr NWDWco8yT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVP+NUDPxE1? NGnDSpdFVVOR M3PSTWlEPTB;NUegcm0> Ml\sPVg4PjFzMR?=
MCF7mdr NYHvbWxQT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVn+NUDPxE1? Mlz4SG1UVw>? NEPpNoxKSzVyPUOuNUBvVQ>? NVPNUG56QTh5NkGxNS=>
P388 NUjnOW45T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MV;JR|UxRTN{IH7N MX[xNFM1Pjl|Mx?=
P388CPT5 R M17DOmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MnrYTWM2OD1{Lkig{txO MV[xNFM1Pjl|Mx?=
KBwt MXXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MmjOTWM2OD12MDDuUS=> MlqzNVA1OTF2N{[=
KBMDR M1HwdWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmjqTWM2OD15MDDuUS=> M2\2flExPDFzNEe2
KBV20C MUTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHzqcHlKSzVyPUOwJI5O NUXidlRUOTB2MUG0O|Y>
KB7D NYLybG9CT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NHLBO45KSzVyPUO1JI5O MWOxNFQyOTR5Nh?=
KBCamp MkfrS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2\DcWlEPTB;MT6wOEDPxE1? M362NlExPDFzNEe2
HT29 Mn3vZ5l1d3SxeHnjbZR6KGG|c3H5 NHnQUWJKSzVyPUiwJI5O NULKS29sOTB6NEG4NFg>
A549 M2n1VYN6fG:2b4jpZ4l1gSCjc4PhfS=> NVvnVnplUUN3ME22O{BvVQ>? MWSxNFg1OThyOB?=
T24 Mo[3Z5l1d3SxeHnjbZR6KGG|c3H5 MWjJR|UxRTh6IH7N NHfkS2IyODh2MUiwPC=>
HOP-62 MlH1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M363eGlEPTB;MUCgcm0> NV;1[VNQOTFyMkCyPFM>
HCT-116 NVrxNGlDT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmTKTWM2OD1|MDDuUS=> MVOxNVAzODJ6Mx?=
SF-539 M{Tobmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mn3lTWM2OD1zMDDuUS=> NWfDSI5oOTFyMkCyPFM>
UACC-62 MWTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVXJR|UxRTFyIH7N MWOxNVAzODJ6Mx?=
OVCAR-3 M1HsW2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYLYOYllUUN3ME2yNlAhdk1? MYqxNVAzODJ6Mx?=
SN12C NFnmcphIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVO1d4xKUUN3ME2yNEBvVQ>? MWWxNVAzODJ6Mx?=
DU-145 MoLlS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWfJR|UxRTFyIH7N NHfjcW8yOTB{MEK4Ny=>
MDA-MB-435 M{LZR2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3XhNmlEPTB;NECgcm0> M3[1cVEyODJyMkiz
WiDr MkHZZ5l1d3SxeHnjbZR6KGG|c3H5 Mmf6SG1UVw>? M{PLXmlEPTB;MUegcm0> NVLhfppTOTF|M{S1Olk>
A549 MorvZ5l1d3SxeHnjbZR6KGG|c3H5 M1HtPGROW09? NXPpfnkyUUN3ME2xOEBvVQ>? NVm3ZphqOTF|M{S1Olk>
MKN45 MkHtZ5l1d3SxeHnjbZR6KGG|c3H5 Mle5SG1UVw>? MlrmTWM2OD1zNzDuUS=> MnjWNVE{OzR3Nkm=
SK-OV-3 M4fSWIN6fG:2b4jpZ4l1gSCjc4PhfS=> MYfEUXNQ MXLJR|UxRTJyIH7N MX[xNVM{PDV4OR?=
H128 NFXufYJkgXSxdH;4bYNqfHliYYPzZZk> NH3BcXVFVVOR NWDQ[HZwUUN3ME2xPEBvVQ>? M{fmTlEyOzN2NU[5
SK-BR-3 M3;SdoN6fG:2b4jpZ4l1gSCjc4PhfS=> NGSwZVVFVVOR NVf2WWZsUUN3ME2yNEBvVQ>? MVixNVM{PDV4OR?=
LX-1 M4e5ToN6fG:2b4jpZ4l1gSCjc4PhfS=> NV7BenI5TE2VTx?= MUPJR|UxRTF{MDDuUS=> M2KxWlEyQDV6N{O3
HCT116 M4TZ[YN6fG:2b4jpZ4l1gSCjc4PhfS=> M1f3SGROW09? MXrJR|UxRTlibl2= MmXkNVE5PTh5M{e=
A2780 NEm4dmdkgXSxdH;4bYNqfHliYYPzZZk> MWnEUXNQ MVfJR|UxRTRibl2= NEnTXlkyOTh3OEezOy=>
IMR-32 Mny2Z5l1d3SxeHnjbZR6KGG|c3H5 MnvGglExKM7:TR?= NFf3N4xFVVOR M{[wO2lEPTB;Mj6yNUBvVQ>? NEfMO4EyOjZzN{i5OC=>
P388 MVHjfZRwfG:6aXPpeJkh[XO|YYm= NWfi[WZ[UUN3ME2xN{BvVQ>? MXqxNlYzODB6MR?=
Lewis MkizZ5l1d3SxeHnjbZR6KGG|c3H5 Mm\HTWM2OD1|MzDuUS=> NFriemcyOjZ{MEC4NS=>
JLC NIrlbYNkgXSxdH;4bYNqfHliYYPzZZk> M3TqbGlEPTB;NT62JI5O NHWyWnAyOjZ{MEC4NS=>
HT-29 MYfjfZRwfG:6aXPpeJkh[XO|YYm= MkHOTWM2OD1zLkSg{txO NYPrRppWOTJ4M{m1OFE>
Caki-2 NHvNV2pkgXSxdH;4bYNqfHliYYPzZZk> NVrUSGdlUUN3ME2zMlk3KM7:TR?= NHX1VYkyOjZ|OUW0NS=>
A549 NEPp[VhkgXSxdH;4bYNqfHliYYPzZZk> M2fNZ2lEPTB;Mj61N{DPxE1? NXT6UXZTOTJ4M{m1OFE>
HEC-1-B M1;o[4N6fG:2b4jpZ4l1gSCjc4PhfS=> Ml;0TWM2OD16Lk[0JO69VQ>? MlPzNVI3Ozl3NEG=
HL-60 M1HFV4N6fG:2b4jpZ4l1gSCjc4PhfS=> M3vIc2lEPTB;Nk[gcm0> MVOxNlY{QTV2MR?=
Col2 NFLj[3hkgXSxdH;4bYNqfHliYYPzZZk> M3\PTJ4yKM7:TR?= NGLKVmVGTDVyPUW3JI5O NG\5OooyPTB2M{SwOy=>
HUVEC MX\jfZRwfG:6aXPpeJkh[XO|YYm= MojFglEh|ryP NIW5[lRGTDVyPUK1PEBvVQ>? NI[0eWEyPTB2M{SwOy=>
KB Mm[zZ5l1d3SxeHnjbZR6KGG|c3H5 MoLuglEh|ryP NFLPb|lGTDVyPUKyJI5O MU[xOVA1OzRyNx?=
LCNaP MYDjfZRwfG:6aXPpeJkh[XO|YYm= MkjYglEh|ryP NYrRXGx6TUR3ME2yPEBvVQ>? NVPheIxJOTVyNEO0NFc>
Lu1 MUnjfZRwfG:6aXPpeJkh[XO|YYm= NFHWdo1,OSEQvF2= M{XGWGVFPTB;Mkmgcm0> NXfCR3lrOTVyNEO0NFc>
RPMI8402 M2TzSIN6fG:2b4jpZ4l1gSCjc4PhfS=> NWjNWI96hjFyIN88US=> MUXJR|UxRTZibl2= M2HMWlE2PDh{OUK5
CPT-K5 NWTucmdS[3m2b4TvfIlkcXS7IHHzd4F6 MWH+NVAh|ryP NFfQclZKSzVyPkGwJO69VQ>? MX6xOVQ5Ojl{OR?=
P388 MnnrZ5l1d3SxeHnjbZR6KGG|c3H5 MlvEglExKM7:TR?= NFXyWIVKSzVyPUG0JI5O NEnrNmMyPTR6MkmyPS=>
P388/CPT45 NFLY[IhkgXSxdH;4bYNqfHliYYPzZZk> NXf2N2RxhjFyIN88US=> NELp[2pKSzVyPkGwJO69VQ>? NXTmUZY{OTV2OEK5Nlk>
KB3-1 NED1PIpkgXSxdH;4bYNqfHliYYPzZZk> NWP4UHh[hjFyIN88US=> MUPJR|UxRTRyIH7N NXH0R29nOTV2OEK5Nlk>
KBV-1 + MDR1 NFfwNYhkgXSxdH;4bYNqfHliYYPzZZk> M4XXb54yOCEQvF2= NHnFS|dKSzVyPUS0NEBvVQ>? NHnZTGcyPTR6MkmyPS=>
KBH Mm\GZ5l1d3SxeHnjbZR6KGG|c3H5 NIHNWlh,OTBizszN NHz3R|JKSzVyPUS0NEBvVQ>? M2Hv[|E2PDh{OUK5
HOP-62 NX\ENmdT[3m2b4TvfIlkcXS7IHHzd4F6 M4DFTZ4yOCEQvF2= M3HsOGdKPTB;MUCgcm0> MUGxOVUxQTF4NB?=
HCT-116 NHrZXZRkgXSxdH;4bYNqfHliYYPzZZk> NI\hTmR,OTBizszN MYHHTVUxRTNyIH7N NIr3WlgyPTVyOUG2OC=>
F-539 Ml\uZ5l1d3SxeHnjbZR6KGG|c3H5 NVrBPYFFhjFyIN88US=> M1P1fmdKPTB;MUCgcm0> NF2yVFgyPTVyOUG2OC=>
UACC-62 NILRXXpkgXSxdH;4bYNqfHliYYPzZZk> MnHhglExKM7:TR?= MXjHTVUxRTFyIH7N Mkf0NVU2ODlzNkS=
OVCAR-3 MkXHZ5l1d3SxeHnjbZR6KGG|c3H5 NHvJfol,OTBizszN NF;VPVdIUTVyPUKyNEBvVQ>? M3HSN|E2PTB7MU[0
SN12C MnjFZ5l1d3SxeHnjbZR6KGG|c3H5 MnHiglExKM7:TR?= NIfaZZFIUTVyPUKwJI5O MYSxOVUxQTF4NB?=
DU-145 M3LCPIN6fG:2b4jpZ4l1gSCjc4PhfS=> NUHKW3l2hjFyIN88US=> M1vmNmdKPTB;MUCgcm0> MoPTNVU2ODlzNkS=
MDA-MB-435 NU\2PHNZ[3m2b4TvfIlkcXS7IHHzd4F6 MoT4glExKM7:TR?= NH;QNodIUTVyPUSwJI5O MWWxOVUxQTF4NB?=
MT-4 MYjjfZRwfG:6aXPpeJkh[XO|YYm= M{jMeWlEPTB;NDDuUS=> NEnnZogyPzJ3NE[2PS=>
CCRF-CEMc Mn\YZ5l1d3SxeHnjbZR6KGG|c3H5 M2n3[WlEPTB;MzDuUS=> NUXQSIt5OTd{NUS2Olk>
WIL-2NSd MY\jfZRwfG:6aXPpeJkh[XO|YYm= NVT3Wmg{UUN3ME21JI5O M4jlb|E4OjV2Nk[5
CCRF-SB NVn2UHJY[3m2b4TvfIlkcXS7IHHzd4F6 MnTMTWM2OD1|IH7N MkX5NVczPTR4Nkm=
CRL 7065 MWfjfZRwfG:6aXPpeJkh[XO|YYm= NISyO3ZKSzVyPUSwNEBvVQ>? M3TOTVE4OjV2Nk[5
SK-MEL-28b NWjwc2tT[3m2b4TvfIlkcXS7IHHzd4F6 MUfJR|UxRTRyIH7N M4[4W|E4OjV2Nk[5
MCF-7 NGnJN4VkgXSxdH;4bYNqfHliYYPzZZk> M{HqR2lEPTB;NECgcm0> Mnj5NVczPTR4Nkm=
SKMES-1 NIiyOG9kgXSxdH;4bYNqfHliYYPzZZk> M3j5[GlEPTB;MUCgcm0> NUPwZWFnOTd{NUS2Olk>
HepG2 Mmr2Z5l1d3SxeHnjbZR6KGG|c3H5 MmrQTWM2OD1|MDDuUS=> NGfJOVQyPzJ3NE[2PS=>
DU145 M3TlWYN6fG:2b4jpZ4l1gSCjc4PhfS=> MYTJR|UxRTFyIH7N MWqxO|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 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
NCT03531827 Recruiting Metastatic Castration Resistant Prostate Cancer|Prostate Neoplasms National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) October 22 2018 Phase 2
NCT01202370 Completed Solid Malignancies University of Kentucky|Arno Therapeutics September 2010 Phase 1
NCT00947739 Completed Advanced Solid Tumors|Lymphomas New Mexico Cancer Care Alliance|Christus Stehlin Foundation for Cancer Research September 2008 Phase 1
NCT02575638 Recruiting Malignant Lymphoma of Extranodal and/or Solid Organ Site|Solid Tumor Cao Pharmaceuticals Inc.|The University of Texas Health Science Center at San Antonio July 2008 Phase 1
NCT00080002 Terminated Cancer of Stomach|Gastroesophageal Cancer Enzon Pharmaceuticals Inc. December 2003 Phase 2
NCT00412542 Completed Glioblastoma Multiforme|Glioma M.D. Anderson Cancer Center|Celgene Corporation October 2003 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.

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Topoisomerase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID