Camptothecin

For research use only. Not for use in humans.

製品コードS1288 別名:NSC-100880

Camptothecin化学構造

分子量(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. Camptothecin induces apoptosis in cancer cells via microRNA-125b-mediated mitochondrial pathways. Phase 2.

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生物活性

製品説明 Camptothecin is a specific inhibitor of DNA topoisomerase I (Topo I) with IC50 of 0.68 μM in a cell-free assay. Camptothecin induces apoptosis in cancer cells via microRNA-125b-mediated mitochondrial pathways. Phase 2.
ターゲット
Topo I [2]
(Cell-free assay)
0.68 μM
体外試験

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.

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SKOV3 M4rjU4N6fG:2b4jpZ4l1gSCjc4PhfS=> NYjQZ2ZjUUN3ME21NUBvVQ>? MmnNPVAxOzV{MB?=
SKVLB NWjucI9t[3m2b4TvfIlkcXS7IHHzd4F6 MULJR|UxRTV|IH7N NWPLbFJXQTByM{WyNC=>
HT29 M2j4eYN6fG:2b4jpZ4l1gSCjc4PhfS=> MU\JR|UxRTh5Lkigcm0> MkPjPVAxOzV{MB?=
KB NIDlNpdkgXSxdH;4bYNqfHliYYPzZZk> NUHVR2hYUUN3ME24JI5O MUW5NFA{PTJy
A427 MWXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MUD+NUDPxE1? MmDlSG1UVw>? NXe2Zo9ZUUN3ME2yOEBvVQ>? NX7pTnNQQTh5NkGxNS=>
PC-3 MW\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXX+NUDPxE1? NXPQOXNNTE2VTx?= NIrE[5ZKSzVyPUW3JI5O MUO5PFc3OTFz
K562adr MYLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYqxUopMhjFizszN MWrEUXNQ MXjJR|UxRTV5IH7N MUO5PFc3OTFz
MCF7mdr NHnQe41Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGSzcIZ,OSEQvF2= M2Tve2ROW09? NVnvTHFYUUN3ME2zMlEhdk1? M{nDZlk5PzZzMUG=
P388 MVPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1vMOGlEPTB;M{Kgcm0> NI[wNZQyODN2NkmzNy=>
P388CPT5 R MXvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGS3[JRKSzVyPUKuPEDPxE1? NUH0dmxxOTB|NE[5N|M>
KBwt M1\Ec2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXPJR|UxRTRyIH7N MV6xNFQyOTR5Nh?=
KBMDR MXTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MX3JR|UxRTdyIH7N M1jXS|ExPDFzNEe2
KBV20C NFnUN2hIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4jWeGlEPTB;M{Cgcm0> NUn3RYlUOTB2MUG0O|Y>
KB7D NEHqfFBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Ml3LTWM2OD1|NTDuUS=> MnfDNVA1OTF2N{[=
KBCamp NX7WVoszT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGC0S5RKSzVyPUGuNFQh|ryP M2LMR|ExPDFzNEe2
HT29 NXHoRYxk[3m2b4TvfIlkcXS7IHHzd4F6 NHjoXVZKSzVyPUiwJI5O NFr6NWEyODh2MUiwPC=>
A549 MUnjfZRwfG:6aXPpeJkh[XO|YYm= Ml;0TWM2OD14NzDuUS=> NE\MSWQyODh2MUiwPC=>
T24 NEnWeoVkgXSxdH;4bYNqfHliYYPzZZk> NXHCNZF7UUN3ME24PEBvVQ>? Ml3LNVA5PDF6MEi=
HOP-62 M4DJTGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Ml3ZTWM2OD1zMDDuUS=> Ml\0NVExOjB{OEO=
HCT-116 NH;hXXpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NIG1V4hKSzVyPUOwJI5O M1mybFEyODJyMkiz
SF-539 M4npemdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4DYNWlEPTB;MUCgcm0> M2jhZVEyODJyMkiz
UACC-62 Mn\IS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYrJR|UxRTFyIH7N MUGxNVAzODJ6Mx?=
OVCAR-3 M3HhTmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYnJR|UxRTJ{MDDuUS=> M17nNFEyODJyMkiz
SN12C MX;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NH\kXHlKSzVyPUKwJI5O NED3dXkyOTB{MEK4Ny=>
DU-145 M1;aXGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGLTd5lKSzVyPUGwJI5O NYTWVnNzOTFyMkCyPFM>
MDA-MB-435 NELoS3pIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NUXs[5FqUUN3ME20NEBvVQ>? M2LDWVEyODJyMkiz
WiDr MULjfZRwfG:6aXPpeJkh[XO|YYm= M2nKSWROW09? MlrMTWM2OD1zNzDuUS=> NYnTd4NmOTF|M{S1Olk>
A549 NGCye|BkgXSxdH;4bYNqfHliYYPzZZk> NXHnNW9nTE2VTx?= M3ziZ2lEPTB;MUSgcm0> MX6xNVM{PDV4OR?=
MKN45 NFnQ[JVkgXSxdH;4bYNqfHliYYPzZZk> M4XjOGROW09? NF6zco5KSzVyPUG3JI5O MUexNVM{PDV4OR?=
SK-OV-3 NWrGVG1x[3m2b4TvfIlkcXS7IHHzd4F6 Mo\ZSG1UVw>? Mli4TWM2OD1{MDDuUS=> MnXSNVE{OzR3Nkm=
H128 NEXPc2VkgXSxdH;4bYNqfHliYYPzZZk> MXXEUXNQ NYP2VYppUUN3ME2xPEBvVQ>? Ml\HNVE{OzR3Nkm=
SK-BR-3 MljPZ5l1d3SxeHnjbZR6KGG|c3H5 NWXQVnQ1TE2VTx?= MV;JR|UxRTJyIH7N MUCxNVM{PDV4OR?=
LX-1 Ml\hZ5l1d3SxeHnjbZR6KGG|c3H5 Mlj6SG1UVw>? NXLKWYh[UUN3ME2xNlAhdk1? NITucJkyOTh3OEezOy=>
HCT116 MVXjfZRwfG:6aXPpeJkh[XO|YYm= NIPoNHpFVVOR M1XZU2lEPTB;OTDuUS=> MV[xNVg2QDd|Nx?=
A2780 M2nLN4N6fG:2b4jpZ4l1gSCjc4PhfS=> NHzLXHlFVVOR NX;2XIY6UUN3ME20JI5O NV24d21EOTF6NUi3N|c>
IMR-32 M1HEWoN6fG:2b4jpZ4l1gSCjc4PhfS=> MmjWglExKM7:TR?= M2j0cGROW09? M4LUV2lEPTB;Mj6yNUBvVQ>? NHz6dGkyOjZzN{i5OC=>
P388 NEjRcYxkgXSxdH;4bYNqfHliYYPzZZk> NHrzWm5KSzVyPUGzJI5O M3\Vc|EzPjJyMEix
Lewis Ml;VZ5l1d3SxeHnjbZR6KGG|c3H5 M4nSS2lEPTB;M{Ogcm0> MV2xNlYzODB6MR?=
JLC NHfVdVBkgXSxdH;4bYNqfHliYYPzZZk> M3PjOWlEPTB;NT62JI5O MnTWNVI3OjByOEG=
HT-29 MnLkZ5l1d3SxeHnjbZR6KGG|c3H5 MWLJR|UxRTFwNDFOwG0> M2rB[lEzPjN7NUSx
Caki-2 NF\Be25kgXSxdH;4bYNqfHliYYPzZZk> NGXkcYxKSzVyPUOuPVYh|ryP NHrJdJoyOjZ|OUW0NS=>
A549 M4G4NIN6fG:2b4jpZ4l1gSCjc4PhfS=> M1zicGlEPTB;Mj61N{DPxE1? M4O1XlEzPjN7NUSx
HEC-1-B M2nKbIN6fG:2b4jpZ4l1gSCjc4PhfS=> NFPLNodKSzVyPUiuOlQh|ryP MYCxNlY{QTV2MR?=
HL-60 NX;acHZp[3m2b4TvfIlkcXS7IHHzd4F6 MkPsTWM2OD14NjDuUS=> NVXXcotQOTJ4M{m1OFE>
Col2 NV\sOG1u[3m2b4TvfIlkcXS7IHHzd4F6 NFnKdZB,OSEQvF2= MkTOSWQ2OD13NzDuUS=> M2DDTVE2ODR|NEC3
HUVEC NG\oZpFkgXSxdH;4bYNqfHliYYPzZZk> MVj+NUDPxE1? MWnFSFUxRTJ3ODDuUS=> M2rQc|E2ODR|NEC3
KB MlX1Z5l1d3SxeHnjbZR6KGG|c3H5 M4HvXZ4yKM7:TR?= M1XwS2VFPTB;MkKgcm0> MXuxOVA1OzRyNx?=
LCNaP MYLjfZRwfG:6aXPpeJkh[XO|YYm= MV\+NUDPxE1? M3fyeGVFPTB;Mkigcm0> Mmn0NVUxPDN2MEe=
Lu1 M4P6WIN6fG:2b4jpZ4l1gSCjc4PhfS=> M3;GdZ4yKM7:TR?= NVu3[3NVTUR3ME2yPUBvVQ>? NXy3b4RQOTVyNEO0NFc>
RPMI8402 M3jrXIN6fG:2b4jpZ4l1gSCjc4PhfS=> MXj+NVAh|ryP M4C5OWlEPTB;NjDuUS=> M1ntTFE2PDh{OUK5
CPT-K5 M4X6VYN6fG:2b4jpZ4l1gSCjc4PhfS=> NXzMcmlMhjFyIN88US=> M4TwZ2lEPTB-MUCg{txO MY[xOVQ5Ojl{OR?=
P388 M1z1[oN6fG:2b4jpZ4l1gSCjc4PhfS=> MmHQglExKM7:TR?= NGXscmJKSzVyPUG0JI5O MmX6NVU1QDJ7Mkm=
P388/CPT45 NH\2elBkgXSxdH;4bYNqfHliYYPzZZk> NVTXbFl[hjFyIN88US=> Mn3RTWM2OD5zMDFOwG0> MYKxOVQ5Ojl{OR?=
KB3-1 NYXRRWhi[3m2b4TvfIlkcXS7IHHzd4F6 M{fHcp4yOCEQvF2= MlfiTWM2OD12MDDuUS=> NEXWTlkyPTR6MkmyPS=>
KBV-1 + MDR1 M1HBeYN6fG:2b4jpZ4l1gSCjc4PhfS=> MmDVglExKM7:TR?= MULJR|UxRTR2MDDuUS=> Ml\6NVU1QDJ7Mkm=
KBH NVPJWpJl[3m2b4TvfIlkcXS7IHHzd4F6 NILyNI5,OTBizszN NGrGSJdKSzVyPUS0NEBvVQ>? MVKxOVQ5Ojl{OR?=
HOP-62 NHjveFZkgXSxdH;4bYNqfHliYYPzZZk> NV7ZSJh[hjFyIN88US=> M2DKNmdKPTB;MUCgcm0> Mon4NVU2ODlzNkS=
HCT-116 MX;jfZRwfG:6aXPpeJkh[XO|YYm= NHjkfZJ,OTBizszN Ml;HS2k2OD1|MDDuUS=> NXrrcZpOOTV3MEmxOlQ>
F-539 MoPIZ5l1d3SxeHnjbZR6KGG|c3H5 MXX+NVAh|ryP M3:yZmdKPTB;MUCgcm0> MWSxOVUxQTF4NB?=
UACC-62 NFHJbIdkgXSxdH;4bYNqfHliYYPzZZk> Mn;uglExKM7:TR?= MX7HTVUxRTFyIH7N MnPMNVU2ODlzNkS=
OVCAR-3 MXTjfZRwfG:6aXPpeJkh[XO|YYm= M13LcJ4yOCEQvF2= NWfYdodOT0l3ME2yNlAhdk1? Mlf2NVU2ODlzNkS=
SN12C M4LtcYN6fG:2b4jpZ4l1gSCjc4PhfS=> M4e5Up4yOCEQvF2= NIrZR2pIUTVyPUKwJI5O M171b|E2PTB7MU[0
DU-145 NUDxe5Fi[3m2b4TvfIlkcXS7IHHzd4F6 MY\+NVAh|ryP NYfDdVJtT0l3ME2xNEBvVQ>? MYexOVUxQTF4NB?=
MDA-MB-435 MoPjZ5l1d3SxeHnjbZR6KGG|c3H5 M{KxT54yOCEQvF2= MkjYS2k2OD12MDDuUS=> NVy5[2xiOTV3MEmxOlQ>
MT-4 MVfjfZRwfG:6aXPpeJkh[XO|YYm= NFnPN4NKSzVyPUSgcm0> MonCNVczPTR4Nkm=
CCRF-CEMc NGXDTIhkgXSxdH;4bYNqfHliYYPzZZk> M1vGUWlEPTB;MzDuUS=> NF3XU44yPzJ3NE[2PS=>
WIL-2NSd Ml3jZ5l1d3SxeHnjbZR6KGG|c3H5 NXrMO28{UUN3ME21JI5O NFnxTVcyPzJ3NE[2PS=>
CCRF-SB MYLjfZRwfG:6aXPpeJkh[XO|YYm= MXjJR|UxRTNibl2= MXyxO|I2PDZ4OR?=
CRL 7065 MVnjfZRwfG:6aXPpeJkh[XO|YYm= M376UmlEPTB;NECwJI5O NEO4cG4yPzJ3NE[2PS=>
SK-MEL-28b MVPjfZRwfG:6aXPpeJkh[XO|YYm= NH;ob|dKSzVyPUSwJI5O NILPbogyPzJ3NE[2PS=>
MCF-7 NUHFbIM3[3m2b4TvfIlkcXS7IHHzd4F6 M2DxWWlEPTB;NECgcm0> MYKxO|I2PDZ4OR?=
SKMES-1 M3PVVYN6fG:2b4jpZ4l1gSCjc4PhfS=> NI\3WJZKSzVyPUGwJI5O MljhNVczPTR4Nkm=
HepG2 NH;rbmxkgXSxdH;4bYNqfHliYYPzZZk> Mn\KTWM2OD1|MDDuUS=> MVSxO|I2PDZ4OR?=
DU145 Mk\QZ5l1d3SxeHnjbZR6KGG|c3H5 M2fodWlEPTB;MUCgcm0> M{THZlE4OjV2Nk[5

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アッセイ
Methods Test Index PMID
Western blot
Cyclin1 / CDK1 / CDK2 ; 

PubMed: 29963130     


Western blot analysis indicated that camptothecin (6 µM) downregulates the expression of cell-cycle-associated proteins, cyclin 1, CDK1 and CDK2 in NPC cells. β-actin was used as a loading control.

Vimentin / Fibronectin / E-cadherin ; 

PubMed: 29963130     


Western blot analysis revealed that camptothecin (6 µM) treatment downregulates the expression of vimentin and fibronectin, and upregulates the expression of E-cadherin in NPC cells. β-actin was used as a loading control. NPC, nasopharyngeal carcinoma.

TGF-β / PI3K / pPI3K / AKT / pAKT ; 

PubMed: 29963130     


Western blot analysis revealed that camptothecin (6 µM) treatment inhibits the expression of TGF-β, PI3K and AKT in NPC cells. 

p53 / Cleaved caspase-3 / Cleaved PARP ; 

PubMed: 17548347     


NPCs in trophic factor-containing media were treated with 10 μM camptothecin for 0, 2, 4, 6, or 8 h, and extracts were immunoblotted for p53, active cleaved caspase-3, cleaved PARP, and total GSK3α/β as a loading control.

29963130 17548347
体内試験 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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[2]
- 合併

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
細胞試験: [2]
- 合併
  • 細胞株: U87MG, A549 and H838 cells
  • 濃度: 0.17 nM–10 mM
  • 反応時間: 48 hours
  • 実験の流れ: 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.
    (参考用のみ)
動物試験:[3]
- 合併
  • 動物モデル: Nude mice (NIH-I high fertility strain) bearing xenografts of CASE, SW48, DOY, SPA, and CLO cells
  • 投薬量: 0–8 mg/kg
  • 投与方法: Administered via i.m. or i.v. injection
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 3 mg/mL (8.61 mM)
Water Insoluble
Ethanol Insoluble

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 348.35
化学式

C20H16N2O4

CAS No. 7689-03-4
Storage powder
in solvent
別名 NSC-100880
Smiles CCC1(O)C(=O)OCC2=C1C=C3N(CC4=C3N=C5C=CC=CC5=C4)C2=O

投与溶媒組成計算器(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)
投与量 mg/kg 動物平均体重 g 投与体積(動物毎) ul 動物数
ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)
% DMSO % % Tween 80 % ddH2O
計算リセット

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須
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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID