Topotecan HCl 化学構造
分子量: 457.91

高品質保証

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製品説明

  • Compare Topoisomerase Inhibitors
    Topoisomerase製品生物活性の比較
  • 研究分野
  • Topotecan HClのメカニズム

製品の説明

生物活性

製品説明 Topotecan HClは、MCF-7リュック細胞とDU-145リュック細胞のためのトポイソメラーゼI阻害剤で、IC50 がそれぞれ 13 nM と 2 nMです。
ターゲット

MCF-7 Luc cells

DU-145 Luc cells

IC50

13 nM

2 nM [1]

In vitro試験 Stronger drug activity of Topotecan is observed for DU-145 Luc and MCF-7 Luc cells. [1] Topotecan causes cytotoxicity during the course of DNA replication by stabilizing the covalent complex between topoisomerase I and DNA and preventing the religation of enzyme-linked single-strand DNA break. Topotecan stabilizes topoisomerase I/DNA cleavable complexes in radiation-resistant human B-lineage acute lymphoblastic leukemia (ALL) cells, causes rapid apoptotic cell death despite high-level expression of bcl-2 protein, and inhibits ALL cell clonogenic growth in a dose-dependent fashion. [2]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
human MDA-MB-435 cells MVrDfZRwfG:6aXRCpIF{e2G7 NV3NXWwyPzJiaB?= M{nIW2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1FSS2PQj20N|Uh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygbYM2OD1zIH7N MkfKNlA{PzFzOEO=
human Bel7402 cells MV;DfZRwfG:6aXRCpIF{e2G7 MkLiPVYhcA>? MnHaR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRoVtPzRyMjDj[YxteyCjZoTldkA6PiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVEvOiCwTR?= NYCwd2ZUOTVzNkWxOFQ>
human HCT8 cells MoH5R5l1d3SxeHnjxsBie3OjeR?= MnLCPVYhcA>? M4XYd2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDhiY3XscJMh[W[2ZYKgPVYhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2xMlUhdk1? NFjNUVkyPTF4NUG0OC=>
human MCF7 cells M13Bc2N6fG:2b4jpZ:Kh[XO|YYm= MWG5OkBp MYrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIFnfGW{IEm2JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MT64JI5O Ml\rNVUyPjVzNES=
human A549 cells NVH2SXdDS3m2b4TvfIlkyqCjc4PhfS=> MlL6PVYhcA>? NGnBdoJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPTR7IHPlcIx{KGGodHXyJFk3KGi{czDifUBOXFRiYYPzZZktKEmFNUC9N{4zKG6P M2XGclE2OTZ3MUS0
human colon carcinoma SW620 cell NIe0ZW5EgXSxdH;4bYPDqGG|c3H5 NWDaVJBES3m2b4TvfIlkKHCxdHXueIlifGmxbjDv[kBVd3CxdHXjZY4hMFSSKTDifUB1cGViY3;tdI92dmRiaX6gbJVu[W5iY3;sc44h[2G{Y3nuc41iKFOZNkKwJINmdGxibHnu[UwhUUN3ME2zMlIhdk1? M3;BVlEzPDB6N{C3
human MESSA cells MYjDfZRwfG:6aXRCpIF{e2G7 NInkbY84OiCq NYXzeYI6S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUWVU1GgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KGGuYX3hdkBjdHWnIHHzd4F6NCCLQ{WwQVQhdk1? NI[yRWgzOTN2MU[3OC=>
human BGC823 cells M3frNWN6fG:2b4jpZ:Kh[XO|YYm= MX65OkBp NX\CO5dyS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSkeFOEKzJINmdGy|IHHmeIVzKDl4IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:PC5|IH7N M2rCdVE2OTZ3MUS0
human Ketr3 cells M2TsbmN6fG:2b4jpZ:Kh[XO|YYm= NFrhWnY6PiCq Mkf2R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gT4V1ejNiY3XscJMh[W[2ZYKgPVYhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME20Mlkhdk1? MU[xOVE3PTF2NB?=
LOX cells Mn35R5l1d3SxeHnjxsBie3OjeR?= NVvsOoY6S3m2b4TvfIlkcXS7IIfhd{Bl\XSncn3pcoVlKGmwII\peJJwKGmwIFzPXEBk\WyuczCocYVt[W6xbXGpJI9nKGi3bXHuJJR2dW:{IHPlcIwhdGmwZYOgZpkhfXOrbnegUXRVKGG|c3H5MEBKSzVyPUWgcm0> NXTBVINYPzh3M{OzNS=>
human A549 cells MorWSpVv[3Srb36gZZN{[Xl? NHTtUXM1KGh? MoDhRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUW0PUBk\WyuczDh[pRmeiB2IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:PSCwTR?= NIPyfJoyQDJyN{e0PC=>
human H69 cells NXLmTm1bS3m2b4TvfIlkyqCjc4PhfS=> M{DhRlczKGh? MV;DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIOlkh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IHHsZY1ieiCkbIXlJIF{e2G7LDDJR|UxRTZibl2= MlzUNlE{PDF4N{S=
human A2780 cells Ml7XR5l1d3SxeHnjxsBie3OjeR?= NIfYR2E4OiCq MmLVR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVI4QDBiY3XscJMhd3[ncnX4dJJme3OrbnegZYxxcGF3YnX0ZVMhcW62ZXfybY4h[XO|ZYPz[YQh[XNiY3XscEB{fXK4aY\hcEBi\nSncjC3NkBpenNiYomgV3JDKGG|c3H5MEBKSzVyPU[gcm0> Mm\oNlI6PTl{NE[=
human LNCAP cells NWX5clNDS3m2b4TvfIlkyqCjc4PhfS=> MkKyO|IhcA>? MVjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDMUmNCWCClZXzsd{Bi\nSncjC3NkBpenNiYomgZYxidWG{IHLseYUh[XO|YYmsJGlEPTB;OTDuUS=> MmC0NlE{PDF4N{S=
human HOP62 cells MXTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVLncXA3T3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hUE:SNkKgZ4VtdHNiYomg[ol3\S2mb4PlJIdzd3e2aDDpcohq[mm2aX;uJIF{e2G7LDDJR|UxRTFyIH7N Mn25NlU6ODl{N{m=
human MCF7 cells NY\vbItDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4PrOWdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJG1ETjdiY3XscJMh[nliZnn2[U1ld3OnIHfyc5d1cCCrbnjpZol1cW:wIHHzd4F6NCCLQ{WwQVExKG6P MYmyOVkxQTJ5OR?=
human UACC62 cells MnviS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Ml7iS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gWWFESzZ{IHPlcIx{KGK7IH\peoUu\G:|ZTDndo94fGhiaX7obYJqfGmxbjDhd5NigSxiSVO1NF0yOCCwTR?= MlrQNlU6ODl{N{m=
human DU145 cells NHvFNI1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVzyNXN{T3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hTFVzNEWgZ4VtdHNiYomg[ol3\S2mb4PlJIdzd3e2aDDpcohq[mm2aX;uJIF{e2G7LDDJR|UxRTFyIH7N NH65cGMzPTlyOUK3PS=>
LoVo cell line MX7DfZRwfG:6aXRCpIF{e2G7 NEPHU5VEgXSxdH;4bYMheG:2ZX70bYF1cW:wIH;mJHRweG:2ZXPhckApXFBrIHL5JJRp\SClb33wc5Vv\CCrbjCobJVu[W5iY3;sc5Jm[3SjbDDjZY5k\XJiTH;Wc{Bk\WyuIHzpcoUtKEmFNUC9NVEvPiCwTR?= NHO4cm8yOjRyOEewOy=>
human lymphoblast tumor cell line RPM18402 MmTBR5l1d3SxeHnjxsBie3OjeR?= NULL[ZZtS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hdHmvcHjvZoxie3RidIXtc5Ih[2WubDDsbY5mKFKSTUG4OFAzNCCLQ{WwQVEzKG6P NVG4eIVTOTJ|OUK3OFU>
human HL60 cells NVjQdoRkTnWwY4Tpc44h[XO|YYm= MXfBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKTE[wJINmdGy|IHL5JHNTSiCvZYToc4QtKEmFNUC9NVIhdk1? M{i3clE6PTRzNEiz
human A375 cells NU\VSHJ7S3m2b4TvfIlkyqCjc4PhfS=> NH[4TWg4OiCq NVeySG5nS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTN5NTDj[YxteyCjZoTldkA4OiCqcoOgZpkh[WyjbXHyJIJtfWViYYPzZZktKEmFNUC9NVMhdk1? NG\uPWozOTN2MU[3OC=>
COR-L23/P cell MlP1R5l1d3SxeHnjxsBie3OjeR?= M{nWb2N6fG:2b4jpZ4l1gSCvZXHzeZJm\CC3c3nu[{B1cGViQ1;SMWwzOyCyYYLlcpRidCBqQ1;SMWwzOy:SKTDoeY1idiCwb36gd41idGxiY3XscEBtfW6pIHPhdoNqdm:vYTDj[YxtKGyrbnWsJGlEPTB;MUOuNkBvVQ>? NF\1N4gyOThyNkeyOC=>
human NCI-H460 cells M3TPeHBzd2yrZnXyZZRqd25iYYPzZZk> NYHuRpVlPzJiaB?= MWPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST3IOFYxKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDjc5VtfGW{IHPveY51\XJiYX7hcJl{cXNuIFnDOVA:OTZibl2= MlPKNlE4QDN|Nkm=
human MOLT4 cells MUnDfZRwfG:6aXRCpIF{e2G7 NHjPe2k4OiCq Mke4R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUW9NXDRiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2xPUBvVQ>? MljpNlQ6ODB5MkW=
human LoVo cells NWXSVW02S3m2b4TvfIlkyqCjc4PhfS=> MVq3NkBp NITZUHpEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBNd1[xIHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9NlAhdk1? MUWyNFM4OTF6Mx?=
RPM18402 tumor cell line NELYWGhRem:uaX\ldoF1cW:wIHHzd4F6 MV3Dc45k\W62cnH0bY9vKHKncYXpdoVlKHSxIHnubIljcXRiY3XscEBxem:uaX\ldoF1cW:wIHnuJHJRVTF6NECyJJR2dW:{IHPlcIwhdGmwZTygTWM2OD1{MDDuUS=> NU\5WndQOTV2OEK5Nlk>
human SN12C cells MWPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFjrT3NIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBUVjF{QzDj[YxteyCkeTDmbZZmNWSxc3Wg[5Jwf3SqIHnubIljcXSrb36gZZN{[XluIFfJOVA:OjBibl2= MWCyOVkxQTJ5OR?=
human RPMI8226 cells MXzDfZRwfG:6aXRCpIF{e2G7 MWDDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDSVG1KQDJ{NjDj[YxteyCkeTDNWHQhdWW2aH;kMEBKSzVyPUKxJI5O NX3CUoFDOTlyMUK5PVY>
HT-29 cells NHPET4hEgXSxdH;4bYPDqGG|c3H5 M3zVN2N6fG:2b4jpZ4l1gSC5YYOg[IV1\XKvaX7l[EBqdiC4aYTyc{BqdiCKVD2yPUBk\Wyuczjjc4xwdilib3[gbJVu[W5idIXtc5Ih[2WubDDsbY5meyCkeTD1d4lv\yCPVGSgZZN{[XluIFnDOVA:OjVibl2= MYq3PFU{OzNz
SK-BR-3 cells NYq2bndPS3m2b4TvfIlkyqCjc4PhfS=> M1naTGlvKF[rdILvJIN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJIJz\WG|dDDjZY5k\XJiY3XscEBtcW6nIDjTT{1DWi1|KTygTWM2OD1{NjDuUS=> NYLBN2REOTF|M{S1Olk>
HeLa cells M1TONmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXXLVoJTT3Kxd4ToJIlvcGmkaYTpc44hd2ZiSHXMZUBk\WyuczDh[pRmeiB2IHThfZMtKEeLNUC9N|Ahdk1? MojPNVc1OTh3OEK=
UACC 62 cells NHf1N4JEgXSxdH;4bYPDqGG|c3H5 NHjqNGdV\XO2ZXSgbY4hfmm2cn:g[o9zKGO7dH;0c5hq[2m2eTDh[4FqdnO2IHj1cYFvKHS3bX;yJINmdGxibHnu[UBWSUOFIE[yJEhu\Wyjbn;tZUktKEeLNUC9N|Ahdk1? M3q3WFExPzF2NUCy
human HCT116 cells MoOwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NX72dJo2T3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hUEOWMUG2JINmdGy|IHL5JIZqfmVvZH;z[UBoem:5dHigbY5pcWKrdHnvckBie3OjeTygS2k2OD1|MDDuUS=> NYPlfHJROjV7MEmyO|k>
human lung cancer cell line (H128) NYn2NWV{S3m2b4TvfIlkyqCjc4PhfS=> NInTSZFKdiCYaYTyc{BkgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBtfW6pIHPhcoNmeiClZXzsJIxqdmViKFixNlgqNCCLQ{WwQVMyKG6P NYG1PVc{OTF|M{S1Olk>
human MES-SA/Dx5 cells MUHDfZRwfG:6aXRCpIF{e2G7 MX7DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSXMuW0FxRIi1JINmdGy|IH;2[ZJmgHC{ZYPzbY5oKE2GUkGgZYZ1\XJiN{KgbJJ{KGK7IHHsZY1ieiCkbIXlJIF{e2G7LDDJR|UxRTN|IH7N M17hNFIyOzRzNke0
human A2780 cells MmX4R5l1d3SxeHnjxsBie3OjeR?= NVOzPXRbPzJiaB?= MVnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBNlc5OCClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUOzJI5O NVvqfIxbOjR7MEC3NlU>
human MDA-MB-435 cells M{TTSWN6fG:2b4jpZ:Kh[XO|YYm= NVjpOHRVPzJiaB?= MmL3R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUSzOUBk\WyuczDpcoN2[mG2ZXSg[o9zKDd{IHjyd{BjgSCPVGSgZZN{[XluIFfJOVA:OzRibl2= M1H1eFIzQDZ5MEG5
human stomach cancer cell line (MKN45) MWTDfZRwfG:6aXRCpIF{e2G7 MVfJckBXcXS{bzDjfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDzeI9u[WOqIHPhcoNmeiClZXzsJIxqdmViKF3LUlQ2MSxiSVO1NF0{QCCwTR?= Mn\zNVE{OzR3Nkm=
human KB3-1 cells MnLrR5l1d3SxeHnjxsBie3OjeR?= M{L0N2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGtDOy1zIHPlcIx{KGGodHXyJG1VXCCjc4PhfUwhUUN3ME20NEBvVQ>? NHXmbVMyQDh{OUOzOC=>
mouse P388 cells MnH3R5l1d3SxeHnjxsBie3OjeR?= MkjKR5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgVFM5QCClZXzsd{Bi\nSncjDNWHQh[XO|YYmsJGlEPTB;NEWgcm0> NYnTZox7OTh6MkmzN|Q>
A427 human lung carcinoma NU\QVoNzWHKxbHnm[ZJifGmxbjDhd5NigQ>? MXnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDt[YF{fXKnZDDh[4FqdnO2IFG0NlchcHWvYX6gcJVv\yClYYLjbY5wdWFuIFnDOVA:PDlibl2= M4\U[Vk5PzZzMUG=
human U251 cells NV;ncoM3TnWwY4Tpc44h[XO|YYm= NWGw[W84Pi1{NDDo NVjpRmxmUW6qaXLpeIlwdiCxZjD0c5BwcXOxbXXyZZNmNTFiaX6gbJVu[W5iVUK1NUBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHj5dI95cWFvaX7keYNm\CCKSV[tNYFteGijIHHjZ5VufWyjdHnvckBqdiCwdXPs[YFzKGW6dILhZ5Qh[W[2ZYKgOkB1dyB{NDDodpMh[nliaX3teY5w[myxdDDhcoFtgXOrczygSWM2OD13NDDuUS=> NHfHPWEzOjNyNU[xNi=>
human colon cancer cell line (WiDr) NUTUSGQ2S3m2b4TvfIlkyqCjc4PhfS=> NEf0ZWNKdiCYaYTyc{BkgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBkd2yxbjDjZY5k\XJiY3XscEBtcW6nIDjXbWRzMSxiSVO1NF02PiCwTR?= M3XNZ|EyOzN2NU[5
human HepG2 cells M332fGN6fG:2b4jpZ:Kh[XO|YYm= MnHUOEBl[Xm| MV7DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDI[ZBIOiClZXzsd{Bi\nSncjC0JIRigXNiYomgUXRVKGG|c3H5MEBKSzVyPU[wJI5O NE\GXI8yQDV3NEmwOi=>
human KB cells MVLDfZRwfG:6aXRCpIF{e2G7 MXK3NkBp NEW5UHNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBMSiClZXzsd{Bi\nSncjC3NkBpenNic4Xs[o9zcG:mYX3pcoUhSiClb3zvdolu\XS{aXOgZZN{[XluIFnDOVA:PjJwNTDuUS=> NE\ueYUzPTByOES1Oi=>
human HCT8 cells NY\ZcllKS3m2b4TvfIlkyqCjc4PhfS=> NVLVUm1XOyCmYYnz NVXq[pRDS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWODDj[YxteyCjZoTldkA{KGSjeYOgZpkhVVSWIHHzd4F6NCCLQ{WwQVcxKG6P M2XFUlIxOzl{NUS1
human GBM2 cells M13Qc3Bzd2yrZnXyZZRqd25iYYPzZZk> NGjCc3I4OiCq MX7BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEeETUKgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKGOnbHygeoli[mmuaYT5JIlv[3WkYYTl[EBnd3JiN{KgbJJ{KGK7IGfTWE0yKG2ndHjv[EwhUUN3ME2wMlE{KM7:TR?= MViyOlM2PTV|Mh?=
SK-MEL-2 cells MYHDfZRwfG:6aXRCpIF{e2G7 NXf0WnRIPzJiaB?= MlPJR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2suVUWOLUKgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KGGuYX3hdkBjdHWnIHHzd4F6NCCLQ{WwQVAvOTRizszN M2rNVVIyOzRzNke0
human IGROV1 cells NFOyXnJEgXSxdH;4bYPDqGG|c3H5 NFziT3I4OiCq M3L6c2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGlIWk:YMTDj[YxteyCjZoTldkA4OiCqcoOgZpkh[WyjbXHyJIJtfWViYYPzZZktKEmFNUC9NE4yPiEQvF2= MlP2NlE{PDF4N{S=
human U87 cells M{C1fXBzd2yrZnXyZZRqd25iYYPzZZk> M1G1eFQ5KGh? MkewRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCXOEegZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1yLkG2JO69VQ>? NV;qNWtOOjR6Mk[4NVg>
human HT1080 cells MUHQdo9tcW[ncnH0bY9vKGG|c3H5 NWnRfXd5PDhiaB?= Ml\hRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKVEGwPFAh[2WubIOgZZN{\XO|ZXSgZZMh\3Kxd4ToJIlvcGmkaYTpc44hcW6ldXLheIVlKG[xcjC0PEBpenNiYomgd5Vt\m:{aH;kZY1qdmViQjDhd5NigSxiSVO1NF0xNjF6IN88US=> M1;Pe|I3PDB6OEG1
human Hep3B cells NGG0Z2ZRem:uaX\ldoF1cW:wIHHzd4F6 Mor5O|IhcA>? MnrxRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKZYCzRkBk\WyuczDh[pRmeiB5MjDodpMh[nliWGTUJIF{e2G7LDDHTVUxRTBwMkKg{txO NXK1PXFHOTl5OU[5OVY>
human GBM3 cells MkHMVJJwdGmoZYLheIlwdiCjc4PhfS=> MlTsO|IhcA>? MYjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEeETUOgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKGOnbHygeoli[mmuaYT5JIlv[3WkYYTl[EBnd3JiN{KgbJJ{KGK7IGfTWE0yKG2ndHjv[EwhUUN3ME2wMlM5KM7:TR?= MXeyOlM2PTV|Mh?=
human KBVIN cells NW\vXY1tS3m2b4TvfIlkyqCjc4PhfS=> M2\HelczKGh? MoXBR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gT2JXUU5iY3XscJMh[W[2ZYKgO|IhcHK|IHL5JHNTSiCjc4PhfUwhUUN3ME2wMlQh|ryP MlvlNlU1Ozh5Nkm=
human GBM1 cells M2PnfnBzd2yrZnXyZZRqd25iYYPzZZk> MmrTO|IhcA>? M2\5W2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iR1LNNUBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkhcW6ldXLheIVlKG[xcjC3NkBpenNiYomgW3NVNTFibXX0bI9lNCCLQ{WwQVAvPDZizszN MoT2NlY{PTV3M{K=
human U937 cells NGHqRYREgXSxdH;4bYPDqGG|c3H5 M1TlTVQ5KGh? MXTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDVPVM4KGOnbHzzJIV5eHKnc4PpcocheDV|IH31eIFvfCCjZoTldkA1QCCqcoOgZpkhW1KEIHHzd4F6KO,:jDDJR|UxRTFwMTFOwG0> NX7aSlZPOTl5MUWzNVk>

... Click to View More Cell Line Experimental Data

In vivo試験 Animals inoculate s.c. with DU-145 Luc cells and then treated with Topotecan demonstrates significant tumor growth and regression as measured with calipers and luminescent imaging. The correlation coefficient is 0.75 for the control untreated group and 0.93 for the Topotecan-treated group. Similarly, tumor progression and regression are measurable using luminescent imaging for untreated and Topotecan-treated mice inoculated i.p. with MCF-7 Luc cells. [1] Topotecan elicited potent antileukemic activity in severe combined immune-deficiency (SCID) mouse models of human poor prognosis ALL. Topotecan markedly improved event-free survival of SCID mice challenged with otherwise fatal doses of humaln leukemia cells at systemic drug exposure levels. [2] Gliomas preferentially express TRAIL R2 and that treatment with Topotecan significantly up-regulates its expression. [3]
臨床試験 Topotecan plus Pazopanib has entered in a phase II clinical trial in the treatment of ovarian cancer.
特集 Topotecan is a water-soluble derivative of camptothecin.

プロトコル (参考用のみ)

細胞アッセイ:

[1]

細胞株 MCF-7 Luc and DU-145 Luc cells
濃度 0 μg/mL - 0.692 μg/mL
反応時間 96 hours
実験の流れ

Topotecan is dissolved in sterile water to a stock concentration of 1 mg/mL, diluted to 6 μg/mL in cultured medium and then serially diluted 1:4 in opaque, white tissue culture-treated microplates to a final volume of 0.1 mL/well. MCF-7 Luc and DU-145 Luc cells are resuspended in 3×104 cells/mL in DMEM with high glucose containing 10% FBS and 0.5 mg/mL Geneticin; 100 μL of cells are added in each well. Plates are incubated for 4 days at 37 °C in 95% humidity/5% CO2. After incubation, 0.05 mL of 0.1 M HEPES buffer (pH 7.9) containing 50 μg/mL D-luciferin is added to each well. After incubation at room temperature for 10 minutes, the culture microplate is measured in a microplate luminometer and a molecular light imager. Results obtained with the microplate luminometer are calculated using no inhibition control wells without exogenous drug and maximum inhibition control wells containing ATP inhibitor. Results for the molecular light imager are similarly calculated using values obtained with a 5 minutes luminescent imager.

動物実験:

[1]

動物モデル Mice with MCF-7 Luc or DU-145 Luc cells
製剤 PBS
投薬量 0.25 mg/mL
投与方法 Administered via i.p.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download Topotecan HCl SDF
分子量 457.91
化学式

C23H23N3O5.HCl

CAS No. 119413-54-6
保管 3年-20℃
2年-80℃in solvent
別名 NSC609699, Nogitecan HCl, SKFS 104864A
溶解度 (25°C) * In vitro DMSO 92 mg/mL (200.91 mM)
Water 92 mg/mL (200.91 mM)
Ethanol <1 mg/mL
In vivo Saline 30 mg/mL
* <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.
化学名 (4S)​-10-​[(dimethylamino)​methyl]​-​4-​ethyl-​4,​9-​dihydroxy-​1H-​pyrano[3',​4':6,​7]​indolizino[1,​2-​b]​quinoline-​3,​14(4H,​12H)​-​dione, hydrochloride (1:1)

文献中の引用 (6)

Frequently Asked Questions

  • Question 1
    I would like get the compound for mice intraperitoneally injection, What would you recommend to improve solubility? What could I use as solvent (%v?) that is nontoxic (unlike Methanol) and could be injected into mice intraperitoneally?

    Answer: Topotecan HCl is generally prepared by Saline for I.P. administration.

技術サポート&よくある質問(FAQ)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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