Doxorubicin (Adriamycin) 化学構造
分子量: 579.98

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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
  • Combination Therapy
    併用療法

製品の説明

生物活性

製品説明 Doxorubicin (Adriamycin) は、DNAトポイソメラーゼIIを妨げて、DNAの損傷とアポトーシスを誘発する抗生エージェントです。
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IC50
In vitro試験 Doxorubicin, an antibiotic anthracycline, is commonly considered to exert its anti-tumor activity at two fundamental levels, altering DNA and producing free radicals to trigger apoptosis of cancer cells through DNA damage. Doxorubicin can block the synthesis of DNA by intercalating into the DNA strand, and inhibits DNA topoisomerase II (TOP2). Doxorubicin is most effective when cells are rapidly proliferating and expressing high levels of TOP2. Additionally, Doxorubicin can trigger apoptosis by producing ceramide (which prompts apoptosis by activating p53 or other downstream pathways such as JNK), the degradation of Akt by serine threonine proteases, the mitochondrial release of cytochrome c, increased FasL (death receptor Fas/CD95 ligand) mRNA production, and a greater production of free radicals. [2] Pre-treatment with GSNO (nitrosoglutathione) suppresses the resistance in the doxorubicin-resistant breast cancer cell line MCF7/Dx, accompanied by enhanced protein glutathionylation and accumulation of doxorubicin in the nucleus. [3] Doxorubicin induced G2/M checkpoint arrest are attributed to elevated cyclin G2 (CycG2) expression and phospho-modification of proteins in the ataxia telangiectasia mutated (ATM) and ATM and Rad3-related (ATR) signaling pathways. [5] Doxorubicin inhibits AMP-activated protein kinase (AMPK), resulting in SIRT1 dysfunction, p53 accumulation, and increased cell death in mouse embryonic fibroblasts (MEFs) and cardiomyocytes, which can be further sensitized by pre-inhibition of AMPK. [6] Doxorubicin elicits a marked heat shock response, and that either inhibition or silencing of heat shock proteins enhance the Doxorubicin apoptotic effect in neuroblastoma cells. Nanomolar Doxorubicin treatment of neuroblastoma cells causes dose-dependent over-ubiquitination of a specific set of proteins in the absence of measurable inhibition of proteasome, and loss of activity of ubiquitinated enzymes such as lactate dehydrogenase and α-enolase, the protein ubiquination patterns of which is similar to those with proteasome inhibitor Bortezomib, indicating that Doxorubicin may also exert its effect by damaging proteins. [8]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
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CAL-39 NUPGNYhKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWjWRYx2UUN3ME25PE4zPCCwTR?= NGjKTnJUSU6JRWK=
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MES-SA NH;GV4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3HbYRVUUN3ME25PU42OyCwTR?= NX3sTotPW0GQR1XS
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NCI-H596 NVPRfVlET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnjR3JOUUN3ME2xNFgvODFibl2= NV:2SmtjW0GQR1XS
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NCI-H2170 NES2empIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXS2bXVRUUN3ME2xNFkvQTJibl2= MVrTRW5ITVJ?
ARH-77 NHX4R2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\qfocxUUN3ME2xNFkvQTlibl2= MmH6V2FPT0WU
BOKU NILSPWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmDpTWM2OD1zMUCuPFchdk1? M3LyPHNCVkeHUh?=
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TE-10 NHnhd4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zCc2lEPTB;MUGyMlY5KG6P MlfrV2FPT0WU
MZ7-mel MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;SU|BKSzVyPUGxNk45PCCwTR?= MUTTRW5ITVJ?
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HCC1937 NIrlcZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXCV5NKSzVyPUGxOU45PCCwTR?= M3jLXXNCVkeHUh?=
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OVCAR-5 NW\jSHQzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPKSnhKSzVyPUGxOk45OSCwTR?= MnvDV2FPT0WU
SW837 NV7ndGJ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjBTWM2OD1zMUeuPVUhdk1? MYTTRW5ITVJ?
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LB647-SCLC MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3:4bmlEPTB;MUKzMlM2KG6P NUXmc3dxW0GQR1XS
NCI-H1703 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlToTWM2OD1zMk[uOFIhdk1? MVrTRW5ITVJ?
KURAMOCHI MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HvPWlEPTB;MUK2Mlc3KG6P MX\TRW5ITVJ?
ATN-1 M3rWPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DjNGlEPTB;MUK3Mlchdk1? MXPTRW5ITVJ?
SK-CO-1 Mki3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1ntcmlEPTB;MUK5MlIyKG6P NGnKWlNUSU6JRWK=
RPMI-7951 NXi0OHhFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTF|MD6xOEBvVQ>? NWS1dWhzW0GQR1XS
NCI-H1648 MlTxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7QTWM2OD1zM{GuPVQhdk1? MWXTRW5ITVJ?
NCI-H64 M4T0OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrkV2hKSzVyPUGzNk43PSCwTR?= M4\HPXNCVkeHUh?=
HT-3 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlSwTWM2OD1zM{OuNFQhdk1? MoDhV2FPT0WU
NCI-H1770 MnjiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPERlVKSzVyPUGzN{4zOSCwTR?= NYG3RXVSW0GQR1XS
NB13 MlPES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7GTWM2OD1zM{SuOVUhdk1? NUjGSnRGW0GQR1XS
NCI-H747 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTF|NT6wNkBvVQ>? M4PLb3NCVkeHUh?=
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JiyoyeP-2003 NEfrdlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDMbGRmUUN3ME2xN|cvQCCwTR?= MY\TRW5ITVJ?
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NCI-H748 Mmr0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTF2Nz6zNUBvVQ>? NHnQZ4FUSU6JRWK=
SK-MEL-3 M3G4O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHDeoFjUUN3ME2xOFcvPjFibl2= M4LnUXNCVkeHUh?=
SNB75 NEL4TW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\LWGlEPTB;MUS4MlY2KG6P NUnKOldMW0GQR1XS
BB65-RCC NI\OUoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULmeWx[UUN3ME2xOFkvOzFibl2= M2TqUXNCVkeHUh?=
NCI-H1355 Mlf6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHXNZBKSzVyPUG1Nk4zPCCwTR?= NH7ub5BUSU6JRWK=
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WSU-NHL MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4nHWWlEPTB;MUW0MlU5KG6P MnzNV2FPT0WU
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SBC-1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fHfGlEPTB;MUW2MlQhdk1? M2PHSnNCVkeHUh?=
OVCAR-4 M{PBZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnqxTWM2OD1zNU[uO|ghdk1? NGj4eFBUSU6JRWK=
NCI-H2347 NHq5XXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHkTWM2OD1zNUiuN|Qhdk1? MYPTRW5ITVJ?
CAMA-1 NGjpdHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIi1VGlKSzVyPUG1PU4{OyCwTR?= NIXC[plUSU6JRWK=
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NCI-H2052 NXHZc5cyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zmRmlEPTB;MU[wMlQ4KG6P MX7TRW5ITVJ?
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T98G Ml\aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvPTWM2OD1{LkiwOFAyKM7:TR?= MnO4V2FPT0WU
DMS-79 NIfIRmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljXTWM2OD1{LkmwPVg5KM7:TR?= MUHTRW5ITVJ?
SNU-475 MoDNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTJwOUK1O|Ih|ryP MnLDV2FPT0WU
COLO-792 NIjjOGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzUT3FKSzVyPUOuNFI5PyEQvF2= MoLuV2FPT0WU
YAPC NG\pVpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1P2SmlEPTB;Mz6zNlg{OiEQvF2= MVrTRW5ITVJ?
UACC-812 M2SyNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTNwM{O3N|gh|ryP NVHkT3BXW0GQR1XS
Mewo NIn6[XRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHmTWM2OD1|LkS2NFg3KM7:TR?= NVLnTXFQW0GQR1XS
COLO-824 Ml\GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\MWZlKSzVyPUOuOVc{PzhizszN MVnTRW5ITVJ?
SCC-9 NFWyTXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPWTWM2OD1|LkmxN|A6KM7:TR?= MXHTRW5ITVJ?
CP50-MEL-B NV\wc21uT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTNwOUi3NFMh|ryP MXzTRW5ITVJ?
NCI-H345 NFjLSnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTRwMEGxO|Qh|ryP Ml3uV2FPT0WU
COR-L88 NITKSZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXz1TY5bUUN3ME20MlM6PThizszN MorPV2FPT0WU
RCM-1 NIrWVmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF:2[FZKSzVyPUSuOFkzPzJizszN NEL2bYxUSU6JRWK=
JVM-3 NW\CNFA6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTRwNkC2NVgh|ryP Mlq1V2FPT0WU
ECC4 M{fOUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTRwN{[1OFEh|ryP M16yOHNCVkeHUh?=
MDA-MB-453 NVXuO3VUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXadGtkUUN3ME20Mlg2OTN2IN88US=> MkPjV2FPT0WU
SK-N-FI MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfKTWM2OD13LkKyPFc4KM7:TR?= NHy1WI5USU6JRWK=
D-502MG M1f2[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnPdXdKSzVyPUWuNlQzPjJizszN NH\6WVlUSU6JRWK=
NCI-H2227 M{fhT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnJZmlKSzVyPUWuN|YzOzFizszN MX3TRW5ITVJ?
DMS-53 NEnMVGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIqzXo5KSzVyPU[uNVcyODZizszN NFvuZ4ZUSU6JRWK=
LB771-HNC NF;tWmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTZwNE[4NFYh|ryP NYK0cm15W0GQR1XS
BB49-HNC MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPpU3FKSzVyPUeuOFE4QTFizszN Mn:5V2FPT0WU
MDA-MB-415 MnzkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHzTWM2OD15LkW3N|A{KM7:TR?= MkXTV2FPT0WU
TALL-1 MmLNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljqTWM2OD15Lkm2PFgh|ryP NY\4OZJ1W0GQR1XS
HCC1395 M{LyTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRThwMUWxNlIh|ryP NF\DdoJUSU6JRWK=
EFE-184 NWHiPZJ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4nBcmlEPTB;OD6zO|IyPiEQvF2= M4LsPHNCVkeHUh?=
EC-GI-10 M4\qe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRThwNki2PFYh|ryP NV;afGpLW0GQR1XS
TT NIjDPVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFP0ZZpKSzVyPUmuNFY6PjZizszN NEL3W2hUSU6JRWK=
U-2-OS MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TMb2lEPTB;OT64NVM6OyEQvF2= Mk\mV2FPT0WU
SHP-77 M3HXVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{X6dWlEPTB;OT65NFI6KM7:TR?= NHXS[4NUSU6JRWK=
HCC1143 M4WwRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTFyLkS3PVch|ryP MW\TRW5ITVJ?
A498 NIW5WFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXqTWM2OD1zOD6yPVc3KM7:TR?= MnfaV2FPT0WU
LS-513 NInZe4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUi5XXl3UUN3ME2xPE43ODl|IN88US=> NWHZW214W0GQR1XS
K052 Mnm2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYj0Uo9lUUN3ME2yNU41PDF6IN88US=> M1y5S3NCVkeHUh?=
SiHa M{DIeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XLXWlEPTB;MkOuN|M4OSEQvF2= MXPTRW5ITVJ?
RCC10RGB NGfiW4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7yRZRKSzVyPUOwMlA3OTFizszN NGnidVNUSU6JRWK=
NCI-SNU-16 M3LpeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXNTWM2OD1|MT6xPFM3KM7:TR?= MWDTRW5ITVJ?
SNU-C1 NXmxZ4JrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnv2TWM2OD1|Mj60NVc2KM7:TR?= Mm[yV2FPT0WU
C32 NULvU44xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTN{Lki3NkDPxE1? MX3TRW5ITVJ?
SW684 M3S4[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDmTWM2OD1|ND6xOVYyKM7:TR?= MX;TRW5ITVJ?
SK-MEL-28 MoGwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPMTWM2OD1|NT61N|c4KM7:TR?= NYfRZW95W0GQR1XS
SK-MEL-1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mkf3TWM2OD1|Nj63OVQ4KM7:TR?= MVrTRW5ITVJ?
NCI-H720 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2WyVmlEPTB;NEGuPVczPiEQvF2= Mn\0V2FPT0WU
P31-FUJ NUnWdoltT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTR2LkOyPFQh|ryP NYjHVlVVW0GQR1XS
NCI-H524 NXHicYpsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPhTVl1UUN3ME20PE45OjR6IN88US=> NULFbZE2W0GQR1XS

... Click to View More Cell Line Experimental Data

In vivo試験 In vivo, Doxorubicin in combination with adenoviral MnSOD (AdMnSOD) plus 1,3-bis(2-chloroethyl)-1-nitrosourea (BCNU) has the greatest effect in decreasing the volumes of MB231 tumors and prolonging survival of mice. [1] Although its use is limited by the chronic and acute toxic side effects it produces, Doxorubicin is essential in treating breast and oesophageal carcinomas, solid tumours in childhood, osteosarcomas, Kaposi's sarcoma, soft tissue sarcomas, and Hodgkin and non-Hodgkin lymphomas. [2]
臨床試験 A Phase III study of Doxorubicin alone vs. Doxorubicin in combination with TH-302 in subjects with locally advanced unresectable or metastatic soft tissue sarcoma is currently ongoing.
特集

プロトコル (参考用のみ)

動物実験: [1]

動物モデル Female athymic nude mice injected s.c. with MB231 cells
製剤 Dissolved in DMSO, and diluted in saline
投薬量 3 mg/kg/day
投与方法 Delivered intratumorly

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 Doxorubicin (Adriamycin) SDF
分子量 579.98
化学式

C27H29NO11.HCl

CAS No. 25316-40-9
保管 3年-20℃
2年-80℃in solvent
別名 NSC 123127
溶解度 (25°C) * In vitro DMSO 100 mg/mL warming (172.41 mM)
Water 20 mg/mL (34.48 mM)
Ethanol <1 mg/mL
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.
化学名 (8S,10S)-10-((2R,4S,5S,6S)-4-amino-5-hydroxy-6-methyl-tetrahydro-2H-pyran-2-yloxy)-6,8,11-trihydroxy-8-(2-hydroxyacetyl)-1-methoxy-7,8,9,10-tetrahydrotetracene-5,12-dione hydrochloride

文献中の引用 (28)

Frequently Asked Questions

  • Question 1
    Why the IC50 of the compound varied over time in our measurement?

    Answer: Sometimes the IC50 value might vary between different batch of compounds due to the slight differences in purity. If different IC50 was seen in the same batch of compound, the problem may lies in the process of dissolvement. Make sure that you see no particles and the solution is clear with your stock solution.

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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