Mitoxantrone (NSC-301739) 2HCl

For research use only.

Catalog No.S2485

33 publications

Mitoxantrone (NSC-301739) 2HCl Chemical Structure

CAS No. 70476-82-3

Mitoxantrone 2HCl (NSC-301739) is a dihydrochloride salt of Mitoxantrone. Mitoxantrone is an inhibitor of type II topoisomerase and protein kinase C (PKC) with IC50 of 8.5 μM for PKC. Mitoxantrone inhibits cell proliferative growth of MCF-7/wt cells with IC50 of 0.42 μM. Mitoxantrone also induces apoptosis.

Selleck's Mitoxantrone (NSC-301739) 2HCl has been cited by 33 publications

Purity & Quality Control

Choose Selective Topoisomerase Inhibitors

Biological Activity

Description Mitoxantrone 2HCl (NSC-301739) is a dihydrochloride salt of Mitoxantrone. Mitoxantrone is an inhibitor of type II topoisomerase and protein kinase C (PKC) with IC50 of 8.5 μM for PKC. Mitoxantrone inhibits cell proliferative growth of MCF-7/wt cells with IC50 of 0.42 μM. Mitoxantrone also induces apoptosis.
Targets
Topoisomerase II [1]
()
PKC [7]
(Cell-free assay)
8.5 μM
In vitro

Mitoxantrone induces DNA fragmentation and the proteolytic cleavage of poly(ADP-ribose) polymerase (PARP), a marker of the activation of caspases, in all the patients studied, demonstrating that the cytotoxic effect of mitoxantrone is due to induction of apoptosis. [1] Mitoxantrone activates NFkappaB and stimulates IkappaBalpha degradation in the promyelocytic leukemia cell line HL60 but not in the variant cells, HL60/MX2 cells, which lack the beta isoform of topoisomerase II and express a truncated alpha isoform that results in an altered subcellular distribution. [2] Mitoxantrone inhibits proliferation of activated PBMCs, B lymphocytes, or antigen-specific T-cell lines (TCLs) stimulated on antigen-presenting cells (APCs) in a dose-dependent manner. Mitoxantrone induces apoptosis of PBMCs, monocytes and DCs at low concentrations, whereas higher doses causes cell lysis. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
L1210 cell MUjDfZRwfG:6aXPpeJkh[XO|YYm= Mn\MOFghcA>? NI\i[4ZEgXSxdH;4bYMheG:2ZX7jfUBz\XG3aYLl[EB1dyCrbnjpZol1KExzMkGwJINmdGxiZ4Lve5RpKGK7IEWwKUBi\nSncjDj[YxtKGS{dXegZ49vfGGldDDmc5IhPDhiaILzMEBKSzVyPUTlMVA2KM7:TR?= M2HzbVk{PzF{NEC=
HL60 cells M2r4VGN6fG:2b4jpZ4l1gSCjc4PhfS=> M3LnVFQ5KGh? M{j6dWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhNPjBiY3XscJMh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhT0l3ME2wMlM{KM7:TR?= NELL[44yPzl4MkCyPC=>
MDA435/LCC6 cells NV\rU5BzWHKxbHnm[ZJifGmxbjDhd5NigQ>? M3fpS2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgUWRCPDN3L1zDR|Yh[2WubIOgZpkhTUyLU1GsJGlEPTB;MD6zOUBvVQ>? MUexO|E2PDVyNR?=
A2780-cell NXnMbnNST3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXTDc45k\W62cnH0bY9vKHKncYXpdoVlKHSxIHnubIljcXRiQUK3PFAu[2WubDDndo94fGhiYomgOVAmNCCLQ{WwQVAvPTVibl2= M13Bclk4ODN2N{G=
G-361 cell MoHhS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MoW0R5l1d3SxeHnjJJBwfGWwY4mgdoVyfWm{ZXSgeI8hcW6qaXLpeEBINTN4MTDj[YxtKGe{b4f0bEBjgSB3MDWsJGlEPTB;MD62OUBvVQ>? MWe5N|cyOjRy
human HL60 cells NEOxWmlRem:uaX\ldoF1cW:wIHHzd4F6 M4\GdVczKGh? M1fhWWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFy2NEBk\WyuczDh[pRmeiB5MjDodpMh[nliU2LCJIF{e2G7LDDJR|UxRTJwNTDuUS=> NUf6S2Q6OjJ7NESxNlE>
human K562 cells MWTDfZRwfG:6aXPpeJkh[XO|YYm= M13kdFUh\GG7cx?= NVTEVooxS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUzV4MjDj[YxteyCjZoTldkA2KGSjeYOgZpkhYFSWIHHzd4F6NCCLQ{WwQVIvPiCwTR?= MVOxPFA4PjF2MB?=
CH1 cell M1zlRWN6fG:2b4jpZ4l1gSCjc4PhfS=> NXn2e5lsS3m2b4TvfIlkKHCxdHXuZ5khemWzdXny[YQhfG9iaX7obYJqfCCFSEGgZ4VtdCCpcn;3eIgh[nliNUClMEBKSzVyPUKuOlUhdk1? M2PvRlk{PzF{NEC=
MES-SA cells NWLlPYZqWHKxbHnm[ZJifGmxbjDhd5NigQ>? MWW3NkBp M4HyNWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgUWVUNVODIHPlcIx{KGK7IF3UWEBie3OjeTDh[pRmeiB5MjDodpMtKEmFNUC9N{BvVQ>? M{LtUFE3QDJ2N{Wx
A549 cells Mme2SpVv[3Srb36gZZN{[Xl? NXnPU|h1SWO2aY\peJkh[WejaX7zeEBCPTR7IHPhcoNmeiClZXzsJIxqdmVuIFnDOVA:Oy5zIH7N MmT6PFk3ODV3OB?=
LoVo cells Mo\4R5l1d3SxeHnjbZR6KGG|c3H5 Mm\oNVQ1KGh? NXfwSFhRS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVG:YbzDjZY5k\XJiY3XscEBtcW6nIIfhd{Bl\XSncn3pcoVlKGGodHXyJFE1PCCqcjygTWM2OD1|LkOgcm0> NX3Nc3p3OTV2NU[yOlg>
P388 cells M1\tSnBzd2yrZnXyZZRqd25iYYPzZZk> NUfwZZhySW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBROzh6IHPlcIx{KGK7IFXMTXNCNCCLQ{WwQVQvOyCwTR?= Ml3ZNVcyPTR3MEW=
human Daudi cells NHvQO4ZRem:uaX\ldoF1cW:wIHHzd4F6 MYW3NkBp NYr6Z5A4SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDEZZVlcSClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUWgcm0> NYPiNYJzOjV7OUi1NFQ>
SKOV-3 cell NHHZdIdEgXSxdH;4bYNqfHliYYPzZZk> MnfoR5l1d3SxeHnjJJBwfGWwY4mgdoVyfWm{ZXSgeI8hcW6qaXLpeEBUU0:YLUOgZ4VtdCCpcn;3eIghPTBnLDDJR|UxRTVwMzDuUS=> MkHlPVM4OTJ2MB?=
OVCAR-3 cell NXPDWopFTnWwY4Tpc44h[XO|YYm= MWPBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCxdnHybYFvKE:YQ1HSMVMh[2WubDDsbY5meyxiSVO1NF02Njhibl2= MnvTPFk3ODV3OB?=
human MES-SA cells NULVcpZ{WHKxbHnm[ZJifGmxbjDhd5NigQ>? NIrHNIE4OiCq MWPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2HUz3TRUBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTZibl2= MVmyOVk6QDVyNB?=
PC3 cancer cell NHqwbHdEgXSxdH;4bYNqfHliYYPzZZk> NIHXT4YyPDRiaB?= MVPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDQR|Mh[2GwY3XyJINmdGxibHnu[UB4[XNiZHX0[ZJucW6nZDDh[pRmeiBzNESgbJItKEmFNUC9O{BvVQ>? M3vLc|E2PDV4Mk[4
MXF7 breast cell MV7GeY5kfGmxbjDhd5NigQ>? NW\jZWNOSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gcYFudWG{eTDjZZJkcW6xbXGgd4Vve2m2aY\lJG1ZTjdiYoLlZZN1KGOnbHygcIlv\SxiSVO1NF05Njdibl2= MYG4PVYxPTV6
HT-29 cell NFS4eWREgXSxdH;4bYNqfHliYYPzZZk> NGLseW8yPDRiaB?= NWTwcZBKS3m2b4TvfIlkKHCxdHXuZ5khemWzdXny[YQhfG9iaX7obYJqfCCKVD2yPUBk\WyuIHfyc5d1cCCkeTC1NEUh[W[2ZYKgZ4VtdCCmcoXnJINwdnSjY4Sg[o9zKDF2NDDodpMtKEmFNU2wMlAyKM7:TR?= MYe5N|cyOjRy
HEK293 cells NVuyT|gzS3m2b4TvfIlkcXS7IHHzd4F6 MXi3NkBp Ml[2R5l1d3SxeHnjbZR6KGGpYXnud5QhUEWNMkmzJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OC5yMTFOwG0> NG\scWgzPDZzMUi5Ny=>
MKN45 cells M16wNmN6fG:2b4jpZ4l1gSCjc4PhfS=> NVjwdoZoOTR2IHi= NV:4WItPS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUuQNEWgZ4Fv[2W{IHPlcIwhdGmwZTD3ZZMh\GW2ZYLtbY5m\CCjZoTldkAyPDRiaIKsJGlEPTB;MD6wNVIh|ryP M{jNRlE2PDV4Mk[4
MES-SA cells MkHPR5l1d3SxeHnjbZR6KGG|c3H5 MWO3NkBp NGrnNJBEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOTVNvU1GgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25iYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjBzMjFOwG0> NGjkXGUzOTR2NEKwOS=>
FM3 cells NFHsbWJRem:uaX\ldoF1cW:wIHHzd4F6 NH:4ZWQ4OiCq MVXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE[PMzDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvODF|IN88US=> NFzFN20zPTl7OEWwOC=>
MCF-7 cells NGjncmhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mn[4TY5pcWKrdH;yfUBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIIT1cY9zKGOnbHygcIlv\SCPQ1[tO{BjemWjc4SgZYRmdm:lYYLjbY5wdWFuIFnDOVA:OC5yMjFOwG0> MmjWO|g2OzN2NR?=
human small-cell lung cancer NGj4ToJEgXSxdH;4bYNqfHliYYPzZZk> NFXGR2FEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckB{dWGubD3j[YxtKGy3bnegZ4Fv[2W{IDjTR2xEMSxiSVO1NF0xNjB{IN88US=> M4nLXFgzPTh6M{W=
human HCT116 cells MYfDfZRwfG:6aXPpeJkh[XO|YYm= MVO3NkBp M4rEPGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDFzNjDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdiCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvODJ{IN88US=> NYnSbHJHOjF2NESyNFU>
human HCT116 cells MlfuVJJwdGmoZYLheIlwdiCjc4PhfS=> MkT2O|IhcA>? MmnZRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQ2SxNVYh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1yLkCyOUDPxE1? M1rtR|I2QTl6NUC0
NCI-H460 cells NFT2d2FEgXSxdH;4bYNqfHliYYPzZZk> NW\oSIQ6PDhiaB?= M3XJTGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG5EUS2KNE[wJINmdGy|IHHmeIVzKDR6IHjyd{BjgSC{ZYPhfpVzcW5iZInlJIF{e2G7LDDFR|UxRTBwMEOg{txO NUXZ[5JsOjN7OEizOVE>
CCRF-CEM cells MnrCR5l1d3SxeHnjbZR6KGG|c3H5 Mo[2OFghcA>? M2W4Z2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGNEWkZvQ1XNJINmdGy|IHHzd4V{e2WmIHHzJINmdGxidnnhZoltcXS7IHHmeIVzKDR6IHjyd{BjgSClZXzseIl1\XJvYnz1[UBie3OjeTygTWM2OD1yLkCzOkDPxE1? NYW1cW5qOjJ3OEK5PVE>
HeLa cells MVTQdo9tcW[ncnH0bY9vKGG|c3H5 MWK3NkBp MWTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEinTHGgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjB2NDFOwG0> NYfPWlhEOjV7OUi1NFQ>
NCI60 cells NWO5bIFSTnWwY4Tpc44h[XO|YYm= M1HaVlQ5KGh? NGCz[XBCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2k3OCClZXzsd{Bi\nSncjC0PEBpenNiYomgV3JDKGG|c3H5MEBIUTVyPUS3Mlg3KG6P MVuxPFcyPTd6Nh?=
UACC375 cell NYLOeGNXTnWwY4Tpc44h[XO|YYm= MlvSRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5ibXXsZY5wdWFiVVHDR|M4PSClZXzsJIxqdmVuIFnDOVA:OC5yNEig{txO MUC4PVYxPTV6
HT1080 cell NXLxV5V2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1;RUWlvcGmkaYTvdpkh[WO2aY\peJkh[WejaX7zeEBpfW2jbjD0eY1weiClZXzsJIxqdmViSGSxNFgxNCCLQ{WwQVAvODZ4IN88US=> MkK1O|g2OzN2NR?=
MES-SA/Dx5 cells MkjaVJJwdGmoZYLheIlwdiCjc4PhfS=> M2PkNFczKGh? NHnIUmpCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3FV{1USS:GeEWgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjB5MzFOwG0> MkPnNlU6QTh3MES=
SF268 cells M4HWc3Bzd2yrZnXyZZRqd25iYYPzZZk> NVvkdI5QPDhiaB?= M2n3TGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1[yOlgh[2WubIOgZYZ1\XJiNEigbJJ{NCCHQ{WwQVAvOzJizszN M2m1VlI{Ozl3NkW2
KB/HeLa cells M2PKNXBzd2yrZnXyZZRqd25iYYPzZZk> M1fPeVQ5KGh? M1L0VmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS1KvTIVN[SClZXzsd{Bi\nSncjC0PEBpenNuIFXDOVA:OC5|NjFOwG0> MkfBNlM{QTV4NU[=
K562 cells NY\JTXZQT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4C5N|czKGh? NVrmNFNPT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hUzV4MjDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSVIH3leIhw\CxiSVO1NF0xNjR{IN88US=> MVuxPFI2QDR2Mh?=
MDA-MB-231 cells NEfZeoRRem:uaX\ldoF1cW:wIHHzd4F6 MlL6O|IhcA>? NGKxR4ZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNiYomgW3NVNTFibXX0bI9lKGGodHXyJFczKGi{czygTWM2OD1yLkm2JO69VQ>? MknnNVc{OzVzOEm=
SF268 cells MYrDfZRwfG:6aXPpeJkh[XO|YYm= MnG1OFghcA>? NHfSTGpEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUTjJ4ODDj[YxteyCjZoTldkA1QCCqcoOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvQTdizszN M2PLc|E4QTZ{MEK4
HCT116 cells NV\pUHhZS3m2b4TvfIlkcXS7IHHzd4F6 NWTWO49GS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUG2JINmdGy|IHL5JG1VXCCjc4PhfUwhUUN3ME2zMlk3KM7:TR?= MVqyNFk2OTV6Mh?=
U937 cells NVrNZ49qS3m2b4TvfIlkcXS7IHHzd4F6 M3L6VmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHU6OzdiY3XscJMh[nliTWTUJIF{e2G7LDDJR|UxRTZwMjFOwG0> Mly2NVk3OTV7MEC=
HepG2 cells NXzSXWlJWHKxbHnm[ZJifGmxbjDhd5NigQ>? Ml;TOFghcA>? NVjBdHRqSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDI[ZBIOiClZXzsd{Bi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUGxMlA2KM7:TR?= MoSwNlQ4QTR5NEe=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-ROS1 / ROS1 / p-STAT3 / STAT3 / p-AKT / AKT / p-ERK / ERK; 

PubMed: 30108778     


Mechanism of action of mitoxantrone in HCC78 cells. Immunoblot analysis of p-ROS1, ROS1, p-STAT3, STAT3, p-AKT, AKT, p-ERK, ERK and GAPDH in HCC78 cells, cells were harvested after treatment with mitoxantrone for 48 h.

30108778
Growth inhibition assay
Cell number; 

PubMed: 24349321     


LNCaP 104-S, 104- R1, 104-R2, PC-3, and DU-145 cells were treated with increasing concentrations of mitoxantrone for 72 hrs. Relative cell number of LNCaP cells was determined by Hoechst dye 33258-based 96-well proliferation assay. Cell numbers were normalized to control (dimethylsulfoxide) of each cell line. Triple asterisks (***) represent statistically significant difference p < 0.001between the treated group and the control group.

24349321
In vivo

Mitoxantrone transiently decreases the growth rate of HID xenografts in mice but does not affect that of PAC120 xenografts. [4] Mitoxantrone results in the severity of the cardiac lesions and the nephropathy and the intestinal toxicity in spontaneously hypertensive rats. Mitoxantrone and iron(III) form a strong 2:1 complex, in which mitoxantrone may be acting as a tridentate ligand. [5]

Protocol

Solubility (25°C)

In vitro DMSO 89 mg/mL (172.01 mM)
Water 89 mg/mL (172.01 mM)
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
Saline
For best results, use promptly after mixing.
30 mg/mL

* 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 517.4
Formula

C22H29ClN4O6.2HCl

CAS No. 70476-82-3
Storage powder
in solvent
Synonyms N/A
Smiles C1=CC(=C2C(=C1NCCNCCO)C(=O)C3=C(C=CC(=C3C2=O)O)O)NCCNCCO.Cl.Cl

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04330820 Recruiting Drug: Venetoclax Oral Tablet Relapsed Adult AML Technische Universität Dresden|AbbVie April 6 2020 Phase 1|Phase 2
NCT02131688 Unknown status Drug: Mitoxantrone Hydrochloride Liposome Malignant Lymphoma CSPC ZhongQi Pharmaceutical Technology Co. Ltd. May 2013 Phase 1
NCT01701375 Terminated Drug: PD 0332991 Relapsed Acute Leukemia|Refractory Acute Leukemia|High-Risk Myelodysplasia Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins|The Leukemia and Lymphoma Society|Pfizer September 2012 Phase 1

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Topoisomerase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID