Mitoxantrone 2HCl

For research use only.

Catalog No.S2485 Synonyms: NSC-301739

28 publications

Mitoxantrone 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.

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Selleck's Mitoxantrone 2HCl has been cited by 28 publications

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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 NXTZT4tOS3m2b4TvfIlkcXS7IHHzd4F6 MnLJOFghcA>? M{jxc2N6fG:2b4jpZ{Bxd3SnbnP5JJJmeXWrcnXkJJRwKGmwaHnibZQhVDF{MUCgZ4VtdCCpcn;3eIgh[nliNUClJIFnfGW{IHPlcIwh\HK3ZzDjc451[WO2IH\vdkA1QCCqcoOsJGlEPTB;NHWtNFUh|ryP NUjhWoc5QTN5MUK0NC=>
HL60 cells NYO2OJRTS3m2b4TvfIlkcXS7IHHzd4F6 NELVfVA1QCCq NUXINGxXS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEx4MDDj[YxteyCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCJSUWwQVAvOzNizszN MYixO|k3OjB{OB?=
MDA435/LCC6 cells Moi0VJJwdGmoZYLheIlwdiCjc4PhfS=> NU\tbm9sSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBOTEF2M{WvUGNEPiClZXzsd{BjgSCHTFnTRUwhUUN3ME2wMlM2KG6P MXWxO|E2PDVyNR?=
A2780-cell NF76TnZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVPDc45k\W62cnH0bY9vKHKncYXpdoVlKHSxIHnubIljcXRiQUK3PFAu[2WubDDndo94fGhiYomgOVAmNCCLQ{WwQVAvPTVibl2= NYXEXJRLQTdyM{S3NS=>
G-361 cell NEToU2dIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEi1OlNEgXSxdH;4bYMheG:2ZX7jfUBz\XG3aYLl[EB1dyCrbnjpZol1KEdvM{[xJINmdGxiZ4Lve5RpKGK7IEWwKUwhUUN3ME2wMlY2KG6P NWHiUnhoQTN5MUK0NC=>
human HL60 cells MV7Qdo9tcW[ncnH0bY9vKGG|c3H5 NXSzVZVEPzJiaB?= M3\CSGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFy2NEBk\WyuczDh[pRmeiB5MjDodpMh[nliU2LCJIF{e2G7LDDJR|UxRTJwNTDuUS=> MlnnNlI6PDRzMkG=
human K562 cells NGPtW3ZEgXSxdH;4bYNqfHliYYPzZZk> NFHUVmQ2KGSjeYO= M{WxTmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGs2PjJiY3XscJMh[W[2ZYKgOUBl[Xm|IHL5JHhVXCCjc4PhfUwhUUN3ME2yMlYhdk1? Mn3UNVgxPzZzNEC=
CH1 cell M2ThTGN6fG:2b4jpZ4l1gSCjc4PhfS=> NFr4RlJEgXSxdH;4bYMheG:2ZX7jfUBz\XG3aYLl[EB1dyCrbnjpZol1KEOKMTDj[YxtKGe{b4f0bEBjgSB3MDWsJGlEPTB;Mj62OUBvVQ>? MnPJPVM4OTJ2MB?=
MES-SA cells M2DK[XBzd2yrZnXyZZRqd25iYYPzZZk> NFzkSZc4OiCq MnPDRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDNSXMuW0FiY3XscJMh[nliTWTUJIF{e2G7IHHmeIVzKDd{IHjyd{whUUN3ME2zJI5O MV[xOlgzPDd3MR?=
A549 cells MonhSpVv[3Srb36gZZN{[Xl? M{nlPGFkfGm4aYT5JIFo[Wmwc4SgRVU1QSClYX7j[ZIh[2WubDDsbY5mNCCLQ{WwQVMvOSCwTR?= MkSxPFk3ODV3OB?=
LoVo cells NEnWNYJEgXSxdH;4bYNqfHliYYPzZZk> MorHNVQ1KGh? NYfGVmpSS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVG:YbzDjZY5k\XJiY3XscEBtcW6nIIfhd{Bl\XSncn3pcoVlKGGodHXyJFE1PCCqcjygTWM2OD1|LkOgcm0> NVnXNVd6OTV2NU[yOlg>
P388 cells NWTWTVN7WHKxbHnm[ZJifGmxbjDhd5NigQ>? M4i2fGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgVFM5QCClZXzsd{BjgSCHTFnTRUwhUUN3ME20MlMhdk1? NHzKO2oyPzF3NEWwOS=>
human Daudi cells M4f6PHBzd2yrZnXyZZRqd25iYYPzZZk> NWXTcGNnPzJiaB?= NHXtfmpCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFTheYRqKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;NTDuUS=> MWOyOVk6QDVyNB?=
SKOV-3 cell MW\DfZRwfG:6aXPpeJkh[XO|YYm= NELPV5JEgXSxdH;4bYMheG:2ZX7jfUBz\XG3aYLl[EB1dyCrbnjpZol1KFONT2[tN{Bk\WyuIHfyc5d1cCB3MDWsJGlEPTB;NT6zJI5O NX;iWFF{QTN5MUK0NC=>
OVCAR-3 cell NIrGW2lHfW6ldHnvckBie3OjeR?= NHXveYRCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDveoFzcWGwIF;WR2FTNTNiY3XscEBtcW6nczygTWM2OD13Lkigcm0> MUe4PVYxPTV6
human MES-SA cells MUjQdo9tcW[ncnH0bY9vKGG|c3H5 MXW3NkBp Ml;SRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRWOtV2Eh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD14IH7N MkPuNlU6QTh3MES=
PC3 cancer cell MYDDfZRwfG:6aXPpeJkh[XO|YYm= MV:xOFQhcA>? MmLOR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gVGM{KGOjbnPldkBk\WyuIHzpcoUhf2G|IHTleIVzdWmwZXSgZYZ1\XJiMUS0JIhzNCCLQ{WwQVchdk1? MmnqNVU1PTZ{Nki=
MXF7 breast cell NW\QT4pZTnWwY4Tpc44h[XO|YYm= NIHuVIJCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDtZY1u[XK7IHPhdoNqdm:vYTDz[Y5{cXSrdnWgUXhHPyCkcnXhd5Qh[2WubDDsbY5mNCCLQ{WwQVgvPyCwTR?= Mnj4PFk3ODV3OB?=
HT-29 cell MkXMR5l1d3SxeHnjbZR6KGG|c3H5 NV7tVWR{OTR2IHi= Mn3MR5l1d3SxeHnjJJBwfGWwY4mgdoVyfWm{ZXSgeI8hcW6qaXLpeEBJXC1{OTDj[YxtKGe{b4f0bEBjgSB3MDWgZYZ1\XJiY3XscEBlenWpIHPvcpRi[3RiZn;yJFE1PCCqcoOsJGlEPT1yLkCxJO69VQ>? NV\XSGpbQTN5MUK0NC=>
HEK293 cells MlS4R5l1d3SxeHnjbZR6KGG|c3H5 NFHDWpU4OiCq NXrFZ4oxS3m2b4TvfIlkcXS7IHHnZYlve3RiSFXLNlk{KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MD6wNUDPxE1? Mk\ENlQ3OTF6OUO=
MKN45 cells MljVR5l1d3SxeHnjbZR6KGG|c3H5 MV6xOFQhcA>? MVvDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNT241PSClYX7j[ZIh[2WubDDsbY5mKHejczDk[ZRmem2rbnXkJIFnfGW{IEG0OEBpeixiSVO1NF0xNjBzMjFOwG0> MVixOVQ2PjJ4OB?=
MES-SA cells M{PC[mN6fG:2b4jpZ4l1gSCjc4PhfS=> NH3HNnA4OiCq MkDLR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWVUNVODIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yh[2WubDDwdo9tcW[ncnH0bY9vKGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9NE4xOTJizszN MkTVNlE1PDR{MEW=
FM3 cells M1zZbHBzd2yrZnXyZZRqd25iYYPzZZk> NVrFbYl6PzJiaB?= MUnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE[PMzDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvODF|IN88US=> NUPQZ5EyOjV7OUi1NFQ>
MCF-7 cells NH;HW|BIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3rvPWlvcGmkaYTvdpkh[WO2aY\peJkh[WejaX7zeEBpfW2jbjD0eY1weiClZXzsJIxqdmViTVPGMVch[nKnYYP0JIFl\W6xY3HyZ4lvd22jLDDJR|UxRTBwMEKg{txO NWCxblhJPzh3M{O0OS=>
human small-cell lung cancer MVrDfZRwfG:6aXPpeJkh[XO|YYm= MV\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDzcYFtdC2lZXzsJIx2dmdiY3HuZ4VzKCiVQ1zDLUwhUUN3ME2wMlAzKM7:TR?= MXe4NlU5QDN3
human HCT116 cells MkPKR5l1d3SxeHnjbZR6KGG|c3H5 NXjN[GpZPzJiaB?= MlT0R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGNVOTF4IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yh[2WubDDwdo9tcW[ncnH0bY9vKGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9NE4xOjJizszN MkjRNlE1PDR{MEW=
human HCT116 cells NIrtdXJRem:uaX\ldoF1cW:wIHHzd4F6 NIrrbIU4OiCq NFTaNnFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFEyPiClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUCuNFI2KM7:TR?= M1HHSlI2QTl6NUC0
NCI-H460 cells MmPoR5l1d3SxeHnjbZR6KGG|c3H5 MkPpOFghcA>? MWHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDOR2kuUDR4MDDj[YxteyCjZoTldkA1QCCqcoOgZpkhemW|YYr1dolvKGS7ZTDhd5NigSxiRVO1NF0xNjB|IN88US=> MlTzNlM6QDh|NUG=
CCRF-CEM cells MYrDfZRwfG:6aXPpeJkh[XO|YYm= M3zj[|Q5KGh? NVvWTYF6S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hS0OURj3DSW0h[2WubIOgZZN{\XO|ZXSgZZMh[2WubDD2bYFjcWyrdImgZYZ1\XJiNEigbJJ{KGK7IHPlcIx1cXSncj3icJVmKGG|c3H5MEBKSzVyPUCuNFM3KM7:TR?= NGDrPWUzOjV6Mkm5NS=>
HeLa cells NYq4cYMxWHKxbHnm[ZJifGmxbjDhd5NigQ>? MVG3NkBp MmGzRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKZVzhJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OC5yNESg{txO MoTHNlU6QTh3MES=
NCI60 cells MXrGeY5kfGmxbjDhd5NigQ>? MVq0PEBp M3jRUGFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7DTVYxKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDTVmIh[XO|YYmsJGdKPTB;NEeuPFYhdk1? MXuxPFcyPTd6Nh?=
UACC375 cell M{LRPGZ2dmO2aX;uJIF{e2G7 M4\oTGFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIH3lcIFvd22jIGXBR2M{PzViY3XscEBtcW6nLDDJR|UxRTBwMES4JO69VQ>? MoDnPFk3ODV3OB?=
HT1080 cell MkLWS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEe2ZmpKdmirYnn0c5J6KGGldHn2bZR6KGGpYXnud5QhcHWvYX6geJVud3JiY3XscEBtcW6nIFjUNVA5OCxiSVO1NF0xNjB4NjFOwG0> MoXYO|g2OzN2NR?=
MES-SA/Dx5 cells NGPmNolRem:uaX\ldoF1cW:wIHHzd4F6 NUnmcnRpPzJiaB?= Ml7CRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRWOtV2EwTHh3IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9NE4xPzNizszN MkTyNlU6QTh3MES=
SF268 cells MmnpVJJwdGmoZYLheIlwdiCjc4PhfS=> MV20PEBp M4Hpc2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1[yOlgh[2WubIOgZYZ1\XJiNEigbJJ{NCCHQ{WwQVAvOzJizszN MlzHNlM{QTV4NU[=
KB/HeLa cells NEnM[JZRem:uaX\ldoF1cW:wIHHzd4F6 NYCzVIlbPDhiaB?= M1O1TGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS1KvTIVN[SClZXzsd{Bi\nSncjC0PEBpenNuIFXDOVA:OC5|NjFOwG0> M2fqRlI{Ozl3NkW2
K562 cells NIe0ZnJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmDPO|IhcA>? NYnnS4RbT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hUzV4MjDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSVIH3leIhw\CxiSVO1NF0xNjR{IN88US=> M4KyXFE5OjV6NESy
MDA-MB-231 cells NIjDfJpRem:uaX\ldoF1cW:wIHHzd4F6 MmfRO|IhcA>? M3;j[mFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTJ|MTDj[YxteyCkeTDXV3QuOSCvZYToc4Qh[W[2ZYKgO|IhcHK|LDDJR|UxRTBwOU[g{txO MYCxO|M{PTF6OR?=
SF268 cells NEDURXJEgXSxdH;4bYNqfHliYYPzZZk> MoX4OFghcA>? MkXjR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2YzPjhiY3XscJMh[W[2ZYKgOFghcHK|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlk4KM7:TR?= MmH0NVc6PjJyMki=
HCT116 cells NXq3SZlVS3m2b4TvfIlkcXS7IHHzd4F6 NInmSo1EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJS1RzMU[gZ4VtdHNiYomgUXRVKGG|c3H5MEBKSzVyPUOuPVYh|ryP Mmi4NlA6PTF3OEK=
U937 cells NISzU21EgXSxdH;4bYNqfHliYYPzZZk> Mo\sR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gWVk{PyClZXzsd{BjgSCPVGSgZZN{[XluIFnDOVA:Pi5{IN88US=> M3joOVE6PjF3OUCw
HepG2 cells MmDuVJJwdGmoZYLheIlwdiCjc4PhfS=> NETke|E1QCCq MYDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEincFeyJINmdGy|IHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OTFwMEWg{txO MnX3NlQ4QTR5NEe=

... 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 NSC-301739
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