Mitoxantrone 2HCl

For research use only.

Catalog No.S2485 Synonyms: NSC-301739

26 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 26 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 MlvKR5l1d3SxeHnjbZR6KGG|c3H5 MmrDOFghcA>? NHjtdZlEgXSxdH;4bYMheG:2ZX7jfUBz\XG3aYLl[EB1dyCrbnjpZol1KExzMkGwJINmdGxiZ4Lve5RpKGK7IEWwKUBi\nSncjDj[YxtKGS{dXegZ49vfGGldDDmc5IhPDhiaILzMEBKSzVyPUTlMVA2KM7:TR?= MkLyPVM4OTJ2MB?=
HL60 cells NGjjcoxEgXSxdH;4bYNqfHliYYPzZZk> M2jLXVQ5KGh? NGnEcZhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJVDZyIHPlcIx{KGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZktKEeLNUC9NE4{OyEQvF2= NFrI[HEyPzl4MkCyPC=>
MDA435/LCC6 cells NILQfmhRem:uaX\ldoF1cW:wIHHzd4F6 NX;0cHVySW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBOTEF2M{WvUGNEPiClZXzsd{BjgSCHTFnTRUwhUUN3ME2wMlM2KG6P NGrxT4wyPzF3NEWwOS=>
A2780-cell M{XXdGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NG\wc|JEd26lZX70doF1cW:wIILldZVqemWmIITvJIlvcGmkaYSgRVI4QDBvY3XscEBoem:5dHigZpkhPTBnLDDJR|UxRTBwNUWgcm0> M2jtcFk4ODN2N{G=
G-361 cell Ml\PS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFrMZpNEgXSxdH;4bYMheG:2ZX7jfUBz\XG3aYLl[EB1dyCrbnjpZol1KEdvM{[xJINmdGxiZ4Lve5RpKGK7IEWwKUwhUUN3ME2wMlY2KG6P M2PiV|k{PzF{NEC=
human HL60 cells MUXQdo9tcW[ncnH0bY9vKGG|c3H5 M{XsNVczKGh? MmHhRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKTE[wJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCVUlKgZZN{[XluIFnDOVA:Oi53IH7N MV6yNlk1PDF{MR?=
human K562 cells MWPDfZRwfG:6aXPpeJkh[XO|YYm= M{\z[|Uh\GG7cx?= M3viS2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGs2PjJiY3XscJMh[W[2ZYKgOUBl[Xm|IHL5JHhVXCCjc4PhfUwhUUN3ME2yMlYhdk1? MnPJNVgxPzZzNEC=
CH1 cell Mlr3R5l1d3SxeHnjbZR6KGG|c3H5 MlTZR5l1d3SxeHnjJJBwfGWwY4mgdoVyfWm{ZXSgeI8hcW6qaXLpeEBEUDFiY3XscEBoem:5dHigZpkhPTBnLDDJR|UxRTJwNkWgcm0> M2G5PFk{PzF{NEC=
MES-SA cells MoriVJJwdGmoZYLheIlwdiCjc4PhfS=> MoLoO|IhcA>? M{HYRWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgUWVUNVODIHPlcIx{KGK7IF3UWEBie3OjeTDh[pRmeiB5MjDodpMtKEmFNUC9N{BvVQ>? MYKxOlgzPDd3MR?=
A549 cells NWDNXmgxTnWwY4Tpc44h[XO|YYm= NGnWZXRC[3Srdnn0fUBi\2GrboP0JGE2PDliY3HuZ4VzKGOnbHygcIlv\SxiSVO1NF0{NjFibl2= NHXaXW85QTZyNUW4
LoVo cells MYPDfZRwfG:6aXPpeJkh[XO|YYm= NFiwelEyPDRiaB?= M{HLOWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGxwXm9iY3HuZ4VzKGOnbHygcIlv\SC5YYOg[IV1\XKvaX7l[EBi\nSncjCxOFQhcHJuIFnDOVA:Oy5|IH7N NYLSbVk4OTV2NU[yOlg>
P388 cells M1n1[nBzd2yrZnXyZZRqd25iYYPzZZk> MnjuRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDQN|g5KGOnbHzzJIJ6KEWOSWPBMEBKSzVyPUSuN{BvVQ>? MmL4NVcyPTR3MEW=
human Daudi cells M1HRcnBzd2yrZnXyZZRqd25iYYPzZZk> NV\IUG1EPzJiaB?= MlvERY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCGYYXkbUBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTVibl2= MXyyOVk6QDVyNB?=
SKOV-3 cell NIDmPGhEgXSxdH;4bYNqfHliYYPzZZk> Mnz5R5l1d3SxeHnjJJBwfGWwY4mgdoVyfWm{ZXSgeI8hcW6qaXLpeEBUU0:YLUOgZ4VtdCCpcn;3eIghPTBnLDDJR|UxRTVwMzDuUS=> M2\WWVk{PzF{NEC=
OVCAR-3 cell NHPyfnVHfW6ldHnvckBie3OjeR?= MnrqRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5ib4\hdolidiCRVlPBVk0{KGOnbHygcIlv\XNuIFnDOVA:PS56IH7N NV\rT2o5QDl4MEW1PC=>
human MES-SA cells NHiyZW9Rem:uaX\ldoF1cW:wIHHzd4F6 M2XpV|czKGh? MWXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2HUz3TRUBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTZibl2= Mlf2NlU6QTh3MES=
PC3 cancer cell NHPW[lREgXSxdH;4bYNqfHliYYPzZZk> MWexOFQhcA>? NIH1ZZVEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBRSzNiY3HuZ4VzKGOnbHygcIlv\SC5YYOg[IV1\XKvaX7l[EBi\nSncjCxOFQhcHJuIFnDOVA:PyCwTR?= NF6xR2syPTR3NkK2PC=>
MXF7 breast cell MYLGeY5kfGmxbjDhd5NigQ>? M{nEN2FvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIH3hcY1ienliY3HyZ4lvd22jIIPlcpNqfGm4ZTDNXGY4KGK{ZXHzeEBk\WyuIHzpcoUtKEmFNUC9PE44KG6P NFPvc4k5QTZyNUW4
HT-29 cell MU\DfZRwfG:6aXPpeJkh[XO|YYm= NWTDc21ZOTR2IHi= M1rMOWN6fG:2b4jpZ{Bxd3SnbnP5JJJmeXWrcnXkJJRwKGmwaHnibZQhUFRvMkmgZ4VtdCCpcn;3eIgh[nliNUClJIFnfGW{IHPlcIwh\HK3ZzDjc451[WO2IH\vdkAyPDRiaILzMEBKSzV;MD6wNUDPxE1? NYDyWVlwQTN5MUK0NC=>
HEK293 cells MW\DfZRwfG:6aXPpeJkh[XO|YYm= MmG4O|IhcA>? NY\LdnJuS3m2b4TvfIlkcXS7IHHnZYlve3RiSFXLNlk{KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MD6wNUDPxE1? NYPJWm1{OjR4MUG4PVM>
MKN45 cells NXH1UVJ5S3m2b4TvfIlkcXS7IHHzd4F6 MoP6NVQ1KGh? M3GydWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1MVjR3IHPhcoNmeiClZXzsJIxqdmVid3HzJIRmfGW{bXnu[YQh[W[2ZYKgNVQ1KGi{LDDJR|UxRTBwMEGyJO69VQ>? Ml7mNVU1PTZ{Nki=
MES-SA cells NV;lR|BDS3m2b4TvfIlkcXS7IHHzd4F6 M2XUV|czKGh? NXe2eJNbS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUWVLWPBJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiY3XscEBxem:uaX\ldoF1cW:wIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OC5yMUKg{txO NVPHSmppOjF2NESyNFU>
FM3 cells MonmVJJwdGmoZYLheIlwdiCjc4PhfS=> MYK3NkBp NFHUWYpCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF\NN{Bk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTBwMEGzJO69VQ>? M1nPbFI2QTl6NUC0
MCF-7 cells MlXyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUexb5NwUW6qaXLpeI9zgSCjY4Tpeol1gSCjZ3HpcpN1KGi3bXHuJJR2dW:{IHPlcIwhdGmwZTDNR2YuPyCkcnXhd5Qh[WSnbn;jZZJkcW6xbXGsJGlEPTB;MD6wNkDPxE1? NXTsc452Pzh3M{O0OS=>
human small-cell lung cancer MWXDfZRwfG:6aXPpeJkh[XO|YYm= M1nzdmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJJNu[WyuLXPlcIwhdHWwZzDjZY5k\XJiKGPDUGMqNCCLQ{WwQVAvODJizszN NE\0Unc5OjV6OEO1
human HCT116 cells NV3kcWVRS3m2b4TvfIlkcXS7IHHzd4F6 NEHZXYY4OiCq MWHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBk\WyuIIDyc4xq\mW{YYTpc44h[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlAzOiEQvF2= NFTyWHIzOTR2NEKwOS=>
human HCT116 cells Ml;MVJJwdGmoZYLheIlwdiCjc4PhfS=> MYe3NkBp M3LYd2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MD6wNlUh|ryP M{jVW|I2QTl6NUC0
NCI-H460 cells NVTMTW1sS3m2b4TvfIlkcXS7IHHzd4F6 M4fIbFQ5KGh? NUi1bWV[S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVkOLLVi0OlAh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IILld4F7fXKrbjDkfYUh[XO|YYmsJGVEPTB;MD6wN{DPxE1? MXeyN|k5QDN3MR?=
CCRF-CEM cells MX3DfZRwfG:6aXPpeJkh[XO|YYm= NULWeVRPPDhiaB?= M{foPWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGNEWkZvQ1XNJINmdGy|IHHzd4V{e2WmIHHzJINmdGxidnnhZoltcXS7IHHmeIVzKDR6IHjyd{BjgSClZXzseIl1\XJvYnz1[UBie3OjeTygTWM2OD1yLkCzOkDPxE1? NE\nb4UzOjV6Mkm5NS=>
HeLa cells NWnYUopyWHKxbHnm[ZJifGmxbjDhd5NigQ>? NV7WNpp{PzJiaB?= NFPxd4FCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjlUIEh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1yLkC0OEDPxE1? NXXlTXV3OjV7OUi1NFQ>
NCI60 cells MXnGeY5kfGmxbjDhd5NigQ>? MoSxOFghcA>? NYX6V2Y6SW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gUmNKPjBiY3XscJMh[W[2ZYKgOFghcHK|IHL5JHNTSiCjc4PhfUwhT0l3ME20O{45PiCwTR?= NG\jTo0yQDdzNUe4Oi=>
UACC375 cell NF3FW4xHfW6ldHnvckBie3OjeR?= MYXBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCvZXzhco9u[SCXQVPDN|c2KGOnbHygcIlv\SxiSVO1NF0xNjB2ODFOwG0> NY\keHhlQDl4MEW1PC=>
HT1080 cell NHjqXFFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{LkemlvcGmkaYTvdpkh[WO2aY\peJkh[WejaX7zeEBpfW2jbjD0eY1weiClZXzsJIxqdmViSGSxNFgxNCCLQ{WwQVAvODZ4IN88US=> NXvIbJlFPzh3M{O0OS=>
MES-SA/Dx5 cells NHezdZRRem:uaX\ldoF1cW:wIHHzd4F6 NHfnbIY4OiCq NHXwR2tCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3FV{1USS:GeEWgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjB5MzFOwG0> MXWyOVk6QDVyNB?=
SF268 cells NHXkN2tRem:uaX\ldoF1cW:wIHHzd4F6 NWrwVZZ2PDhiaB?= MkLWRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVRkK2PEBk\WyuczDh[pRmeiB2ODDodpMtKEWFNUC9NE4{OiEQvF2= MVuyN|M6PTZ3Nh?=
KB/HeLa cells NVzIWZd7WHKxbHnm[ZJifGmxbjDhd5NigQ>? Mke5OFghcA>? NXnn[oRGSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLRk9J\UyjIHPlcIx{KGGodHXyJFQ5KGi{czygSWM2OD1yLkO2JO69VQ>? NGfUR5ozOzN7NU[1Oi=>
K562 cells NIjrfmdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYfP[VZXPzJiaB?= NVzUNJQ{T3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hUzV4MjDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSVIH3leIhw\CxiSVO1NF0xNjR{IN88US=> MWCxPFI2QDR2Mh?=
MDA-MB-231 cells M3nEUnBzd2yrZnXyZZRqd25iYYPzZZk> Mmf5O|IhcA>? MmrlRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuOjNzIHPlcIx{KGK7IGfTWE0yKG2ndHjv[EBi\nSncjC3NkBpenNuIFnDOVA:OC57NjFOwG0> Mn6zNVc{OzVzOEm=
SF268 cells M2PyNWN6fG:2b4jpZ4l1gSCjc4PhfS=> NV\DNFVEPDhiaB?= MXfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTSlI3QCClZXzsd{Bi\nSncjC0PEBpenNiYomgV3JDKGG|c3H5MEBIUTVyPUCuPVch|ryP MXWxO|k3OjB{OB?=
HCT116 cells MkPGR5l1d3SxeHnjbZR6KGG|c3H5 NW\qXmxQS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUG2JINmdGy|IHL5JG1VXCCjc4PhfUwhUUN3ME2zMlk3KM7:TR?= NVzadZQzOjB7NUG1PFI>
U937 cells MoDxR5l1d3SxeHnjbZR6KGG|c3H5 Mm\PR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gWVk{PyClZXzsd{BjgSCPVGSgZZN{[XluIFnDOVA:Pi5{IN88US=> MYOxPVYyPTlyMB?=
HepG2 cells MV3Qdo9tcW[ncnH0bY9vKGG|c3H5 NWDMNGNwPDhiaB?= MnXBRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKZYDHNkBk\WyuczDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTFzLkC1JO69VQ>? NV;TWIpyOjR5OUS3OFc>

... 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