Mitoxantrone 2HCl

For research use only.

Catalog No.S2485 Synonyms: NSC-301739

19 publications

Mitoxantrone 2HCl Chemical Structure

Molecular Weight(MW): 517.4

Mitoxantrone is a type II topoisomerase inhibitor with IC50 of 2.0 μM, 0.42 mM for HepG2 and MCF-7/wt cells, respectively.

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Selleck's Mitoxantrone 2HCl has been cited by 19 publications

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Choose Selective Topoisomerase Inhibitors

Biological Activity

Description Mitoxantrone is a type II topoisomerase inhibitor with IC50 of 2.0 μM, 0.42 mM for HepG2 and MCF-7/wt cells, respectively.
Targets
Topoisomerase II [1]
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 NHPtW41EgXSxdH;4bYNqfHliYYPzZZk> NWTzXGc{PDhiaB?= MlPPR5l1d3SxeHnjJJBwfGWwY4mgdoVyfWm{ZXSgeI8hcW6qaXLpeEBNOTJzMDDj[YxtKGe{b4f0bEBjgSB3MDWgZYZ1\XJiY3XscEBlenWpIHPvcpRi[3RiZn;yJFQ5KGi{czygTWM2OD12ZT2wOUDPxE1? Mn3UPVM4OTJ2MB?=
HL60 cells NWK1bI1RS3m2b4TvfIlkcXS7IHHzd4F6 MVO0PEBp NGq3PWNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJVDZyIHPlcIx{KGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZktKEeLNUC9NE4{OyEQvF2= NV;JcJlxOTd7NkKwNlg>
MDA435/LCC6 cells MlrKVJJwdGmoZYLheIlwdiCjc4PhfS=> NIq0Z5lCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JG1FSTR|NT;MR2M3KGOnbHzzJIJ6KEWOSWPBMEBKSzVyPUCuN|Uhdk1? M4LuWlE4OTV2NUC1
A2780-cell Mn3XS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NW\iXpE4S2:wY3XueJJifGmxbjDy[ZF2cXKnZDD0c{BqdmirYnn0JGEzPzhyLXPlcIwh\3Kxd4ToJIJ6KDVyJTygTWM2OD1yLkW1JI5O NUPYWZo5QTdyM{S3NS=>
G-361 cell NFjwfWJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXnDfZRwfG:6aXOgdI91\W6leTDy[ZF2cXKnZDD0c{BqdmirYnn0JGcuOzZzIHPlcIwh\3Kxd4ToJIJ6KDVyJTygTWM2OD1yLk[1JI5O NWDIR|g1QTN5MUK0NC=>
human HL60 cells NUL1bohzWHKxbHnm[ZJifGmxbjDhd5NigQ>? NYXzbI5UPzJiaB?= NYPQS4FRSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIUFYxKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDTVmIh[XO|YYmsJGlEPTB;Mj61JI5O NYDDfIJDOjJ7NESxNlE>
human K562 cells NXW0UJdES3m2b4TvfIlkcXS7IHHzd4F6 NGDEfHc2KGSjeYO= MoKwR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gT|U3OiClZXzsd{Bi\nSncjC1JIRigXNiYomgXHRVKGG|c3H5MEBKSzVyPUKuOkBvVQ>? MnHZNVgxPzZzNEC=
CH1 cell NIH1[JNEgXSxdH;4bYNqfHliYYPzZZk> M1HFeGN6fG:2b4jpZ{Bxd3SnbnP5JJJmeXWrcnXkJJRwKGmwaHnibZQhS0hzIHPlcIwh\3Kxd4ToJIJ6KDVyJTygTWM2OD1{Lk[1JI5O M3XvO|k{PzF{NEC=
MES-SA cells NYfO[JdQWHKxbHnm[ZJifGmxbjDhd5NigQ>? MUi3NkBp Ml7HRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDNSXMuW0FiY3XscJMh[nliTWTUJIF{e2G7IHHmeIVzKDd{IHjyd{whUUN3ME2zJI5O MoH0NVY5OjR5NUG=
A549 cells NIXwOI1HfW6ldHnvckBie3OjeR?= NWW5T5llSWO2aY\peJkh[WejaX7zeEBCPTR7IHPhcoNmeiClZXzsJIxqdmVuIFnDOVA:Oy5zIH7N MXG4PVYxPTV6
LoVo cells MXvDfZRwfG:6aXPpeJkh[XO|YYm= MlW2NVQ1KGh? MVLDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDMc3ZwKGOjbnPldkBk\WyuIHzpcoUhf2G|IHTleIVzdWmwZXSgZYZ1\XJiMUS0JIhzNCCLQ{WwQVMvOyCwTR?= NVniVW9kOTV2NU[yOlg>
P388 cells MmPYVJJwdGmoZYLheIlwdiCjc4PhfS=> NH7UdlRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JHA{QDhiY3XscJMh[nliRVzJV2EtKEmFNUC9OE4{KG6P Mn7TNVcyPTR3MEW=
human Daudi cells Ml\tVJJwdGmoZYLheIlwdiCjc4PhfS=> M1m1bFczKGh? M4rjfGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iRHH1[Ikh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD13IH7N MnnMNlU6QTh3MES=
SKOV-3 cell MoXXR5l1d3SxeHnjbZR6KGG|c3H5 NHXlOWtEgXSxdH;4bYMheG:2ZX7jfUBz\XG3aYLl[EB1dyCrbnjpZol1KFONT2[tN{Bk\WyuIHfyc5d1cCB3MDWsJGlEPTB;NT6zJI5O MnPkPVM4OTJ2MB?=
OVCAR-3 cell M2PyXWZ2dmO2aX;uJIF{e2G7 NXnXV4pTSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gc5ZiemmjbjDPWmNCWi1|IHPlcIwhdGmwZYOsJGlEPTB;NT64JI5O NEjPR|Q5QTZyNUW4
human MES-SA cells NEi2UoZRem:uaX\ldoF1cW:wIHHzd4F6 NWHsO3ZFPzJiaB?= MmrsRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRWOtV2Eh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD14IH7N M{HSUVI2QTl6NUC0
PC3 cancer cell NHPvbZFEgXSxdH;4bYNqfHliYYPzZZk> M3rWZlE1PCCq NHnG[3REgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBRSzNiY3HuZ4VzKGOnbHygcIlv\SC5YYOg[IV1\XKvaX7l[EBi\nSncjCxOFQhcHJuIFnDOVA:PyCwTR?= NEXkb3AyPTR3NkK2PC=>
MXF7 breast cell MVfGeY5kfGmxbjDhd5NigQ>? NV6yWYJOSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gcYFudWG{eTDjZZJkcW6xbXGgd4Vve2m2aY\lJG1ZTjdiYoLlZZN1KGOnbHygcIlv\SxiSVO1NF05Njdibl2= NH3WNIw5QTZyNUW4
HT-29 cell MkP1R5l1d3SxeHnjbZR6KGG|c3H5 MoXYNVQ1KGh? NFXhPWNEgXSxdH;4bYMheG:2ZX7jfUBz\XG3aYLl[EB1dyCrbnjpZol1KEiWLUK5JINmdGxiZ4Lve5RpKGK7IEWwKUBi\nSncjDj[YxtKGS{dXegZ49vfGGldDDmc5IhOTR2IHjyd{whUUN3PUCuNFEh|ryP MWS5N|cyOjRy
HEK293 cells MnzzR5l1d3SxeHnjbZR6KGG|c3H5 NFvBc4E4OiCq MWnDfZRwfG:6aXPpeJkh[WejaX7zeEBJTUt{OUOgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjBzIN88US=> Mnv6NlQ3OTF6OUO=
MKN45 cells M{LlRmN6fG:2b4jpZ4l1gSCjc4PhfS=> MXSxOFQhcA>? NEfkOVlEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOU052NTDjZY5k\XJiY3XscEBtcW6nIIfhd{Bl\XSncn3pcoVlKGGodHXyJFE1PCCqcjygTWM2OD1yLkCxNkDPxE1? NFvzbYYyPTR3NkK2PC=>
MES-SA cells MVHDfZRwfG:6aXPpeJkh[XO|YYm= M1K1W|czKGh? NVrtOG5OS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUWVLWPBJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiY3XscEBxem:uaX\ldoF1cW:wIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OC5yMUKg{txO M{XuelIyPDR2MkC1
FM3 cells NFG4dm9Rem:uaX\ldoF1cW:wIHHzd4F6 M4TKbFczKGh? MmrkRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCITUOgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjBzMzFOwG0> NEXhSFkzPTl7OEWwOC=>
MCF-7 cells MVTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MY\Jcohq[mm2b4L5JIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5idIXtc5Ih[2WubDDsbY5mKE2FRj23JIJz\WG|dDDh[IVvd2OjcnPpco9u[SxiSVO1NF0xNjB{IN88US=> M{HqWVc5PTN|NEW=
human small-cell lung cancer M2roUGN6fG:2b4jpZ4l1gSCjc4PhfS=> MnrrR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gd41idGxvY3XscEBtfW6pIHPhcoNmeiBqU1PMR{ktKEmFNUC9NE4xOiEQvF2= MoXpPFI2QDh|NR?=
human HCT116 cells M{LpbGN6fG:2b4jpZ4l1gSCjc4PhfS=> MkTtO|IhcA>? M{XvUWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDFzNjDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdiCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvODJ{IN88US=> M4j1c|IyPDR2MkC1
human HCT116 cells NWTtZplLWHKxbHnm[ZJifGmxbjDhd5NigQ>? MXK3NkBp MlrERY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQ2SxNVYh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1yLkCyOUDPxE1? MYGyOVk6QDVyNB?=
NCI-H460 cells NFTq[2VEgXSxdH;4bYNqfHliYYPzZZk> NIrnV2w1QCCq MVfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDOR2kuUDR4MDDj[YxteyCjZoTldkA1QCCqcoOgZpkhemW|YYr1dolvKGS7ZTDhd5NigSxiRVO1NF0xNjB|IN88US=> MlzNNlM6QDh|NUG=
CCRF-CEM cells NHvEeWVEgXSxdH;4bYNqfHliYYPzZZk> MkTTOFghcA>? MlO5R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gR2NTTi2FRV2gZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCC4aXHibYxqfHliYX\0[ZIhPDhiaILzJIJ6KGOnbHz0bZRmei2kbIXlJIF{e2G7LDDJR|UxRTBwMEO2JO69VQ>? NYXoR4liOjJ3OEK5PVE>
HeLa cells NHfaWWpRem:uaX\ldoF1cW:wIHHzd4F6 M3j0SlczKGh? M{LLO2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSHXMZUBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTBwMES0JO69VQ>? MnrmNlU6QTh3MES=
NCI60 cells NWXPS4tRTnWwY4Tpc44h[XO|YYm= NE\teGQ1QCCq NVvlPHdWSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gUmNKPjBiY3XscJMh[W[2ZYKgOFghcHK|IHL5JHNTSiCjc4PhfUwhT0l3ME20O{45PiCwTR?= NH;hT|UyQDdzNUe4Oi=>
UACC375 cell NVvnU3Z7TnWwY4Tpc44h[XO|YYm= NWD6XmR1SW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gcYVt[W6xbXGgWWFESzN5NTDj[YxtKGyrbnWsJGlEPTB;MD6wOFgh|ryP MYK4PVYxPTV6
HT1080 cell NVL5[VRRT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NI\6bXlKdmirYnn0c5J6KGGldHn2bZR6KGGpYXnud5QhcHWvYX6geJVud3JiY3XscEBtcW6nIFjUNVA5OCxiSVO1NF0xNjB4NjFOwG0> MY[3PFU{OzR3
MES-SA/Dx5 cells Ml;PVJJwdGmoZYLheIlwdiCjc4PhfS=> NXzEdlNpPzJiaB?= MWXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2HUz3TRU9FgDViY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlA4OyEQvF2= NF3DbZYzPTl7OEWwOC=>
SF268 cells NFGxc|BRem:uaX\ldoF1cW:wIHHzd4F6 M4X4e|Q5KGh? NH30WWlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPGNlY5KGOnbHzzJIFnfGW{IES4JIhzeyxiRVO1NF0xNjN{IN88US=> MoTtNlM{QTV4NU[=
KB/HeLa cells NVnmcW1IWHKxbHnm[ZJifGmxbjDhd5NigQ>? MYW0PEBp MoCxRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCNQj;I[WxiKGOnbHzzJIFnfGW{IES4JIhzeyxiRVO1NF0xNjN4IN88US=> M3TEV|I{Ozl3NkW2
K562 cells NXnJ[|NyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MomxO|IhcA>? MojFS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gT|U3OiClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRUKG2ndHjv[EwhUUN3ME2wMlQzKM7:TR?= NWnRN5kzOTh{NUi0OFI>
MDA-MB-231 cells NWX0O|UxWHKxbHnm[ZJifGmxbjDhd5NigQ>? NWXET4VzPzJiaB?= NIT2eo1CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNiYomgW3NVNTFibXX0bI9lKGGodHXyJFczKGi{czygTWM2OD1yLkm2JO69VQ>? NEPTepcyPzN|NUG4PS=>
SF268 cells MWLDfZRwfG:6aXPpeJkh[XO|YYm= MmD5OFghcA>? NWnaWI1QS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0Z{NkigZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjl5IN88US=> M17vV|E4QTZ{MEK4
HCT116 cells NV;BdVl[S3m2b4TvfIlkcXS7IHHzd4F6 MlPCR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGNVOTF4IHPlcIx{KGK7IF3UWEBie3OjeTygTWM2OD1|Lkm2JO69VQ>? NV3m[|J5OjB7NUG1PFI>
U937 cells NVz4fVZTS3m2b4TvfIlkcXS7IHHzd4F6 M3K4[WN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHU6OzdiY3XscJMh[nliTWTUJIF{e2G7LDDJR|UxRTZwMjFOwG0> NIjzdGIyQTZzNUmwNC=>
HepG2 cells NV;DRXZ7WHKxbHnm[ZJifGmxbjDhd5NigQ>? NH7PeYM1QCCq NHfyPG9CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjldGczKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MUGuNFUh|ryP MWqyOFc6PDd2Nx?=

... 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 Cl.Cl.OCCNCCNC1=CC=C(NCCNCCO)C2=C1C(=O)C3=C(O)C=CC(=C3C2=O)O

In vivo Formulation Calculator (Clear solution)

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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

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Topoisomerase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID