Mitoxantrone (NSC-301739) 2HCl

Catalog No.S2485

For research use only.

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.

Mitoxantrone (NSC-301739) 2HCl Chemical Structure

CAS No. 70476-82-3

Selleck's Mitoxantrone (NSC-301739) 2HCl has been cited by 39 publications

Purity & Quality Control

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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 NHjiVZFEgXSxdH;4bYNqfHliYYPzZZk> MYi0PEBp NIOye4dEgXSxdH;4bYMheG:2ZX7jfUBz\XG3aYLl[EB1dyCrbnjpZol1KExzMkGwJINmdGxiZ4Lve5RpKGK7IEWwKUBi\nSncjDj[YxtKGS{dXegZ49vfGGldDDmc5IhPDhiaILzMEBKSzVyPUTlMVA2KM7:TR?= MnK3PVM4OTJ2MB?=
HL60 cells M1nhUWN6fG:2b4jpZ4l1gSCjc4PhfS=> NYLObYtEPDhiaB?= Mlq0R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGw3OCClZXzsd{Bi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBIUTVyPUCuN|Mh|ryP NXHRdGZHOTd7NkKwNlg>
MDA435/LCC6 cells MVXQdo9tcW[ncnH0bY9vKGG|c3H5 MmntRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDNSGE1OzVxTFPDOkBk\WyuczDifUBGVEmVQTygTWM2OD1yLkO1JI5O M3zLVFE4OTV2NUC1
A2780-cell Mn;HS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mki2R49v[2WwdILheIlwdiC{ZYH1bZJm\CC2bzDpcohq[mm2IFGyO|gxNWOnbHyg[5Jwf3SqIHL5JFUxLSxiSVO1NF0xNjV3IH7N NVfjXWJMQTdyM{S3NS=>
G-361 cell MY\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mkn0R5l1d3SxeHnjJJBwfGWwY4mgdoVyfWm{ZXSgeI8hcW6qaXLpeEBINTN4MTDj[YxtKGe{b4f0bEBjgSB3MDWsJGlEPTB;MD62OUBvVQ>? MlL5PVM4OTJ2MB?=
human HL60 cells NInZdJdRem:uaX\ldoF1cW:wIHHzd4F6 Mki0O|IhcA>? M{jGcGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFy2NEBk\WyuczDh[pRmeiB5MjDodpMh[nliU2LCJIF{e2G7LDDJR|UxRTJwNTDuUS=> MYOyNlk1PDF{MR?=
human K562 cells MVvDfZRwfG:6aXPpeJkh[XO|YYm= NUfkbFNKPSCmYYnz MmTUR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gT|U3OiClZXzsd{Bi\nSncjC1JIRigXNiYomgXHRVKGG|c3H5MEBKSzVyPUKuOkBvVQ>? MWqxPFA4PjF2MB?=
CH1 cell NGXBbm1EgXSxdH;4bYNqfHliYYPzZZk> NXvHUVd5S3m2b4TvfIlkKHCxdHXuZ5khemWzdXny[YQhfG9iaX7obYJqfCCFSEGgZ4VtdCCpcn;3eIgh[nliNUClMEBKSzVyPUKuOlUhdk1? NUTpOWYxQTN5MUK0NC=>
MES-SA cells NHTVPJZRem:uaX\ldoF1cW:wIHHzd4F6 NU\BSlhKPzJiaB?= M3fSRmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgUWVUNVODIHPlcIx{KGK7IF3UWEBie3OjeTDh[pRmeiB5MjDodpMtKEmFNUC9N{BvVQ>? NYfPbXVkOTZ6MkS3OVE>
A549 cells NVS2bWluTnWwY4Tpc44h[XO|YYm= MoDqRYN1cX[rdImgZYdicW6|dDDBOVQ6KGOjbnPldkBk\WyuIHzpcoUtKEmFNUC9N{4yKG6P Mn;PPFk3ODV3OB?=
LoVo cells NFz2NHJEgXSxdH;4bYNqfHliYYPzZZk> MWSxOFQhcA>? Mn3KR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUI9XdyClYX7j[ZIh[2WubDDsbY5mKHejczDk[ZRmem2rbnXkJIFnfGW{IEG0OEBpeixiSVO1NF0{NjNibl2= M1nDU|E2PDV4Mk[4
P388 cells MmDhVJJwdGmoZYLheIlwdiCjc4PhfS=> NX\Vd3dnSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBROzh6IHPlcIx{KGK7IFXMTXNCNCCLQ{WwQVQvOyCwTR?= NIf6T2EyPzF3NEWwOS=>
human Daudi cells M{\0PHBzd2yrZnXyZZRqd25iYYPzZZk> NWTW[Fd[PzJiaB?= NXzyd3ZkSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDEZZVlcSClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUWgcm0> MmDMNlU6QTh3MES=
SKOV-3 cell NWLKW3E1S3m2b4TvfIlkcXS7IHHzd4F6 NEm5[2ZEgXSxdH;4bYMheG:2ZX7jfUBz\XG3aYLl[EB1dyCrbnjpZol1KFONT2[tN{Bk\WyuIHfyc5d1cCB3MDWsJGlEPTB;NT6zJI5O MmfoPVM4OTJ2MB?=
OVCAR-3 cell M2\uZ2Z2dmO2aX;uJIF{e2G7 MXzBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCxdnHybYFvKE:YQ1HSMVMh[2WubDDsbY5meyxiSVO1NF02Njhibl2= MVu4PVYxPTV6
human MES-SA cells MW\Qdo9tcW[ncnH0bY9vKGG|c3H5 NYTafnBKPzJiaB?= NVvJcnUySW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSXMuW0FiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME22JI5O MYqyOVk6QDVyNB?=
PC3 cancer cell NIfpVpREgXSxdH;4bYNqfHliYYPzZZk> M1rZXVE1PCCq NHrQPZJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBRSzNiY3HuZ4VzKGOnbHygcIlv\SC5YYOg[IV1\XKvaX7l[EBi\nSncjCxOFQhcHJuIFnDOVA:PyCwTR?= NHrGSG8yPTR3NkK2PC=>
MXF7 breast cell NFPYXZVHfW6ldHnvckBie3OjeR?= Mnu2RY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5ibXHtcYFzgSClYYLjbY5wdWFic3Xud4l1cX[nIF3YSlch[nKnYYP0JINmdGxibHnu[UwhUUN3ME24Mlchdk1? MVW4PVYxPTV6
HT-29 cell MWnDfZRwfG:6aXPpeJkh[XO|YYm= MoTaNVQ1KGh? NUTZRlRbS3m2b4TvfIlkKHCxdHXuZ5khemWzdXny[YQhfG9iaX7obYJqfCCKVD2yPUBk\WyuIHfyc5d1cCCkeTC1NEUh[W[2ZYKgZ4VtdCCmcoXnJINwdnSjY4Sg[o9zKDF2NDDodpMtKEmFNU2wMlAyKM7:TR?= MVG5N|cyOjRy
HEK293 cells MkfQR5l1d3SxeHnjbZR6KGG|c3H5 MoDoO|IhcA>? NEPmRWVEgXSxdH;4bYNqfHliYXfhbY5{fCCKRVuyPVMh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1yLkCxJO69VQ>? NYLLPWkzOjR4MUG4PVM>
MKN45 cells MVHDfZRwfG:6aXPpeJkh[XO|YYm= NWfpR|JWOTR2IHi= M3zQbWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1MVjR3IHPhcoNmeiClZXzsJIxqdmVid3HzJIRmfGW{bXnu[YQh[W[2ZYKgNVQ1KGi{LDDJR|UxRTBwMEGyJO69VQ>? NHPiVJkyPTR3NkK2PC=>
MES-SA cells MULDfZRwfG:6aXPpeJkh[XO|YYm= M4jFe|czKGh? NX\qNHl5S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUWVLWPBJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiY3XscEBxem:uaX\ldoF1cW:wIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OC5yMUKg{txO NHfhWmMzOTR2NEKwOS=>
FM3 cells M2fEcHBzd2yrZnXyZZRqd25iYYPzZZk> NYPNdHN1PzJiaB?= MXrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE[PMzDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvODF|IN88US=> M{ThflI2QTl6NUC0
MCF-7 cells NFzwUJVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFjycFJKdmirYnn0c5J6KGGldHn2bZR6KGGpYXnud5QhcHWvYX6geJVud3JiY3XscEBtcW6nIF3DSk04KGK{ZXHzeEBi\GWwb3PhdoNqdm:vYTygTWM2OD1yLkCyJO69VQ>? NGTGeVc4QDV|M{S1
human small-cell lung cancer M2T6SmN6fG:2b4jpZ4l1gSCjc4PhfS=> Ml3vR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gd41idGxvY3XscEBtfW6pIHPhcoNmeiBqU1PMR{ktKEmFNUC9NE4xOiEQvF2= NVW5UnhOQDJ3OEizOS=>
human HCT116 cells NUDLU45zS3m2b4TvfIlkcXS7IHHzd4F6 NXPwfVlFPzJiaB?= MX\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBk\WyuIIDyc4xq\mW{YYTpc44h[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlAzOiEQvF2= MlPTNlE1PDR{MEW=
human HCT116 cells M33tdnBzd2yrZnXyZZRqd25iYYPzZZk> NEnDXWI4OiCq M{Xk[mFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MD6wNlUh|ryP MVmyOVk6QDVyNB?=
NCI-H460 cells MkPmR5l1d3SxeHnjbZR6KGG|c3H5 M3PVW|Q5KGh? NFfxeY1EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBPS0lvSES2NEBk\WyuczDh[pRmeiB2ODDodpMh[nlicnXzZZp2emmwIHT5[UBie3OjeTygSWM2OD1yLkCzJO69VQ>? NInjU4UzOzl6OEO1NS=>
CCRF-CEM cells NVjudGtxS3m2b4TvfIlkcXS7IHHzd4F6 NWTT[JdQPDhiaB?= Mny5R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gR2NTTi2FRV2gZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCC4aXHibYxqfHliYX\0[ZIhPDhiaILzJIJ6KGOnbHz0bZRmei2kbIXlJIF{e2G7LDDJR|UxRTBwMEO2JO69VQ>? NYLyZoN2OjJ3OEK5PVE>
HeLa cells M{DqdHBzd2yrZnXyZZRqd25iYYPzZZk> MUW3NkBp NVLOTG5USW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDI[WxiKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MD6wOFQh|ryP NHXmd28zPTl7OEWwOC=>
NCI60 cells NFyzfZdHfW6ldHnvckBie3OjeR?= MXm0PEBp M3jzPWFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7DTVYxKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDTVmIh[XO|YYmsJGdKPTB;NEeuPFYhdk1? NGDLTHEyQDdzNUe4Oi=>
UACC375 cell M{LMNWZ2dmO2aX;uJIF{e2G7 NHrHPFBCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDt[Yxidm:vYTDVRWNEOzd3IHPlcIwhdGmwZTygTWM2OD1yLkC0PEDPxE1? NVXidnBJQDl4MEW1PC=>
HT1080 cell MmXMS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2TiSmlvcGmkaYTvdpkh[WO2aY\peJkh[WejaX7zeEBpfW2jbjD0eY1weiClZXzsJIxqdmViSGSxNFgxNCCLQ{WwQVAvODZ4IN88US=> NIX2eYU4QDV|M{S1
MES-SA/Dx5 cells NIDOcVZRem:uaX\ldoF1cW:wIHHzd4F6 NUH0PYplPzJiaB?= MonpRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRWOtV2EwTHh3IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9NE4xPzNizszN Mkn3NlU6QTh3MES=
SF268 cells NV3TXGNFWHKxbHnm[ZJifGmxbjDhd5NigQ>? M1TQOVQ5KGh? M3;RXmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1[yOlgh[2WubIOgZYZ1\XJiNEigbJJ{NCCHQ{WwQVAvOzJizszN MlfZNlM{QTV4NU[=
KB/HeLa cells M2npZXBzd2yrZnXyZZRqd25iYYPzZZk> M17E[FQ5KGh? NI\reItCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFvCM2hmVGFiY3XscJMh[W[2ZYKgOFghcHK|LDDFR|UxRTBwM{[g{txO Mmj5NlM{QTV4NU[=
K562 cells MWPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mn35O|IhcA>? MljUS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gT|U3OiClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRUKG2ndHjv[EwhUUN3ME2wMlQzKM7:TR?= MV2xPFI2QDR2Mh?=
MDA-MB-231 cells MnzoVJJwdGmoZYLheIlwdiCjc4PhfS=> NUfxWIpVPzJiaB?= NWDmcmd3SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHL5JHdUXC1zIH3leIhw\CCjZoTldkA4OiCqcoOsJGlEPTB;MD65OkDPxE1? MYqxO|M{PTF6OR?=
SF268 cells NYD6V3ZtS3m2b4TvfIlkcXS7IHHzd4F6 MV[0PEBp Mnf4R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2YzPjhiY3XscJMh[W[2ZYKgOFghcHK|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlk4KM7:TR?= MYWxO|k3OjB{OB?=
HCT116 cells NH\wNWNEgXSxdH;4bYNqfHliYYPzZZk> Mmn3R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGNVOTF4IHPlcIx{KGK7IF3UWEBie3OjeTygTWM2OD1|Lkm2JO69VQ>? NYnLbnZZOjB7NUG1PFI>
U937 cells MlHLR5l1d3SxeHnjbZR6KGG|c3H5 MnzmR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gWVk{PyClZXzsd{BjgSCPVGSgZZN{[XluIFnDOVA:Pi5{IN88US=> NFTW[4syQTZzNUmwNC=>
HepG2 cells NITv[nBRem:uaX\ldoF1cW:wIHHzd4F6 MnzDOFghcA>? NVm1NXAxSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDI[ZBIOiClZXzsd{Bi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUGxMlA2KM7:TR?= NYDRVplEOjR5OUS3OFc>
Assay
Methods Test Index PMID
Western blot p-ROS1 / ROS1 / p-STAT3 / STAT3 / p-AKT / AKT / p-ERK / ERK 30108778
Growth inhibition assay Cell number 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 (from reference)

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 517.4
Formula

C22H29ClN4O6.2HCl

CAS No. 70476-82-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC(=C2C(=C1NCCNCCO)C(=O)C3=C(C=CC(=C3C2=O)O)O)NCCNCCO.Cl.Cl

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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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

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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