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 36 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 MnfnR5l1d3SxeHnjbZR6KGG|c3H5 NVzOb2xsPDhiaB?= MnfFR5l1d3SxeHnjJJBwfGWwY4mgdoVyfWm{ZXSgeI8hcW6qaXLpeEBNOTJzMDDj[YxtKGe{b4f0bEBjgSB3MDWgZYZ1\XJiY3XscEBlenWpIHPvcpRi[3RiZn;yJFQ5KGi{czygTWM2OD12ZT2wOUDPxE1? NUTocIR1QTN5MUK0NC=>
HL60 cells MYfDfZRwfG:6aXPpeJkh[XO|YYm= MWS0PEBp M2D1VWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhNPjBiY3XscJMh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhT0l3ME2wMlM{KM7:TR?= NYXLWWJUOTd7NkKwNlg>
MDA435/LCC6 cells M1HGe3Bzd2yrZnXyZZRqd25iYYPzZZk> NXW2boxISW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBOTEF2M{WvUGNEPiClZXzsd{BjgSCHTFnTRUwhUUN3ME2wMlM2KG6P M3K4XFE4OTV2NUC1
A2780-cell MU\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mlz2R49v[2WwdILheIlwdiC{ZYH1bZJm\CC2bzDpcohq[mm2IFGyO|gxNWOnbHyg[5Jwf3SqIHL5JFUxLSxiSVO1NF0xNjV3IH7N NHHTU486PzB|NEex
G-361 cell NWLPdHU{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NV25SpE2S3m2b4TvfIlkKHCxdHXuZ5khemWzdXny[YQhfG9iaX7obYJqfCCJLUO2NUBk\WyuIHfyc5d1cCCkeTC1NEUtKEmFNUC9NE43PSCwTR?= NYTLfI1wQTN5MUK0NC=>
human HL60 cells MX;Qdo9tcW[ncnH0bY9vKGG|c3H5 NX[zN41{PzJiaB?= NVqxWFM2SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIUFYxKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDTVmIh[XO|YYmsJGlEPTB;Mj61JI5O MUCyNlk1PDF{MR?=
human K562 cells NFrWNFBEgXSxdH;4bYNqfHliYYPzZZk> M2X4eFUh\GG7cx?= NIjTTZNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBMPTZ{IHPlcIx{KGGodHXyJFUh\GG7czDifUBZXFRiYYPzZZktKEmFNUC9Nk43KG6P M2XsXlE5ODd4MUSw
CH1 cell NGfM[5BEgXSxdH;4bYNqfHliYYPzZZk> MYfDfZRwfG:6aXOgdI91\W6leTDy[ZF2cXKnZDD0c{BqdmirYnn0JGNJOSClZXzsJIdzd3e2aDDifUA2OCVuIFnDOVA:Oi54NTDuUS=> MYG5N|cyOjRy
MES-SA cells MVfQdo9tcW[ncnH0bY9vKGG|c3H5 NHTBPWw4OiCq Ml3JRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDNSXMuW0FiY3XscJMh[nliTWTUJIF{e2G7IHHmeIVzKDd{IHjyd{whUUN3ME2zJI5O MV2xOlgzPDd3MR?=
A549 cells MmXkSpVv[3Srb36gZZN{[Xl? MnraRYN1cX[rdImgZYdicW6|dDDBOVQ6KGOjbnPldkBk\WyuIHzpcoUtKEmFNUC9N{4yKG6P MlntPFk3ODV3OB?=
LoVo cells NHy0NXREgXSxdH;4bYNqfHliYYPzZZk> MnvSNVQ1KGh? MYnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDMc3ZwKGOjbnPldkBk\WyuIHzpcoUhf2G|IHTleIVzdWmwZXSgZYZ1\XJiMUS0JIhzNCCLQ{WwQVMvOyCwTR?= NF3oR5EyPTR3NkK2PC=>
P388 cells NHLlbXFRem:uaX\ldoF1cW:wIHHzd4F6 MV;BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IGCzPFgh[2WubIOgZpkhTUyLU1GsJGlEPTB;ND6zJI5O NEnwfWwyPzF3NEWwOS=>
human Daudi cells MYjQdo9tcW[ncnH0bY9vKGG|c3H5 NFvDO|M4OiCq NXrlTnhLSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDEZZVlcSClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUWgcm0> MU[yOVk6QDVyNB?=
SKOV-3 cell MU\DfZRwfG:6aXPpeJkh[XO|YYm= MmO2R5l1d3SxeHnjJJBwfGWwY4mgdoVyfWm{ZXSgeI8hcW6qaXLpeEBUU0:YLUOgZ4VtdCCpcn;3eIghPTBnLDDJR|UxRTVwMzDuUS=> NWTWTIhzQTN5MUK0NC=>
OVCAR-3 cell M17ObmZ2dmO2aX;uJIF{e2G7 NWLpR41GSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gc5ZiemmjbjDPWmNCWi1|IHPlcIwhdGmwZYOsJGlEPTB;NT64JI5O NUPZU5g5QDl4MEW1PC=>
human MES-SA cells NUL4eoFWWHKxbHnm[ZJifGmxbjDhd5NigQ>? MUG3NkBp Mn3PRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRWOtV2Eh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD14IH7N NE[xNIszPTl7OEWwOC=>
PC3 cancer cell M330WWN6fG:2b4jpZ4l1gSCjc4PhfS=> MW[xOFQhcA>? NI\ORYlEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBRSzNiY3HuZ4VzKGOnbHygcIlv\SC5YYOg[IV1\XKvaX7l[EBi\nSncjCxOFQhcHJuIFnDOVA:PyCwTR?= NFfsV|QyPTR3NkK2PC=>
MXF7 breast cell NIfLfWJHfW6ldHnvckBie3OjeR?= M4LTcmFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIH3hcY1ienliY3HyZ4lvd22jIIPlcpNqfGm4ZTDNXGY4KGK{ZXHzeEBk\WyuIHzpcoUtKEmFNUC9PE44KG6P M1HnfVg6PjB3NUi=
HT-29 cell NITaUZREgXSxdH;4bYNqfHliYYPzZZk> MX:xOFQhcA>? MmHWR5l1d3SxeHnjJJBwfGWwY4mgdoVyfWm{ZXSgeI8hcW6qaXLpeEBJXC1{OTDj[YxtKGe{b4f0bEBjgSB3MDWgZYZ1\XJiY3XscEBlenWpIHPvcpRi[3RiZn;yJFE1PCCqcoOsJGlEPT1yLkCxJO69VQ>? NVj2Rm15QTN5MUK0NC=>
HEK293 cells MYPDfZRwfG:6aXPpeJkh[XO|YYm= NXH4fJlJPzJiaB?= MVPDfZRwfG:6aXPpeJkh[WejaX7zeEBJTUt{OUOgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjBzIN88US=> Mk\uNlQ3OTF6OUO=
MKN45 cells M{\FT2N6fG:2b4jpZ4l1gSCjc4PhfS=> NXnqW3BSOTR2IHi= NFzp[VlEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOU052NTDjZY5k\XJiY3XscEBtcW6nIIfhd{Bl\XSncn3pcoVlKGGodHXyJFE1PCCqcjygTWM2OD1yLkCxNkDPxE1? MYKxOVQ2PjJ4OB?=
MES-SA cells M1WwUmN6fG:2b4jpZ4l1gSCjc4PhfS=> NVPFN5d5PzJiaB?= NIrjSJBEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOTVNvU1GgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25iYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjBzMjFOwG0> NGHRSoMzOTR2NEKwOS=>
FM3 cells NFP1UGxRem:uaX\ldoF1cW:wIHHzd4F6 NFTrWYI4OiCq MkLiRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCITUOgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjBzMzFOwG0> NGn4SVEzPTl7OEWwOC=>
MCF-7 cells MVvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVPJcohq[mm2b4L5JIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5idIXtc5Ih[2WubDDsbY5mKE2FRj23JIJz\WG|dDDh[IVvd2OjcnPpco9u[SxiSVO1NF0xNjB{IN88US=> NEmzRmU4QDV|M{S1
human small-cell lung cancer Mo[3R5l1d3SxeHnjbZR6KGG|c3H5 NX20fnBGS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4he22jbHytZ4VtdCCudX7nJINidmOncjCoV2NNSyluIFnDOVA:OC5yMjFOwG0> MX24NlU5QDN3
human HCT116 cells NVO1d4NmS3m2b4TvfIlkcXS7IHHzd4F6 M3\kWFczKGh? MVnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBk\WyuIIDyc4xq\mW{YYTpc44h[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlAzOiEQvF2= MlT0NlE1PDR{MEW=
human HCT116 cells MoniVJJwdGmoZYLheIlwdiCjc4PhfS=> M1jGUVczKGh? NY\pbHRmSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlAzPSEQvF2= NHq0bJgzPTl7OEWwOC=>
NCI-H460 cells MXzDfZRwfG:6aXPpeJkh[XO|YYm= M{K2XFQ5KGh? NXrFXFgyS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVkOLLVi0OlAh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IILld4F7fXKrbjDkfYUh[XO|YYmsJGVEPTB;MD6wN{DPxE1? MWWyN|k5QDN3MR?=
CCRF-CEM cells NVXWRmRVS3m2b4TvfIlkcXS7IHHzd4F6 MYK0PEBp MlvyR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gR2NTTi2FRV2gZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCC4aXHibYxqfHliYX\0[ZIhPDhiaILzJIJ6KGOnbHz0bZRmei2kbIXlJIF{e2G7LDDJR|UxRTBwMEO2JO69VQ>? NHzmOoUzOjV6Mkm5NS=>
HeLa cells NY[2NnFSWHKxbHnm[ZJifGmxbjDhd5NigQ>? MWO3NkBp MkToRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKZVzhJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OC5yNESg{txO NVLXVXY{OjV7OUi1NFQ>
NCI60 cells MYTGeY5kfGmxbjDhd5NigQ>? MUO0PEBp NX36boNsSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gUmNKPjBiY3XscJMh[W[2ZYKgOFghcHK|IHL5JHNTSiCjc4PhfUwhT0l3ME20O{45PiCwTR?= NVmzR4dbOTh5MUW3PFY>
UACC375 cell NVj1To9oTnWwY4Tpc44h[XO|YYm= MVPBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCvZXzhco9u[SCXQVPDN|c2KGOnbHygcIlv\SxiSVO1NF0xNjB2ODFOwG0> M4f2NVg6PjB3NUi=
HT1080 cell Mn;OS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXGxOVBNUW6qaXLpeI9zgSCjY4Tpeol1gSCjZ3HpcpN1KGi3bXHuJJR2dW:{IHPlcIwhdGmwZTDIWFExQDBuIFnDOVA:OC5yNk[g{txO Mo[zO|g2OzN2NR?=
MES-SA/Dx5 cells M1T2TnBzd2yrZnXyZZRqd25iYYPzZZk> NUTkWGt3PzJiaB?= NGL5XHNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3FV{1USS:GeEWgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjB5MzFOwG0> NVW5NXh2OjV7OUi1NFQ>
SF268 cells MnLWVJJwdGmoZYLheIlwdiCjc4PhfS=> NYOyNoR[PDhiaB?= M2DjUWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1[yOlgh[2WubIOgZYZ1\XJiNEigbJJ{NCCHQ{WwQVAvOzJizszN MnTHNlM{QTV4NU[=
KB/HeLa cells Mnj0VJJwdGmoZYLheIlwdiCjc4PhfS=> MUC0PEBp NVvZTFFoSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLRk9J\UyjIHPlcIx{KGGodHXyJFQ5KGi{czygSWM2OD1yLkO2JO69VQ>? NYrQUpBbOjN|OUW2OVY>
K562 cells M2LaSmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIPDT|E4OiCq M{HL[Wdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJGs2PjJiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VWyCvZYToc4QtKEmFNUC9NE41OiEQvF2= NH\ONowyQDJ3OES0Ni=>
MDA-MB-231 cells Mn3ZVJJwdGmoZYLheIlwdiCjc4PhfS=> M{HhVlczKGh? M4jVNmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTJ|MTDj[YxteyCkeTDXV3QuOSCvZYToc4Qh[W[2ZYKgO|IhcHK|LDDJR|UxRTBwOU[g{txO MkWzNVc{OzVzOEm=
SF268 cells Mn3YR5l1d3SxeHnjbZR6KGG|c3H5 NWexU2tTPDhiaB?= MYjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTSlI3QCClZXzsd{Bi\nSncjC0PEBpenNiYomgV3JDKGG|c3H5MEBIUTVyPUCuPVch|ryP NYXjR|FoOTd7NkKwNlg>
HCT116 cells NVHLSGRzS3m2b4TvfIlkcXS7IHHzd4F6 NFLS[GpEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJS1RzMU[gZ4VtdHNiYomgUXRVKGG|c3H5MEBKSzVyPUOuPVYh|ryP NHfQU|UzODl3MUW4Ni=>
U937 cells M3fYVWN6fG:2b4jpZ4l1gSCjc4PhfS=> NV73Wpc2S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hXTl|NzDj[YxteyCkeTDNWHQh[XO|YYmsJGlEPTB;Nj6yJO69VQ>? M1zPdFE6PjF3OUCw
HepG2 cells NVPRU5BZWHKxbHnm[ZJifGmxbjDhd5NigQ>? NHPl[Gg1QCCq M4XNNmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSHXwS|Ih[2WubIOgZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1zMT6wOUDPxE1? NEDLVJgzPDd7NEe0Oy=>
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

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 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)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

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%DMSO %

Calculation results:

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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