Vadimezan (ASA404)

Catalog No.S1537 Synonyms: NSC 640488, DMXAA

For research use only.

Vadimezan (ASA404, NSC 640488, DMXAA) is a vascular disrupting agents (VDA) and competitive inhibitor of DT-diaphorase with Ki of 20 μM and IC50 of 62.5 μM in cell-free assays, respectively. DMXAA (Vadimezan) is also a STING agonist with potential antineoplastic activity. DMXAA (Vadimezan) potently induces IFN-β but relatively low TNF-α expression in vitro. DMXAA (Vadimezan) has antiviral activity. Phase 3.

Vadimezan (ASA404) Chemical Structure

CAS No. 117570-53-3

Selleck's Vadimezan (ASA404) has been cited by 21 publications

Purity & Quality Control

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Biological Activity

Description Vadimezan (ASA404, NSC 640488, DMXAA) is a vascular disrupting agents (VDA) and competitive inhibitor of DT-diaphorase with Ki of 20 μM and IC50 of 62.5 μM in cell-free assays, respectively. DMXAA (Vadimezan) is also a STING agonist with potential antineoplastic activity. DMXAA (Vadimezan) potently induces IFN-β but relatively low TNF-α expression in vitro. DMXAA (Vadimezan) has antiviral activity. Phase 3.
Targets
DT-diaphorase [1]
(Cell-free assay)
DT-diaphorase [1]
(Cell-free assay)
20 μM(Ki) 20 μM(Ki)
In vitro

In DLD-1 human colon carcinoma cells, DMXAA inhibits DT-diaphorase activity without significant effects on the activity of cytochrome b5 reductase and cytochrome P450 reductase. Combination of menadione and DMXAA leads to an increase in the antiproliferative activity of DLD-1 cells. [1] DMXAA, as an antiviral agent, inhibits VSV-induced cytotoxicity and influenza virus replication in RAW 264.7 macrophages. [2] A recent study shows that DMXAA has non-immune-mediated inhibitory effects against several kinase members of VEGFR (vascular endothelial growth factor receptor), such as VEGFR2 signalling in human umbilical vein endothelial cells. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human BJ cells NEfEUo5EgXSxdH;4bYPDqGG|c3H5 NVG2bmxXOjRiaB?= NULROVlUS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSkpiY3XscJMh[W[2ZYKgNlQhcHK|IHL5JG1VXCCjc4PhfUwhS0N3ME20PE46KM7:TR?= MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDVzOEK5OUc,OjR3MUiyPVU9N2F-
HECPP cells M1LaW2Z2dmO2aX;uJIF{e2G7 MY[xNEB2\y:vTB?= NFXsVmVC[3SrdnH0bY9vKG:oIF7GMYtieHCjQjDpckBJTUOSUDDj[YxteyCjdDCxNEB2\y:vTB?= MnP2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd4MU[xNVQoRjF5NkG2NVE1RC:jPh?=
MCF7 MmSwRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MX6yOEBpenN? MoPsRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3JINmdGy|IHPvMZRz\WG2ZXSge4l1cCCyeYLhco95[W62aH;u[UBifCBzOkGgcY9t[XJicnH0bY8h[W[2ZYKgNlQhcHK|IHL5JG1VXCCjc4PhfUwhUUN3MDC9JFEyNjh7IN88UU4> NXi3UXBPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmxNlk2OTFpPkK5NVI6PTFzPD;hQi=>
MDA-MB-231 MmTkRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MlzjNlQhcHK| M3nmVmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTJ|MTDj[YxteyClbz30doVifGWmIIfpeIgheHm{YX7vfIFvfGixbnWgZZQhOTpzIH3vcIFzKHKjdHnvJIFnfGW{IEK0JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTBiPTCxNk4yOiEQvF2u M1vRS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUK5OVEyLz5{OUGyPVUyOTxxYU6=
K562 M17IS2FvfGmycn;sbYZmemG2aY\lJIF{e2G7 NFG3WIgzPCCqcoO= NHvRO5JCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFu1OlIh[2WubIOgZ48ufHKnYYTl[EB4cXSqIID5doFvd3ijboToc45mKGG2IEG6NUBud2yjcjDyZZRqdyCjZoTldkAzPCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOTlwMUSg{txONg>? Ml3TQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjlzMkm1NVEoRjJ7MUK5OVEyRC:jPh?=
HepG2 M1HNbmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NYn3SJZKOjRiaILz MYrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEincFeyJINmdGy|IHPvMZRz\WG2ZXSge4l1cCCyeYLhco95[W62aH;u[UBifCBzOkGgcY9t[XJicnH0bY8h[W[2ZYKgNlQhcHK|IHL5JG1VXCCjc4PhfUwhUUN3MDC9JFIyNjJ3IN88UU4> NU[2VnVKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmxNlk2OTFpPkK5NVI6PTFzPD;hQi=>
COLO320 NVu5PWJ{SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MnLhOFghcHK| NI[5OXZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFPPUG8{OjBiY3XscJMh[W[2ZYKgOFghcHK|IHL5JGNEUzhiYYPzZZktKEmFNUCgQUA{QS53IN88UU4> M3HUdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{e2N|czLz5{OEO3OlM4OjxxYU6=
MDA-MB-231 NGrhNm1CdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NGi1OG41QCCqcoO= MlvWRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuOjNzIHPlcIx{KGGodHXyJFQ5KGi{czDifUBES0t6IHHzd4F6NCCLQ{WwJF0hPDhwNDFOwG0v MmDSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh|N{[zO|IoRjJ6M{e2N|czRC:jPh?=
MDA-MB-231 NHr1OYNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXKySFF1OjRiaILz NEnoN49Iem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBOTEFvTVKtNlMyKGOnbHzzJIFnfGW{IEK0JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTBiPTC0PE41OiEQvF2u MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTZyOUGyNUc,Ojl4MEmxNlE9N2F-
MDA-MB-231 NWPsToJ1SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NVe2dHpNOjRiaILz MoTORY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuOjNzIHPlcIx{KGGodHXyJFI1KGi{czDifUBOXFRiYYPzZZktKEmFNUCgQUA1QC52NDFOwG0v NUjvRnJ2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmxNlk2OTFpPkK5NVI6PTFzPD;hQi=>
A673 MWHxTHRUKGG|c3H5 MlrFdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEF4N{OgZ4VtdHN? MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
DAOY M1X1TJFJXFNiYYPzZZk> MUXxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhTEGRWTDj[Yxtew>? MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
RD MmLJdWhVWyCjc4PhfS=> M3HpXZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCURDDj[Yxtew>? NXPudmRbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-SH NYCy[G83eUiWUzDhd5NigQ>? NGfKbFlyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1UUCClZXzsdy=> NIXyemc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
MG 63 (6-TG R) MYPxTHRUKGG|c3H5 MUnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVUdiNkOgLFYuXEdiUjmgZ4VtdHN? MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
NB1643 M2XvNpFJXFNiYYPzZZk> M{f0dpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQkG2OFMh[2WubIO= NXni[I13RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Rh41 MVLxTHRUKGG|c3H5 NU\leIs4eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGLoOFEh[2WubIO= NWPmfI9vRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-MC M{\hZpFJXFNiYYPzZZk> NH;nbFhyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1OSyClZXzsdy=> MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
MDA-MB-231 NGS0cYtCeG:ydH;zbZMh[XO|YYm= MnvaNlQhfG9iOU[geW0> M1HEZlQ5KGi{cx?= NGG1fYpKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5kemWjc3WgbY4h[2ynYY\l[EBk[XOyYYPlMVMh\XiycnXzd4lwdiCjdDCyOEB1dyB7NjD1UUBi\nSncjC0PEBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ M33XZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{e2N|czLz5{OEO3OlM4OjxxYU6=
MDA-MB-231 MVfBdI9xfG:|aYOgZZN{[Xl? NHzpdGgzPCC2bzC5OkB2VQ>? NWjaRZVmPDhiaILz NFLJb4lKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5kemWjc3WgbY4h[2ynYY\l[EBRSVKSIHzleoVtKGG2IEK0JJRwKDl4IIXNJIFnfGW{IES4JIhzeyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM> NYnvO4p4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkizO|Y{PzJpPkK4N|c3Ozd{PD;hQi=>
MDA-MB-231 NVTrUo5jTnWwY4Tpc44h[XO|YYm= MXSyOEB1dyB7NjD1US=> NUX6dlM5PDhiaILz MWTE[YNz\WG|ZTDpckBk[XOyYYPlMVMhdGW4ZXygbY4hcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDheEAzPCC2bzC5OkB2VSCjZoTldkA1QCCqcoOgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m| MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDN5NkO3Nkc,Ojh|N{[zO|I9N2F-
MDA-MB-231 MnTNSpVv[3Srb36gZZN{[Xl? MWGyOEB1dyB7NjD1US=> MUG0PEBpenN? M3j0cWlv[3KnYYPlJIlvKHB3MzDs[ZZmdCCrbjDoeY1idiCPRFGtUWIuOjNzIHPlcIx{KGG2IEK0JJRwKDl4IIXNJIFnfGW{IES4JIhzeyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM> NUD1bo1WRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkizO|Y{PzJpPkK4N|c3Ozd{PD;hQi=>
MDA-MB-231 NFTT[W1HfW6ldHnvckBie3OjeR?= MW[yOEB1dyB7NjD1US=> MXO0PEBpenN? MkfkSIVkemWjc3WgbY4h[2G|cHHz[U06KGyndnXsJIlvKGi3bXHuJG1FSS2PQj2yN|Eh[2WubIOgZZQhOjRidH:gPVYhfU1iYX\0[ZIhPDhiaILzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?= MmH1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh|N{[zO|IoRjJ6M{e2N|czRC:jPh?=
MDA-MB-231 MU\GeY5kfGmxbjDhd5NigQ>? NFTUUVMzPCC2bzC5OkB2VQ>? MmPIOFghcHK| NYrOU2ROTGWlcnXhd4UhcW5iTVTNNkBt\X[nbDDpckBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHH0JFI1KHSxIEm2JJVOKGGodHXyJFQ5KGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? MnPqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh|N{[zO|IoRjJ6M{e2N|czRC:jPh?=
HepG2 MkP4R4VtdCCleXPs[UBienKnc4SgZZN{[Xl? MXOwMlIhfU1? NYDWSlU5OjRiaILz NIDzR2NE\WyuIHP5Z4xmKGG{cnXzeEBqdiCqdX3hckBJ\XCJMjDj[YxteyCjc4Pld5Nm\CCjczDhZ4N2dXWuYYTpc44h[XRiUzDwbIF{\SCjdDCwMlIhfU1iYX\0[ZIhOjRiaILzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[oxwfyCleYTvcYV1emmlIH3leIhw\CC{ZXzheIl3\SC2bzDjc451em:u NVHGOItJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmxNlk2OTFpPkK5NVI6PTFzPD;hQi=>
HepG2 M3fJS2NmdGxiY4njcIUh[XK{ZYP0JIF{e2G7 M4SzdVI1KGi{cx?= NE\ZdJdE\WyuIHP5Z4xmKGG{cnXzeEBqdiCqdX3hckBJ\XCJMjDj[YxteyCjc4Pld5Nm\CCjczDhZ4N2dXWuYYTpc44h[XRiUzDwbIF{\SClbz30doVifGWmIIfpeIgheHm{YX7vfIFvfGixbnWgZZQhOTpzIH3vcIFzKHKjdHnvJIFnfGW{IEK0JIhzeyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pLXLhd4VlKG[ub4egZ5l1d22ndILpZ{Bu\XSqb3S= MnO2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjlzMkm1NVEoRjJ7MUK5OVEyRC:jPh?=
HepG2 NYPueJhGSXCxcITvd4l{KGG|c3H5 NHTMfm0xNjJidV2= NHzRdYszPCCqcoO= M2PMWmlv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gbJVu[W5iSHXwS|Ih[2WubIOgZZN{\XO|ZXSgZZMhcW6lcnXhd4UhcW5iY3zlZZZm\CClYYPwZZNmNTNibHX2[Yx{KGG2IECuNkB2VSCjZoTldkAzPCCqcoOgZpkhX2W|dHXyckBjdG:2IH3leIhw\A>? NUHrWVJrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmxNlk2OTFpPkK5NVI6PTFzPD;hQi=>
HepG2 NHnofpBCeG:ydH;zbZMh[XO|YYm= M3PBV|AvOiC3TR?= M4\ORlI1KGi{cx?= MVTJcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHj1cYFvKEincFeyJINmdGy|IHHzd4V{e2WmIHHzJIlv[3KnYYPlJIlvKGOuZXH2[YQh[2G|cHHz[U06KGyndnXsd{BifCByLkKgeW0h[W[2ZYKgNlQhcHK|IHL5JHdme3Sncn6gZoxwfCCvZYToc4Q> MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF{OUWxNUc,OjlzMkm1NVE9N2F-
HepG2 Ml3lRZBweHSxc3nzJIF{e2G7 MmTiNlQhcHK| NInoU2FKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIFjldGczKGOnbHzzJIF{e2W|c3XkJIF{KGmwY4LlZZNmKGmwIHPs[YF3\WRiUFHSVEBt\X[nbIOgZ48ufHKnYYTl[EB4cXSqIID5doFvd3ijboToc45mKGG2IEG6NUBud2yjcjDyZZRqdyCjZoTldkAzPCCqcoOgZpkhX2W|dHXyckBjdG:2IH3leIhw\A>? NU\jW|E1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmxNlk2OTFpPkK5NVI6PTFzPD;hQi=>
HepG2 NHLpOlRCeG:ydH;zbZMh[XO|YYm= NXmycVhROC5{IIXN NGO5cJYzPCCqcoO= M{fEOmlv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gbJVu[W5iSHXwS|Ih[2WubIOgZZN{\XO|ZXSgZZMhcW6lcnXhd4UhcW5iY3zlZZZm\CCSQWLQJIxmfmWuczDheEAxNjJidV2gZYZ1\XJiMkSgbJJ{KGK7IGfld5Rmem5iYnzveEBu\XSqb3S= MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF{OUWxNUc,OjlzMkm1NVE9N2F-
HepG2 MUPBdI9xfG:|aYOgZZN{[Xl? Mny3NlQhcHK| NEfHZZVKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIFjldGczKGOnbHzzJIF{e2W|c3XkJIF{KGmwY4LlZZNmKGmwIHPs[YF3\WRiY3HzdIF{\S1|IHzleoVteyClbz30doVifGWmIIfpeIgheHm{YX7vfIFvfGixbnWgZZQhOTpzIH3vcIFzKHKjdHnvJIFnfGW{IEK0JIhzeyCkeTDX[ZN1\XKwIHLsc5QhdWW2aH;k NGW1fVE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUGyPVUyOSd-MkmxNlk2OTF:L3G+
HepG2 MYrBdI9xfG:|aYOgZZN{[Xl? NFK5eVEzPCCqcoO= NXu2cm9XUW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyCrbnPy[YF{\SCrbjDjcIVifmWmIHPhd5Bie2VvOTDs[ZZmdHNiY3:teJJm[XSnZDD3bZRpKHC7cnHuc5hidnSqb37lJIF1KDF8MTDtc4xieiC{YYTpc{Bi\nSncjCyOEBpenNiYomgW4V{fGW{bjDicI91KG2ndHjv[C=> M1XRd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUK5OVEyLz5{OUGyPVUyOTxxYU6=
HepG2 MX;BdI9xfG:|aYOgZZN{[Xl? MUGyOEBpenN? MoLaTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCKZYDHNkBk\WyuczDhd5Nme3OnZDDhd{Bld3ewcnXneYxifGmxbjDv[kBD[2xveFyg[ZhxemW|c3nvckBkdy22cnXheIVlKHerdHigdJlz[W6xeHHueIhwdmViYYSgNVoyKG2xbHHyJJJifGmxIHHmeIVzKDJ2IHjyd{BjgSCZZYP0[ZJvKGKub4SgcYV1cG:m NH[1dog9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUGyPVUyOSd-MkmxNlk2OTF:L3G+
HepG2 MV;BdI9xfG:|aYOgZZN{[Xl? MWOyOEBpenN? NGHMU2xKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIFjldGczKGOnbHzzJIF{e2W|c3XkJIF{KHWycnXneYxifGmxbjDv[kBDcWRiZYjwdoV{e2mxbjDjc{11emWjdHXkJJdqfGhicInyZY5wgGGwdHjvcoUh[XRiMUqxJI1wdGG{IILheIlwKGGodHXyJFI1KGi{czDifUBY\XO2ZYLuJIJtd3RibXX0bI9l NEiwSYc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUGyPVUyOSd-MkmxNlk2OTF:L3G+
Assay
Methods Test Index PMID
Western blot p-p38 / p38 ; p-MK2 / pERK / p-JNK 21819972
Growth inhibition assay Cell proliferation 30138430
In vivo DMXAA treatment significantly protects C57BL/6J mice infected i.n. with 200 p.f.u. mouse-adapted H1N1 influenza PR8 virus with 60% survival, while the control group only exhibited 20% survival. [2] DMXAA significantly delays tumor growth induced by chemical carcinogen, increases the time to tumor doubling and increases time from treatment to euthanasia. After the treatment of DMXAA, median tumor doubling time, median tumour tripling time and median time from treatment to euthanasia in tumor-bearing animals are increased by approximately 4.4-, 1.8- and 2.7-fold, respectively. [4]

Protocol (from reference)

Kinase Assay:[1]
  • DT-diaphorase activity and kinetic analysis of enzyme inhibition :

    Purified DT-diaphorase enzyme activity is assayed by measuring the reduction of cytochrome c at 550 nm on a Beckman DU 650 spectrophotometer. Each assay contains cytochrome c (70 μM), NADH (variable concentrations), purified DT-diaphorase (0.032 μg), and menadione (variable concentrations) in a final volume of 1 mL Tris–HCl buffer (50 mM, pH 7.4) containing 0.14% BSA. The reaction is started by the addition of NADH. Rates of reduction are calculated over the initial part of the reaction curve (30 seconds), and results are expressed in terms of μmol cytochrome c reduced/min/mg protein using a molar extinction coefficient of 21.1 mM−1 cm−1 for reduced cytochrome c. Enzyme assays are carried out at room temperature and all reactions are performed in triplicate. Inhibition of purified DT-diaphorase activity is performed by the inclusion of DMXAA (at various concentrations) in the reaction, and inhibition characteristics are determined by varying the concentration of NADH (constant menadione) or menadione (constant NADH) at several concentrations of inhibitor. Ki values are obtained by plotting 1/V against. The activity of DT-diaphorase in DLD-1 cells is determined by measuring the dicumarol-sensitive reduction of DCPIP at 600 nm. Briefly, DLD-1 cells in mid-exponential growth are harvested by scraping into ice-cold buffer (Tris–HCl, 25 mM, pH 7.4 and 250 mM sucrose) and sonicated on ice. Enzyme assay conditions are 2 mM NADH, 40 μM DCPIP, 20 μL of dicumarol (when required) in a final volume of 1 mL Tris–HCl (25 mM, pH 7.4) containing BSA (0.7 mg/mL). Results are expressed as the dicumarol-sensitive reduction of DCPIP using a molar extinction coefficient of 21 mM−1 cm−1. Protein levels are determined using the Bradford assay

Cell Research:[1]
  • Cell lines: DLD-1 and H460 cells
  • Concentrations: 0-2 mM
  • Incubation Time: 96 hours
  • Method: DLD-1 human colon carcinoma and H460 human non-small cell lung carcinoma cells are routinely maintained as monolayer cultures in RPMI 1640 culture medium supplemented with foetal calf serum (10%), sodium pyruvate (2 mM), penicillin/streptomycin (50 IU mL−1/50 μg mL-1) and l-glutamine (2 mM). Chemosensitivity is assessed using the MTT assay and all assays are performed under aerobic conditions. Briefly, cells are plated into each well of a 96-well culture plate and incubated overnight in an atmosphere containing 5% CO2. Culture medium is completely removed from each well and replaced with medium containing a range of drug concentrations. In the case of menadione alone, the duration of drug exposure is 1 hour, after which the cells are washed twice with Hanks' balanced salt solution prior to the addition of 200 μL fresh RPMI 1640 medium to each well of the plate. In the case of DMXAA alone, the duration of drug exposure is 3 hours. Following a four-day incubation, cell survival is determined using the MTT assay. For combinations of DMXAA with menadione, cells are initially set up and a non-toxic (>95% cell survival) concentration of DMXAA is selected. Cells are then initially exposed to DMXAA (2 mM) for a period of 2 hours, following which the medium is removed and replaced with medium containing the inhibitor (DMXAA at a constant concentration of 2 mM) and menadione (at a range of drug concentrations). Following a further 7-hour incubation, cells are washed twice with Hanks' balanced salt solution prior to the addition of growth medium.
  • (Only for Reference)
Animal Research:[4]
  • Animal Models: Chemical carcinogen (NMU) is injected into female Wistar rats.
  • Dosages: ≤300 mg/kg
  • Administration: Administered via i.p.
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 7 mg/mL
(24.79 mM)
Water Insoluble
Ethanol Insoluble

* 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 282.29
Formula

C17H14O4

CAS No. 117570-53-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(C2=C(C=C1)C(=O)C3=CC=CC(=C3O2)CC(=O)O)C

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

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%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
NCT00856336 Completed Drug: DMXAA Refractory Tumors Antisoma Research May 2003 Phase 1
NCT00863733 Completed Drug: DMXAA Solid Tumors Cancer Research UK|Cancer Society Auckland May 1996 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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