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 24 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 M1:zdGN6fG:2b4jpZ:Kh[XO|YYm= MYGyOEBp MknrR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRmoh[2WubIOgZYZ1\XJiMkSgbJJ{KGK7IF3UWEBie3OjeTygR2M2OD12OD65JO69VQ>? NVrjTVJFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1NVgzQTVpPkK0OVE5Ojl3PD;hQi=>
HECPP cells M2TibmZ2dmO2aX;uJIF{e2G7 MoHzNVAhfWdxbVy= MVTBZ5RqfmG2aX;uJI9nKE6ILXvhdJBiSiCrbjDISWNRWCClZXzsd{BifCBzMDD1[{9uVA>? NHvD[WE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{[xOlEyPCd-MUe2NVYyOTR:L3G+
MCF7 MmDORY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NFLnN3gzPCCqcoO= NFvwcJpCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlch[2WubIOgZ48ufHKnYYTl[EB4cXSqIID5doFvd3ijboToc45mKGG2IEG6NUBud2yjcjDyZZRqdyCjZoTldkAzPCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOTFwOEmg{txONg>? M2XCb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUK5OVEyLz5{OUGyPVUyOTxxYU6=
MDA-MB-231 M1jkXmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MlLmNlQhcHK| NYn2Xm9YSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHPvMZRz\WG2ZXSge4l1cCCyeYLhco95[W62aH;u[UBifCBzOkGgcY9t[XJicnH0bY8h[W[2ZYKgNlQhcHK|IHL5JG1VXCCjc4PhfUwhUUN3MDC9JFEzNjF{IN88UU4> MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF{OUWxNUc,OjlzMkm1NVE9N2F-
K562 NEXVepdCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MWKyOEBpenN? MmjERY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCNNU[yJINmdGy|IHPvMZRz\WG2ZXSge4l1cCCyeYLhco95[W62aH;u[UBifCBzOkGgcY9t[XJicnH0bY8h[W[2ZYKgNlQhcHK|IHL5JG1VXCCjc4PhfUwhUUN3MDC9JFE6NjF2IN88UU4> MnXaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjlzMkm1NVEoRjJ7MUK5OVEyRC:jPh?=
HepG2 M3e1[GFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MX:yOEBpenN? MYLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEincFeyJINmdGy|IHPvMZRz\WG2ZXSge4l1cCCyeYLhco95[W62aH;u[UBifCBzOkGgcY9t[XJicnH0bY8h[W[2ZYKgNlQhcHK|IHL5JG1VXCCjc4PhfUwhUUN3MDC9JFIyNjJ3IN88UU4> MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF{OUWxNUc,OjlzMkm1NVE9N2F-
COLO320 NF[2cJVCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MkWwOFghcHK| MoLORY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCFT1zPN|IxKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDDR2s5KGG|c3H5MEBKSzVyIE2gN|kvPSEQvF2u M2DC[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{e2N|czLz5{OEO3OlM4OjxxYU6=
MDA-MB-231 MXrBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MoG4OFghcHK| MX7BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2GQT3NRk0zOzFiY3XscJMh[W[2ZYKgOFghcHK|IHL5JGNEUzhiYYPzZZktKEmFNUCgQUA1QC52IN88UU4> NYT4eFZNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkizO|Y{PzJpPkK4N|c3Ozd{PD;hQi=>
MDA-MB-231 M3LkUWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4LOTVI1KGi{cx?= NUjIeYFQT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hVUSDLV3CMVI{OSClZXzsd{Bi\nSncjCyOEBpenNiYomgUXRVKGG|c3H5MEBKSzVyIE2gOFgvPDJizszNMi=> NF3qOlA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OU[wPVEzOSd-Mkm2NFkyOjF:L3G+
MDA-MB-231 MXfBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NHTTZYszPCCqcoO= NXnnWGVbSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHHmeIVzKDJ2IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSB2OD60OEDPxE1w MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF{OUWxNUc,OjlzMkm1NVE9N2F-
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RD MULxTHRUKGG|c3H5 NXzpO|VVeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGLEJINmdGy| NVLuNGpTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-SH Mk\WdWhVWyCjc4PhfS=> NGDyboZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1UUCClZXzsdy=> NUHYb|U{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
MG 63 (6-TG R) NF3We|FyUFSVIHHzd4F6 NFLPRlFyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTVegOlMhMDZvVFegVkkh[2WubIO= MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
NB1643 M13MT5FJXFNiYYPzZZk> Mn;5dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE6EMU[0N{Bk\Wyucx?= MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Rh41 NUjFNFAzeUiWUzDhd5NigQ>? NXrB[ZhMeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGLoOFEh[2WubIO= Mo\qQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SK-N-MC MkSzdWhVWyCjc4PhfS=> NEf1UIZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1OSyClZXzsdy=> M{nWXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
MDA-MB-231 MYjBdI9xfG:|aYOgZZN{[Xl? MWSyOEB1dyB7NjD1US=> M1PFRVQ5KGi{cx?= M4S3UGlv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gbJVu[W5iTVTBMW1DNTJ|MTDj[YxteyCjc4Pld5Nm\CCjczDpcoNz\WG|ZTDpckBkdGWjdnXkJINie3Cjc3WtN{BmgHC{ZYPzbY9vKGG2IEK0JJRwKDl4IIXNJIFnfGW{IES4JIhzeyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM> MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDN5NkO3Nkc,Ojh|N{[zO|I9N2F-
MDA-MB-231 NWfwToc4SXCxcITvd4l{KGG|c3H5 M{jVcFI1KHSxIEm2JJVO MnXWOFghcHK| MWDJcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHj1cYFvKE2GQT3NRk0zOzFiY3XscJMh[XO|ZYPz[YQh[XNiaX7jdoVie2ViaX6gZ4xm[X[nZDDQRXJRKGyndnXsJIF1KDJ2IITvJFk3KHWPIHHmeIVzKDR6IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= MmG3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh|N{[zO|IoRjJ6M{e2N|czRC:jPh?=
MDA-MB-231 MnflSpVv[3Srb36gZZN{[Xl? NIPEVVYzPCC2bzC5OkB2VQ>? Ml3kOFghcHK| M3mwdWRm[3KnYYPlJIlvKGOjc4Dhd4UuOyCuZY\lcEBqdiCqdX3hckBOTEFvTVKtNlMyKGOnbHzzJIF1KDJ2IITvJFk3KHWPIHHmeIVzKDR6IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDN5NkO3Nkc,Ojh|N{[zO|I9N2F-
MDA-MB-231 NWrybINYTnWwY4Tpc44h[XO|YYm= MnjkNlQhfG9iOU[geW0> M{XVc|Q5KGi{cx?= NGjZRoNKdmO{ZXHz[UBqdiCyNUOgcIV3\WxiaX6gbJVu[W5iTVTBMW1DNTJ|MTDj[YxteyCjdDCyOEB1dyB7NjD1UUBi\nSncjC0PEBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDN5NkO3Nkc,Ojh|N{[zO|I9N2F-
MDA-MB-231 M3ryXmZ2dmO2aX;uJIF{e2G7 NUn6W3Q4OjRidH:gPVYhfU1? MVu0PEBpenN? NFrub5NF\WO{ZXHz[UBqdiClYYPwZZNmNTlibHX2[YwhcW5iaIXtZY4hVUSDLV3CMVI{OSClZXzsd{BifCB{NDD0c{A6PiC3TTDh[pRmeiB2ODDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz MlLaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh|N{[zO|IoRjJ6M{e2N|czRC:jPh?=
MDA-MB-231 MYDGeY5kfGmxbjDhd5NigQ>? MlzKNlQhfG9iOU[geW0> NUe4bFZIPDhiaILz NILZVHNF\WO{ZXHz[UBqdiCPRF2yJIxmfmWuIHnuJIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNiYYSgNlQhfG9iOU[geW0h[W[2ZYKgOFghcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDN5NkO3Nkc,Ojh|N{[zO|I9N2F-
HepG2 NUC0SGFzS2WubDDjfYNt\SCjcoLld5Qh[XO|YYm= MkTHNE4zKHWP MUSyOEBpenN? MXPD[YxtKGO7Y3zlJIFzemW|dDDpckBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyCjY3P1cZVt[XSrb36gZZQhWyCyaHHz[UBifCByLkKgeW0h[W[2ZYKgNlQhcHK|IHL5JJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnetZoF{\WRiZnzve{BkgXSxbXX0dolkKG2ndHjv[EBz\WyjdHn2[UB1dyClb370do9t MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF{OUWxNUc,OjlzMkm1NVE9N2F-
HepG2 NET1R3BE\WyuIHP5Z4xmKGG{cnXzeEBie3OjeR?= MkHONlQhcHK| MVnD[YxtKGO7Y3zlJIFzemW|dDDpckBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyCjY3P1cZVt[XSrb36gZZQhWyCyaHHz[UBkdy22cnXheIVlKHerdHigdJlz[W6xeHHueIhwdmViYYSgNVoyKG2xbHHyJJJifGmxIHHmeIVzKDJ2IHjyd{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oNWKjc3XkJIZtd3diY4n0c41mfHKrYzDt[ZRpd2R? MlrSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjlzMkm1NVEoRjJ7MUK5OVEyRC:jPh?=
HepG2 M3viXWFxd3C2b4Ppd{Bie3OjeR?= NF\PW|gxNjJidV2= NHnoe5IzPCCqcoO= MnTSTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCKZYDHNkBk\WyuczDhd5Nme3OnZDDhd{BqdmO{ZXHz[UBqdiClbHXheoVlKGOjc4Dhd4UuOyCuZY\lcJMh[XRiMD6yJJVOKGGodHXyJFI1KGi{czDifUBY\XO2ZYLuJIJtd3RibXX0bI9l NH:2fVA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUGyPVUyOSd-MkmxNlk2OTF:L3G+
HepG2 MUPBdI9xfG:|aYOgZZN{[Xl? M{DqVlAvOiC3TR?= NIrWdYUzPCCqcoO= NXXveYJ3UW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyCrbnPy[YF{\SCrbjDjcIVifmWmIHPhd5Bie2VvOTDs[ZZmdHNiYYSgNE4zKHWPIHHmeIVzKDJ2IHjyd{BjgSCZZYP0[ZJvKGKub4SgcYV1cG:m NIXRdYI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUGyPVUyOSd-MkmxNlk2OTF:L3G+
HepG2 MWHBdI9xfG:|aYOgZZN{[Xl? MoPWNlQhcHK| M4rZWWlv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gbJVu[W5iSHXwS|Ih[2WubIOgZZN{\XO|ZXSgZZMhcW6lcnXhd4UhcW5iY3zlZZZm\CCSQWLQJIxmfmWuczDjc{11emWjdHXkJJdqfGhicInyZY5wgGGwdHjvcoUh[XRiMUqxJI1wdGG{IILheIlwKGGodHXyJFI1KGi{czDifUBY\XO2ZYLuJIJtd3RibXX0bI9l MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF{OUWxNUc,OjlzMkm1NVE9N2F-
HepG2 Moe1RZBweHSxc3nzJIF{e2G7 NYLUUo46OC5{IIXN Mn3ZNlQhcHK| Mkm4TY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCKZYDHNkBk\WyuczDhd5Nme3OnZDDhd{BqdmO{ZXHz[UBqdiClbHXheoVlKFCDUmCgcIV3\Wy|IHH0JFAvOiC3TTDh[pRmeiB{NDDodpMh[nliV3XzeIVzdiCkbH;0JI1mfGixZB?= NGHIU|Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUGyPVUyOSd-MkmxNlk2OTF:L3G+
HepG2 M{LzVWFxd3C2b4Ppd{Bie3OjeR?= M37ENFI1KGi{cx?= MVnJcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHj1cYFvKEincFeyJINmdGy|IHHzd4V{e2WmIHHzJIlv[3KnYYPlJIlvKGOuZXH2[YQh[2G|cHHz[U0{KGyndnXsd{Bkdy22cnXheIVlKHerdHigdJlz[W6xeHHueIhwdmViYYSgNVoyKG2xbHHyJJJifGmxIHHmeIVzKDJ2IHjyd{BjgSCZZYP0[ZJvKGKub4SgcYV1cG:m NHLyemY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUGyPVUyOSd-MkmxNlk2OTF:L3G+
HepG2 M3X3d2Fxd3C2b4Ppd{Bie3OjeR?= M1PvSFI1KGi{cx?= NWS1fIxZUW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyCrbnPy[YF{\SCrbjDjcIVifmWmIHPhd5Bie2VvOTDs[ZZmdHNiY3:teJJm[XSnZDD3bZRpKHC7cnHuc5hidnSqb37lJIF1KDF8MTDtc4xieiC{YYTpc{Bi\nSncjCyOEBpenNiYomgW4V{fGW{bjDicI91KG2ndHjv[C=> MoDaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjlzMkm1NVEoRjJ7MUK5OVEyRC:jPh?=
HepG2 M{DYXGFxd3C2b4Ppd{Bie3OjeR?= MkDENlQhcHK| M4S0TGlv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gbJVu[W5iSHXwS|Ih[2WubIOgZZN{\XO|ZXSgZZMh\G:5boLl[5Vt[XSrb36gc4YhSmOuLYjMJIV5eHKnc4Ppc44h[29vdILlZZRm\CC5aYToJJB6emGwb4jhcpRpd26nIHH0JFE7OSCvb3zhdkBz[XSrbzDh[pRmeiB{NDDodpMh[nliV3XzeIVzdiCkbH;0JI1mfGixZB?= M2PPe|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUK5OVEyLz5{OUGyPVUyOTxxYU6=
HepG2 MVPBdI9xfG:|aYOgZZN{[Xl? MWmyOEBpenN? M{fPWmlv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gbJVu[W5iSHXwS|Ih[2WubIOgZZN{\XO|ZXSgZZMhfXC{ZXf1cIF1cW:wIH;mJGJq\CCneIDy[ZN{cW:wIHPvMZRz\WG2ZXSge4l1cCCyeYLhco95[W62aH;u[UBifCBzOkGgcY9t[XJicnH0bY8h[W[2ZYKgNlQhcHK|IHL5JHdme3Sncn6gZoxwfCCvZYToc4Q> M3XiWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUK5OVEyLz5{OUGyPVUyOTxxYU6=
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.
Animal Research:[4]
  • Animal Models: Chemical carcinogen (NMU) is injected into female Wistar rats.
  • Dosages: ≤300 mg/kg
  • Administration: Administered via i.p.

Solubility (25°C)

In vitro

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)

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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

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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