Vadimezan (ASA404)

For research use only.

Catalog No.S1537 Synonyms: NSC 640488, DMXAA

14 publications

Vadimezan (ASA404) Chemical Structure

CAS No. 117570-53-3

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.

Selleck's Vadimezan (ASA404) has been cited by 14 publications

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  • (B and C) sh-scrambled or sh-ck2a–transducted L929 cells (B) and Raw cells (C) were stimulated by DMXAA (100 μg/ml) for various times. Cytosolic and nuclear extracts were prepared as described in Materials and Methods. Five percent of the cytosolic proteins and 20% of the nuclear proteins were resolved by 10% SDS-PAGE. Subsequently, immunoblotting was conducted by indicated Abs. The amounts of Tubulin and Lamin B1 in cytosol versus nuclei detected by respective Abs were used as internal control for fractionation.

    J Immunol, 2015, 194:4477-4488. Vadimezan (ASA404) purchased from Selleck.

  • (E) WT and ASC−/− macrophages were stimulated with 1 μg/ml of tumor-derived DNA in the presence of lipofectamine or 50 μg/ml of DMXAA at different time points. Whole cell extracts were analysed with antibodies against pTBK1, total TBK1, pIRF3, total IRF3 and GAPDH.

    J Immunol, 2016, 196(7):3191-8. Vadimezan (ASA404) purchased from Selleck.

  • (B and C) sh-scrambled or sh-ck2α–transducted L929 cells (B) and Raw cells (C) were stimulated by DMXAA (100 μg/ml) for various times. Cytosolic and nuclear extracts were prepared as described in Materials and Methods. Five percent of the cytosolic proteins and 20% of the nuclear proteins were resolved by 10% SDS-PAGE. Subsequently, immunoblotting was conducted by indicated Abs. The amounts of Tubulin and Lamin B1 in cytosol versus nuclei detected by respective Abs were used as internal control for fractionation.

    J Immunol, 2015, 194(9):4477-88. Vadimezan (ASA404) purchased from Selleck.

  • (b-e) HEK293T cells were transiently transfected with empty vector (b), plasmids encoding hSTING(H232) (c), hSTING(R232) (d), or mSTING (e) together with IFNβ-luciferase reporter. After 24 h, cells were transfected with 2′,3′‐cGAMP (2 μg/mL) or stimulated with CMA (50 μg/mL), DMXAA (50 μM) and α-mangostin. Luciferase activity was measured 24 h after stimulation. Error bars represent the SD of independent experiments (n=3); *P<0.05, **P<0.01, ***P<0.001 (Student's t-test).

    ChemMedChem, 2018, 13(19):2057-2064. Vadimezan (ASA404) purchased from Selleck.

  • (A) 24 h after incubation of co-culture of B16.F10 cells and TAMs with different concentrations of DMXAA; (B) 24 h after incubation of co-culture of B16.F10 cells and TAMs with different concentrations of SIM administered alone or in combination with 100 μM DMXAA; (C) 24 h after incubation of mono-cultured B16.F10 cells with 100 μM DMXAA administered alone and with different concentrations of SIM administered alone or in combination with 100 μM DMXAA. Data are shown as mean ± SD of triplicate measurements; DMXAA: cells incubated with different concentrations of DMXAA; SIM: cells incubated with different concentrations of SIM; SIM+ 100 μM DMXAA: cells incubated with different concentrations of SIM administered in combination with 100 μM DMXAA; The two-way ANOVA Multiple Comparison Test with Bonferroni post-tests was used to compare overall effects of different drug concentrations (*, P<0.05; **, P<0.01; ***, P<0.001).

    PLoS One, 2018, 13(8):e0202827. Vadimezan (ASA404) purchased from Selleck.

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 NUXpd5JmS3m2b4TvfIlkyqCjc4PhfS=> MnP5NlQhcA>? NXjLd21lS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSkpiY3XscJMh[W[2ZYKgNlQhcHK|IHL5JG1VXCCjc4PhfUwhS0N3ME20PE46KM7:TR?= NGPpe|Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEWxPFI6PSd-MkS1NVgzQTV:L3G+
HECPP cells NH3XO5BHfW6ldHnvckBie3OjeR?= M3S2elExKHWpL33M NX;DTZFxSWO2aY\heIlwdiCxZjDOSk1s[XCyYVKgbY4hUEWFUGCgZ4VtdHNiYYSgNVAhfWdxbVy= NGfjW2E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{[xOlEyPCd-MUe2NVYyOTR:L3G+
MCF7 NWO0NWU2SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MWeyOEBpenN? MmO5RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3JINmdGy|IHPvMZRz\WG2ZXSge4l1cCCyeYLhco95[W62aH;u[UBifCBzOkGgcY9t[XJicnH0bY8h[W[2ZYKgNlQhcHK|IHL5JG1VXCCjc4PhfUwhUUN3MDC9JFEyNjh7IN88UU4> NGDOOY89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUGyPVUyOSd-MkmxNlk2OTF:L3G+
MDA-MB-231 NGD1PG1CdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M1\HdVI1KGi{cx?= M2PTN2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTJ|MTDj[YxteyClbz30doVifGWmIIfpeIgheHm{YX7vfIFvfGixbnWgZZQhOTpzIH3vcIFzKHKjdHnvJIFnfGW{IEK0JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTBiPTCxNk4yOiEQvF2u MlLiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjlzMkm1NVEoRjJ7MUK5OVEyRC:jPh?=
K562 MYjBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NHrZOHAzPCCqcoO= NGrrd4lCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFu1OlIh[2WubIOgZ48ufHKnYYTl[EB4cXSqIID5doFvd3ijboToc45mKGG2IEG6NUBud2yjcjDyZZRqdyCjZoTldkAzPCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOTlwMUSg{txONg>? M2D3flxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUK5OVEyLz5{OUGyPVUyOTxxYU6=
HepG2 MUnBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NEnYenkzPCCqcoO= M{XZOWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSHXwS|Ih[2WubIOgZ48ufHKnYYTl[EB4cXSqIID5doFvd3ijboToc45mKGG2IEG6NUBud2yjcjDyZZRqdyCjZoTldkAzPCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOjFwMkWg{txONg>? NH7yNmw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUGyPVUyOSd-MkmxNlk2OTF:L3G+
COLO320 MXzBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MXO0PEBpenN? MUnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEORTF:zNlAh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IFPDT|gh[XO|YYmsJGlEPTBiPTCzPU42KM7:TT6= MkXCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh|N{[zO|IoRjJ6M{e2N|czRC:jPh?=
MDA-MB-231 NHrsSmxCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NWPMTWNrPDhiaILz M3fISWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTJ|MTDj[YxteyCjZoTldkA1QCCqcoOgZpkhS0ONODDhd5NigSxiSVO1NEA:KDR6LkSg{txONg>? MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDN5NkO3Nkc,Ojh|N{[zO|I9N2F-
MDA-MB-231 MXHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NX\jXWx4OjRiaILz NU\HPG1LT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hVUSDLV3CMVI{OSClZXzsd{Bi\nSncjCyOEBpenNiYomgUXRVKGG|c3H5MEBKSzVyIE2gOFgvPDJizszNMi=> NIPFO2c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OU[wPVEzOSd-Mkm2NFkyOjF:L3G+
MDA-MB-231 NE\SeWlCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NV\qe2RDOjRiaILz NHvNNWdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNiYX\0[ZIhOjRiaILzJIJ6KE2WVDDhd5NigSxiSVO1NEA:KDR6LkS0JO69VS5? MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF{OUWxNUc,OjlzMkm1NVE9N2F-
A673 M3TnW5FJXFNiYYPzZZk> MWLxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSTZ5MzDj[Yxtew>? MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
DAOY M{\aNpFJXFNiYYPzZZk> NXS3ZndWeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFTBU3kh[2WubIO= MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
RD M4m2eJFJXFNiYYPzZZk> NHLObW9yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUlSgZ4VtdHN? M{\KeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-SH NWP0TmN4eUiWUzDhd5NigQ>? NIDlRW1yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1UUCClZXzsdy=> MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
MG 63 (6-TG R) Mk\FdWhVWyCjc4PhfS=> MUfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVUdiNkOgLFYuXEdiUjmgZ4VtdHN? MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
NB1643 M4TQV5FJXFNiYYPzZZk> NFe1Oo5yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKxOlQ{KGOnbHzz M4nGfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Rh41 MYXxTHRUKGG|c3H5 MnvCdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqNEGgZ4VtdHN? NEPkTJI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SK-N-MC NGTPR2tyUFSVIHHzd4F6 MmO0dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tUWMh[2WubIO= MlLVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
MDA-MB-231 NUX6eWFuSXCxcITvd4l{KGG|c3H5 NVu2PXFrOjRidH:gPVYhfU1? MWi0PEBpenN? NU\1NGlZUW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHHzd4V{e2WmIHHzJIlv[3KnYYPlJIlvKGOuZXH2[YQh[2G|cHHz[U0{KGW6cILld5Nqd25iYYSgNlQhfG9iOU[geW0h[W[2ZYKgOFghcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? NEexPIc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEO3OlM4Oid-MkizO|Y{PzJ:L3G+
MDA-MB-231 Mk\WRZBweHSxc3nzJIF{e2G7 MnHwNlQhfG9iOU[geW0> MlPNOFghcHK| M2HFZWlv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gbJVu[W5iTVTBMW1DNTJ|MTDj[YxteyCjc4Pld5Nm\CCjczDpcoNz\WG|ZTDpckBkdGWjdnXkJHBCWlBibHX2[Ywh[XRiMkSgeI8hQTZidV2gZYZ1\XJiNEigbJJ{KGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=> MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDN5NkO3Nkc,Ojh|N{[zO|I9N2F-
MDA-MB-231 MYDGeY5kfGmxbjDhd5NigQ>? MX2yOEB1dyB7NjD1US=> MkLMOFghcHK| NEPscYxF\WO{ZXHz[UBqdiClYYPwZZNmNTNibHX2[YwhcW5iaIXtZY4hVUSDLV3CMVI{OSClZXzsd{BifCB{NDD0c{A6PiC3TTDh[pRmeiB2ODDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz MorCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh|N{[zO|IoRjJ6M{e2N|czRC:jPh?=
MDA-MB-231 MUPGeY5kfGmxbjDhd5NigQ>? M3i3WlI1KHSxIEm2JJVO NHjGUWU1QCCqcoO= MYfJcoNz\WG|ZTDpckBxPTNibHX2[YwhcW5iaIXtZY4hVUSDLV3CMVI{OSClZXzsd{BifCB{NDD0c{A6PiC3TTDh[pRmeiB2ODDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz MnfPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh|N{[zO|IoRjJ6M{e2N|czRC:jPh?=
MDA-MB-231 NULXc45STnWwY4Tpc44h[XO|YYm= NWez[21OOjRidH:gPVYhfU1? NFLLNpE1QCCqcoO= NH:3XFlF\WO{ZXHz[UBqdiClYYPwZZNmNTlibHX2[YwhcW5iaIXtZY4hVUSDLV3CMVI{OSClZXzsd{BifCB{NDD0c{A6PiC3TTDh[pRmeiB2ODDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz M3;qTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{e2N|czLz5{OEO3OlM4OjxxYU6=
MDA-MB-231 NGe3dplHfW6ldHnvckBie3OjeR?= M3[xW|I1KHSxIEm2JJVO M1fxblQ5KGi{cx?= M4rSU2Rm[3KnYYPlJIlvKE2GTUKgcIV3\WxiaX6gbJVu[W5iTVTBMW1DNTJ|MTDj[YxteyCjdDCyOEB1dyB7NjD1UUBi\nSncjC0PEBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ M4CwPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{e2N|czLz5{OEO3OlM4OjxxYU6=
HepG2 Mn;iR4VtdCCleXPs[UBienKnc4SgZZN{[Xl? NIiyenQxNjJidV2= MUGyOEBpenN? NYHKZ4k6S2WubDDjfYNt\SCjcoLld5QhcW5iaIXtZY4hUGWyR{KgZ4VtdHNiYYPz[ZN{\WRiYYOgZYNkfW23bHH0bY9vKGG2IGOgdIhie2ViYYSgNE4zKHWPIHHmeIVzKDJ2IHjyd{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oNWKjc3XkJIZtd3diY4n0c41mfHKrYzDt[ZRpd2RicnXsZZRqfmVidH:gZ49vfHKxbB?= Mk\zQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjlzMkm1NVEoRjJ7MUK5OVEyRC:jPh?=
HepG2 MYjD[YxtKGO7Y3zlJIFzemW|dDDhd5NigQ>? Mk\aNlQhcHK| NEPscIhE\WyuIHP5Z4xmKGG{cnXzeEBqdiCqdX3hckBJ\XCJMjDj[YxteyCjc4Pld5Nm\CCjczDhZ4N2dXWuYYTpc44h[XRiUzDwbIF{\SClbz30doVifGWmIIfpeIgheHm{YX7vfIFvfGixbnWgZZQhOTpzIH3vcIFzKHKjdHnvJIFnfGW{IEK0JIhzeyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pLXLhd4VlKG[ub4egZ5l1d22ndILpZ{Bu\XSqb3S= NUnuWlVLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmxNlk2OTFpPkK5NVI6PTFzPD;hQi=>
HepG2 MXXBdI9xfG:|aYOgZZN{[Xl? M3noOVAvOiC3TR?= MWWyOEBpenN? MVnJcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHj1cYFvKEincFeyJINmdGy|IHHzd4V{e2WmIHHzJIlv[3KnYYPlJIlvKGOuZXH2[YQh[2G|cHHz[U0{KGyndnXsd{BifCByLkKgeW0h[W[2ZYKgNlQhcHK|IHL5JHdme3Sncn6gZoxwfCCvZYToc4Q> MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF{OUWxNUc,OjlzMkm1NVE9N2F-
HepG2 NULXbWU{SXCxcITvd4l{KGG|c3H5 MYWwMlIhfU1? M1fjNFI1KGi{cx?= NVe2bIx{UW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyCrbnPy[YF{\SCrbjDjcIVifmWmIHPhd5Bie2VvOTDs[ZZmdHNiYYSgNE4zKHWPIHHmeIVzKDJ2IHjyd{BjgSCZZYP0[ZJvKGKub4SgcYV1cG:m M1r3XlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUK5OVEyLz5{OUGyPVUyOTxxYU6=
HepG2 MXfBdI9xfG:|aYOgZZN{[Xl? MW[yOEBpenN? M4\iTmlv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gbJVu[W5iSHXwS|Ih[2WubIOgZZN{\XO|ZXSgZZMhcW6lcnXhd4UhcW5iY3zlZZZm\CCSQWLQJIxmfmWuczDjc{11emWjdHXkJJdqfGhicInyZY5wgGGwdHjvcoUh[XRiMUqxJI1wdGG{IILheIlwKGGodHXyJFI1KGi{czDifUBY\XO2ZYLuJIJtd3RibXX0bI9l NUHyWVdjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmxNlk2OTFpPkK5NVI6PTFzPD;hQi=>
HepG2 M130R2Fxd3C2b4Ppd{Bie3OjeR?= NVPMOpVMOC5{IIXN MUSyOEBpenN? NFGyd2dKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIFjldGczKGOnbHzzJIF{e2W|c3XkJIF{KGmwY4LlZZNmKGmwIHPs[YF3\WRiUFHSVEBt\X[nbIOgZZQhOC5{IIXNJIFnfGW{IEK0JIhzeyCkeTDX[ZN1\XKwIHLsc5QhdWW2aH;k MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF{OUWxNUc,OjlzMkm1NVE9N2F-
HepG2 MXPBdI9xfG:|aYOgZZN{[Xl? MknPNlQhcHK| NIXiXI1KdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIFjldGczKGOnbHzzJIF{e2W|c3XkJIF{KGmwY4LlZZNmKGmwIHPs[YF3\WRiY3HzdIF{\S1|IHzleoVteyClbz30doVifGWmIIfpeIgheHm{YX7vfIFvfGixbnWgZZQhOTpzIH3vcIFzKHKjdHnvJIFnfGW{IEK0JIhzeyCkeTDX[ZN1\XKwIHLsc5QhdWW2aH;k MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF{OUWxNUc,OjlzMkm1NVE9N2F-
HepG2 MWrBdI9xfG:|aYOgZZN{[Xl? MlPCNlQhcHK| NG\FV|hKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIFjldGczKGOnbHzzJIF{e2W|c3XkJIF{KGmwY4LlZZNmKGmwIHPs[YF3\WRiY3HzdIF{\S17IHzleoVteyClbz30doVifGWmIIfpeIgheHm{YX7vfIFvfGixbnWgZZQhOTpzIH3vcIFzKHKjdHnvJIFnfGW{IEK0JIhzeyCkeTDX[ZN1\XKwIHLsc5QhdWW2aH;k NH\zdHM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUGyPVUyOSd-MkmxNlk2OTF:L3G+
HepG2 NHzvXWVCeG:ydH;zbZMh[XO|YYm= M2rYT|I1KGi{cx?= MYPJcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHj1cYFvKEincFeyJINmdGy|IHHzd4V{e2WmIHHzJIRwf26{ZXf1cIF1cW:wIH;mJGJkdC26TDDlfJBz\XO|aX;uJINwNXS{ZXH0[YQhf2m2aDDwfZJidm:6YX70bI9v\SCjdDCxPlEhdW:uYYKgdoF1cW9iYX\0[ZIhOjRiaILzJIJ6KFenc4Tldo4h[myxdDDt[ZRpd2R? NFz3Vno9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUGyPVUyOSd-MkmxNlk2OTF:L3G+
HepG2 NETTPIxCeG:ydH;zbZMh[XO|YYm= MV6yOEBpenN? NHTtNZJKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIFjldGczKGOnbHzzJIF{e2W|c3XkJIF{KHWycnXneYxifGmxbjDv[kBDcWRiZYjwdoV{e2mxbjDjc{11emWjdHXkJJdqfGhicInyZY5wgGGwdHjvcoUh[XRiMUqxJI1wdGG{IILheIlwKGGodHXyJFI1KGi{czDifUBY\XO2ZYLuJIJtd3RibXX0bI9l NXvOO20{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmxNlk2OTFpPkK5NVI6PTFzPD;hQi=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-p38 / p38 ; 

PubMed: 21819972     


Mouse macrophages (MHS) were stimulated with 20 µg/ml DMXAA in culture. At various time points, the culture supernatants and the cells were collected and assayed for amount of p38 phosphorylation with immunoblots. 

p-MK2 / pERK / p-JNK ; 

PubMed: 21819972     


Mouse macrophages (MHS) were pre-exposed to IFN-γ, followed by DMXAA treatment at 20 µg/ml. The cells also extracted to determine the effect of IFN-γ priming on DMXAA-induced MAPK pathways activation.

21819972
Growth inhibition assay
Cell proliferation ; 

PubMed: 30138430     


24 h after incubation of co-culture of B16.F10 cells and TAMs with different concentrations of DMXAA; 

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

Kinase Assay:[1]
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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]
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  • 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]
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  • 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 powder
in solvent
Synonyms NSC 640488, DMXAA
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)
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Step 2: Enter the in vivo formulation ()
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Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
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    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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

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

Tel: +1-832-582-8158 Ext:3

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VDA Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID