Temozolomide

For research use only.

Catalog No.S1237 Synonyms: CCRG81045, NSC 362856,TMZ

70 publications

Temozolomide Chemical Structure

Molecular Weight(MW): 194.15

Temozolomide is a monofunctional SN-1 alkylating agent that can modify nitrogen atoms in the DNA ring and the extracyclic oxygen group, chemically converted to MTIC and degrades to methyldiazonium cation, which transfers methyl groups to DNA at physiologic pH. A DNA damage inducer in L-1210 and L-1210/BCNU cells. Temozolomide induces apoptosis and exhibits antitumor activity.

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Selleck's Temozolomide has been cited by 70 publications

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Biological Activity

Description Temozolomide is a monofunctional SN-1 alkylating agent that can modify nitrogen atoms in the DNA ring and the extracyclic oxygen group, chemically converted to MTIC and degrades to methyldiazonium cation, which transfers methyl groups to DNA at physiologic pH. A DNA damage inducer in L-1210 and L-1210/BCNU cells. Temozolomide induces apoptosis and exhibits antitumor activity.
Features Methazolastone is a second-generation alkylating agent.
Targets
DNA replication [1]
(L-1210, L-1210/BCNU cells)
In vitro

Methazolastone causes formation of DNA alkali-labile sites which are present in similar amounts and repaired at a similar rate in L-1210 and L-1210/BCNU cell lines. In L-1210 but not in L-1210/BCNU methazolastone induces an arrest of cells in SL-G2-M phases.[1] Methazolastone sensitivity of both chemo-sensitive and resistant cells (D54-R and U87-R) is enhanced significantly under hyperoxia. Both Methazolastone and hyperoxia are associated with increased phosphorylation of ERK p44/42 MAPK (Erk1/2), but to a lesser extent in D54-R cells, suggesting that Erk1/2 activity may be involved in regulation of hyperoxia and Methazolastone-mediated cell death. Hyperoxia enhances Methazolastone toxicity in GBM cells by induction of apoptosis, possibly via MAPK-related pathways. [2] Methazolastone induces in monocytes the DNA damage response pathways ATM-Chk2 and ATR-Chk1 resulting in p53 activation. [3] Chronic Methazolastone exposure results in acquired Methazolastone-resistance and elevates miR-21 expression. [4] Methazolastone treatment triggers endoplasmic reticula (ER) stress with increased expression of GADD153 and GRP78 proteins, and deceases pro-caspase 12 protein. Methazolastone induces autophagy through mitochondrial damage- and ER stress-dependent mechanisms to protect glioma cells. [5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Kelly NH7Y[pdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TuXlQ5KGh? NHj4cpVKSzVyPUGzPU4zOOLCidMx5qCKPS57NTFOwG0> MVeyOVk3ODJ6Mh?=
KellyCis83 Mn3DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1Xpd|Q5KGh? NYXO[FhkUUN3ME2yOVEvODEkgJpCtgKBkTF3Lke1JO69VQ>? M2nYeFI2QTZyMkiy
SK-N-AS M3e4fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnyU4E1QCCq M2\zTGlEPTB;MkK3Mlcx6oDLwsJihKkzOi5zNTFOwG0> NUXEd41DOjV7NkCyPFI>
SK-N-ASCis24 M{jQ[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXOOFghcA>? MUTJR|UxRTR6MD62NQKBkcLz4pEJNVAyNjF3IN88US=> M3;ZUVI2QTZyMkiy
CHP-212 M3vMU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXniN5ZVPDhiaB?= NGHRXWRKSzVyPUeuPVfjiIoEsfMAjVAvPjlizszN MUKyOVk3ODJ6Mh?=
CHP-212Cis100 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fvbVQ5KGh? MnfrTWM2OD17LkW15qCKyrIkgJmwMlg5KM7:TR?= NHW5fHMzPTl4MEK4Ni=>
U87  NWD2U|VwTnWwY4Tpc44hSXO|YYm= MUSxNFAh|ryP NWTwOWxQOjRvN{KgbC=> M3H3PYlv\HWlZYOgSINTOSCneIDy[ZN{cW:w NULCdFhZOjV6MEi4Olg>
LN229 Ml;uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml:5NE02OCEQvF2= NUj2[lFjUUN3ME2xOkDPxE1? M{Hh[VI2PzVyMkez
TR-LN229 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFHKVmcxNTVyIN88US=> NVLYeWE2UUN3ME23O{DPxE1? M1z4[VI2PzVyMkez
U87  MXzBdI9xfG:|aYOgRZN{[Xl? MXuw5qCUOjBy4pEJxtVO NFLBeHYzPCCq NWP2OYJV\W6qYX7j[ZMhS1FiaX7keYNm\CCjcH;weI9{cXN? Ml;VNlU3QDF4Nki=
U251MG M1K4R2Fxd3C2b4Ppd{BCe3OjeR?= NIH2bGQyODEEoN88US=> MmfiOFghcA>? MYXQRnM> NVLEWIF4cW6mdXPld{BieG:ydH;zbZM> M{\IPFI2PjhyNE[0
U87MG NVrFZmxISXCxcITvd4l{KEG|c3H5 NVT0Z2c2OTBywrFOwG0> M3vFb|Q5KGh? NU\N[IN4WEKV MXvpcoR2[2W|IHHwc5B1d3Orcx?= M1X0d|I2PjhyNE[0
U87 NXzqfpNsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVSyR3g5PTBvM{WwJO69VQ>? MX[0POKhcMLi MX7pcohq[mm2czDj[YxtKGe{b4f0bEB{dGmpaITsfS=> MWCyOVU2PDJ{Mx?=
U118  M4jwNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV[1NE0{PTBizszN NEnHSmM1QMLiaNMg MXfpcohq[mm2czDj[YxtKGe{b4f0bEB{dGmpaITsfS=> MoLUNlU2PTR{MkO=
U87 M3X4RWZ2dmO2aX;uJGF{e2G7 NUnjOY52OjVyL{O1NEDPxE1? M3GwNlQ5yqCqwrC= MnvI[Y5p[W6lZYOgWG1ZNWmwZIXj[YQheC2SS1OtdIFvKGSnY4LlZZNm M17icFI2PTV2MkKz
U118  MnzESpVv[3Srb36gRZN{[Xl? NIn1WYEzPTBxM{WwJO69VQ>? NF3zcYM1QMLiaNMg NHjSXFRmdmijbnPld{BVVVhvaX7keYNm\CCyLWDLR{1x[W5iZHXjdoVie2V? NHr3bZkzPTV3NEKyNy=>
U87 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFXFVo4zPTBxM{WwJO69VQ>? M4LDTFQ5yqCqwrC= M{Pkfolv[3KnYYPld{B1cGVicHXyZ4VvfGGpZTDv[kBk\WyuczDpckBUKGGwZDDHNk9OyqClb4Ty[YF1\WRid3n0bEBVVVh? MYeyOVU2PDJ{Mx?=
A375 NXK0Olc6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\MOFjDqGkEoB?= NITnOHZKSzVyPUK2OUDPxE1? NInxS2czPTV{NEW1Ni=>
A2058 NGKwbldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUO0POKhcMLi MVrJR|UxRTF{IN88US=> MkXuNlU2OjR3NUK=
M238 NWXvdWp3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH3IOFQ1QMLiaNMg MmHITWM2OD12MDFOwG0> MXmyOVUzPDV3Mh?=
M249 MmXNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1TpdFQ5yqCqwrC= MYXJR|UxRTJ3NDFOwG0> MmfRNlU2OjR3NUK=
M21 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjK[ndpPDkEoHlCpC=> MnfnTWM2OD1{MkGg{txO MX:yOVUzPDV3Mh?=
U251 M2DjSGN6fG:2b4jpeJkhSXO|YYm= NFG0[FMzOCEQvF5CpC=> M4PnNFQ5yqCqwrC= NXPZeGkyemWmdXPl[JMhfGinIIDldoNmdnSjZ3XzJI9nKGOxbH;ubYV{KG[xcn3l[C=> MnHONlU1OzR|OEG=
LN229 MmniR5l1d3SxeHn0fUBCe3OjeR?= MVOyNEDPxE4EoB?= NEW0fpo1QMLiaNMg MlftdoVlfWOnZIOgeIhmKHCncnPlcpRi\2W|IH;mJINwdG:waXXzJIZwem2nZB?= MXKyOVQ{PDN6MR?=
U373MG-LUC MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DWfVczKGh? M2HkeGlEPTB-NkCwJO69VQ>? M37aUVI2PDNzOUWz
U87  M2jpVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWq2UFA2OjVvMkCwJO69VQ>? NXnVRmZkPDkEoHlCpC=> MVTpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M1jSNlI2PDByN{S1
U251 NXPMblJqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGX5cYEzPS1{MECg{txO MlXUOFjDqGkEoB?= NYDLWJV6cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NV:yemo6OjV2MEC3OFU>
U251 MofwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MofENVAxNTRyMDFOwG0> NGLFZno4Oi97NjDo MmXXeIhmKGGwdHmtdJJwdGmoZYLheIl3\SCnZn\lZ5Qh[2GwIHLlJIVvcGGwY3XkJIJ6KGexc4P5dI9tKGWwaHHuZ4VlKMLi M{D3T|I2Ozd3Mkex
U373 MmjsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkmyNVAxNTRyMDFOwG0> MkfzO|IwQTZiaB?= NUft[3MxfGinIHHueIkueHKxbHnm[ZJifGm4ZTDl[oZm[3RiY3HuJIJmKGWwaHHuZ4VlKGK7IHfvd5N6eG:uIHXubIFv[2WmINMg M13UW|I2Ozd3Mkex
U343 NYrCPG9uT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYe0[JpZOTByLUSwNEDPxE1? NFzMbHI4Oi97NjDo MoLKeIhmKGGwdHmtdJJwdGmoZYLheIl3\SCnZn\lZ5Qh[2GwIHLlJIVvcGGwY3XkJIJ6KGexc4P5dI9tKGWwaHHuZ4VlKMLi NHuweoczPTN5NUK3NS=>
U87MG-luc2 NHPocHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XIR|ExOC12MECg{txO MYS3Nk86PiCq MVj0bIUh[W62aT3wdo9tcW[ncnH0bZZmKGWoZnXjeEBk[W5iYnWg[Y5p[W6lZXSgZpkh\2:|c4nwc4wh\W6qYX7j[YQhyqB? MmroNlU{PzV{N{G=
U87 Mn;uSpVv[3Srb36gRZN{[Xl? NFjLSnozODBizszN NV7nVopNPDhiaB?= NXfCZm51cW6lcnXhd4V{KEKUQ1OzJI1TVkFiZYjwdoV{e2mxbh?= MUmyOVM{Pzd{MR?=
U251 MWXGeY5kfGmxbjDBd5NigQ>? MXeyNFAh|ryP MkfhOFghcA>? MlTCbY5kemWjc3XzJGJTS0N|IH3SUmEh\XiycnXzd4lwdg>? M3n4TFI2OzN5N{Kx
A172 M3XhXGZ2dmO2aX;uJGF{e2G7 M2HaclIxOCEQvF2= MYm0PEBp NF3kR3JqdmO{ZXHz[ZMhSlKFQ{OgcXJPSSCneIDy[ZN{cW:w MUCyOVM{Pzd{MR?=
U251 MX;GeY5kfGmxbjDBd5NigQ>? NX25W4dFOjByIN88US=> NX7vWYxFPDhiaB?= M2n2VYlv[3KnYYPld{B1cGViZYjwdoV{e2mxbjDv[kBDWkODMTygRnJESTJuIGLBSFUyKGGwZDDGRW5ETDJ? M4e3SlI2OzN5N{Kx
A172 NFrHTmJHfW6ldHnvckBCe3OjeR?= NFjv[YIzODBizszN M2m0UVQ5KGh? NYTodmZ{cW6lcnXhd4V{KHSqZTDlfJBz\XO|aX;uJI9nKEKUQ1GxMEBDWkODMjygVmFFPTFiYX7kJGZCVkOGMh?= NX7jfVB4OjV|M{e3NlE>
U87 M3XK[WZ2dmO2aX;uJGF{e2G7 NEn5[IYzODBizszN MV6yOE84Oi9zMkCgbC=> MXrpcoNz\WG|ZYOg{tNJOkG[IH\vZ4kh\m:{bXH0bY9vKHSrbXWt[IVx\W6mZX70cJk> Mn7vNlU{Ozd5MkG=
U251 M2fQTmZ2dmO2aX;uJGF{e2G7 MWSyNFAh|ryP NHvTUIUzPC95Mj:xNlAhcA>? NFvpe5JqdmO{ZXHz[ZMh|rOKMlHYJIZw[2liZn;ycYF1cW:wIITpcYUu\GWyZX7k[Y51dHl? NELp[WIzPTN|N{eyNS=>
A172 M{TMTmZ2dmO2aX;uJGF{e2G7 MnPWNlAxKM7:TR?= Mlm1NlQwPzJxMUKwJIg> NYnXb3N1cW6lcnXhd4V{KM7|SELBXEBnd2OrIH\vdo1ifGmxbjD0bY1mNWSncHXu[IVvfGy7 NEjvR|AzPTN|N{eyNS=>
SNB19V MnziS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDkVopmPyCm NFPMWpRFVVOR MmfqS2k2OD1|NT63xtEyOiEQvF2= NIjDengzPTJ5N{S0NS=>
SNB19M MkG1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV23JIQ> NYewRYcyTE2VTx?= MkHPS2k2OD12NkmuPeKyQDhizszN NFfsRZAzPTJ5N{S0NS=>
SNB19VR NXzP[mF7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXy3JIQ> MYPEUXNQ MVvHTVUxRTJ6MD6yxtEyQCEQvF2= MoD6NlUzPzd2NEG=
U373V MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV23JIQ> NXfRPXhMTE2VTx?= MV;HTVUxRTZ6LkFCtVMzKM7:TR?= MVyyOVI4PzR2MR?=
U373M MlLMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPBO{Bl NFTtfXBFVVOR M2rDTGdKPTB;M{[4MlfDuTh4IN88US=> MYeyOVI4PzR2MR?=
U373VR Mnm3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7sdZVnPyCm NHH2T2tFVVOR NEe4TXdIUTVyPUK4PE45yrF|MzFOwG0> M{TuZ|I2Ojd5NESx
U87MG M1[yb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1K0U|ch\A>? NFj6UnJFVVOR M{DHTGdKPTB;M{iuN:KyOjBizszN NUeyRZlDOjV{N{e0OFE>
HCT116 NV3sXWJ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4TpNlch\A>? M1;pZ2ROW09? M4roUWdKPTB;NUe5MlnDuTN{IN88US=> M2XIUFI2Ojd5NESx
DLD1 Ml;NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\rTFch\A>? NVvCfphiTE2VTx?= MVrHTVUxRTVyMT60xtE6OyEQvF2= NH\EWo8zPTJ5N{S0NS=>
MRC5 M2nU[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3aUGo4KGR? NE\NbVdFVVOR NEfkT3JIUTVyPUS0PU41yrF6IN88US=> MoLPNlUzPzd2NEG=
SNB19V  Ml6zSpVv[3Srb36gRZN{[Xl? NWThRWc2OTByIN88UeKhXE2c MnPFNE04OiCq MlLSbY5kemWjc3XzJO6{UDKDWDDlfJBz\XO|aX;uJIJmfHenZX6gNVYh[W6mIEeyJIg> NWHiT4pKOjV{N{e0OFE>
T98G  MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXm1M|ExNzF3IN88US=> NU\BVXNDOjUEoHi= MWXpcoR2[2W|IHPlcIwh\GWjdHig[I9{\S2mZYDlcoRmdnSueTDh[pRmeiClb37jc41qfGGwdD30[Y1wgm:ub33p[IUhf2m2aDDOVIU3NVCGVB?= MUKyOVI3Ojl4MR?=
U251  Mk\YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PKTlUwOTBxMUWg{txO MorLNlTDqGh? MlvzbY5lfWOnczDj[YxtKGSnYYToJIRwe2VvZHXw[Y5l\W62bImgZYZ1\XJiY3;uZ49ucXSjboSteIVud3qxbH;tbYRmKHerdHigUnBmPi2SRGS= NF\BUnkzPTJ4Mkm2NS=>
T98G  MYnGeY5kfGmxbjDBd5NigQ>? NFvBcFQyPSEQvF2= NUjrdHlXOjUEoHi= NW[4eVI5cW6lcnXhd4V{KESQQT3mdoFodWWwdHH0bY9vKGmwIF7Q[VYuWESWIITy[YF1\WRiZ3zpc41iKGOnbHzz NFuxSY0zPTJ4Mkm2NS=>
U251  M1q4[mZ2dmO2aX;uJGF{e2G7 Mn7VNVUh|ryP MnLrNlTDqGh? MUHpcoNz\WG|ZYOgSG5CNW[{YXft[Y51[XSrb36gbY4hVlCnNj3QSHQhfHKnYYTl[EBodGmxbXGgZ4VtdHN? MXqyOVI3Ojl4MR?=
U-87 MG NGO2N2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY[3NkBp M{LC[GlEPTB;MD65N{BuVcLi NVGxc4ZSOjV{NEWzN|I>
U-118 MG NHewV5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1jPOlczKGh? M4[5PGlEPTB;MT6wOUBuVcLi NFLYdYszPTJ2NUOzNi=>
U87 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zYXVI1KGh? NW\BPGJ1UUN3ME2yOlAvOzRizszNxsA> MVmyOVE4OzJ|Mx?=
U87 GSLCs NHjrU|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX[yOEBp MnT3TWM2OD15Nk[uNVEh|ryPwrC= NWHsXppqOjVzN{OyN|M>
U87MG MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1jmbFczKGh? NHKxWIlKSzVyPUG1MlYzPSEQvF5CpC=> MXmyOVA2ODlzNR?=
U251 M2jDd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\lNVAxNTRyMDFOwG0> NUHKbGF1PDhiaB?= NVXZUZcyTE2VTx?= MlvqbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NVTxWVFVOjR4MkO3N|Y>
U87 NYq1eXAyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX[xNFAuPDByIN88US=> NXTzTFA3PDhiaB?= NUDTUmhtTE2VTx?= Mn\jbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> Mmr1NlQ3OjN5M{[=
MDA-MB-231-br NV2zSXVtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWewPIhFOC1zMDFOwG0> NHj2ZnU1QCCq NF;pU49FVVOR MXLpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MWWyOFYzOzd|Nh?=
HCC-1937 NGrLeVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX6wMVMxOCEQvF2= M1zaV|Q5KGh? NEHv[Y1FVVOR M1q0VYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NYXLb3F4OjR4MkO3N|Y>
MDA-MB-231 M2HFeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIrCXYwxNTRyIN88US=> MonLOFghcA>? MkfCSG1UVw>? M2e4dolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NFzKSFIzPDZ{M{ezOi=>
MDA-MB-468 M3zhcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjQNE02ODBizszN MkDVOFghcA>? NGW2dmJFVVOR Mn\XbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MVOyOFYzOzd|Nh?=
T47D MlPTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\Sc4oxNTFyMDFOwG0> NITVcpY1QCCq MVrEUXNQ M4rycIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NXfYcGxpOjR4MkO3N|Y>
MCF7 MnTWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3TTId[OC1zMECwJO69VQ>? MUm0PEBp M2jmfWROW09? NFfG[HNqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NYrMcGhiOjR4MkO3N|Y>
Hs683 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWCwMVExODBizszN NU\4WmdrQTZiaB?= NWDrRnZRUUN3ME2xNlgvQSEQvF2= NUXMSWVYOjR2OUW5NFc>
U87 MlTGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1O3cVAuOTByMDFOwG0> MkSwPVYhcA>? M4n1S2lEPTB;MUiuOFUh|ryP M3r1VlI1PDl3OUC3
LNZ308 MkPCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NES4ZpcxNTFyMECg{txO M4\mO|k3KGh? NWO1b4FqUUN3ME2zNlYvPyEQvF2= M1\2[|I1PDl3OUC3
U87 MX\BdI9xfG:|aYOgRZN{[Xl? NUCwR3E3OTByIN88US=> NF22VYU1QCCq NWfIWldITE2VTx?= NFH2epRqdmO{ZXHz[ZMhfGinIHPhd5Bie2VvMz:3JIFkfGm4aYT5 Ml:wNlQ1QDF3OE[=
U251  NU[wO5NUSXCxcITvd4l{KEG|c3H5 NVfnR|FlOTByIN88US=> MYi0PEBp NVjFRYpxTE2VTx?= M2XLR4lv[3KnYYPld{B1cGViY3HzdIF{\S1|L{egZYN1cX[rdIm= MoHENlQ1QDF3OE[=
U251 MlW4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUmyOEBp M1L6NmlEPTB;OE[uNlnjiIoEsfMAjVEvPThizszN M4DjNVI1OzJ4OUW0
U251 NF7hXo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUW0PEBp M{Ho[mlEPTB;N{WuN|TjiIoEsfMAjVEvODJizszN MnzoNlQ{OjZ7NUS=
U251 NE[0ZWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHSN2FEPzJiaB?= MWrJR|UxRTd{LkSy5qCKyrIkgJmxMlQ2KM7:TR?= NILZZZczPDN{Nkm1OC=>
U251 NEnTRotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGC5eWg6PiCq NGDpN2NKSzVyPU[5Mlgz6oDLwsJihKk{NjB2IN88US=> NEjQNmkzPDN{Nkm1OC=>
T98G NUXIW21GT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HmbFAuPzVyIN88US=> NF60Spo4Oi97NjDo MoLwbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MYiyOFMzPDB6MB?=
U251-MG NFL4d45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4eySFAuQDByIN88US=> MVW3NkBp NWWwNpRRcW6qaXLpeJMh[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK= M4jLZVI1ODl|NkOw
D54-MG NGjiTmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rGOVAuQDByIN88US=> NH[4dog4OiCq M4iyUIlvcGmkaYTzJINmdGxidnnhZoltcXS7IHnuJIEh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ MnvZNlQxQTN4M{C=
SHG-44 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTBPHlnOTBvMkCwJO69VQ>? MUS5OkBp NXTYXW1uUUN3ME25Mlc{KMLzIEKuNVIh|ryP MUWyOFA3PTV4OR?=
U373  Mn\xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXwPIcyOC1{MECg{txO NG\xO|E6PiCq MoTaTWM2OD1zMD6xN{DDuSBzLkCyJO69VQ>? MX:yOFA3PTV4OR?=
HT-29  Mn;wSpVv[3Srb36gRZN{[Xl? MXq1NFAh|ryP MVyyOE81QCCq MVHlcohidmOnczD0bIUhdGW4ZXzzJI9nKM7|LViyRXjDqA>? MmXNNlQxOzhyNki=
PC-3  MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1f0blAuOjVizszN NWq5TpB4PDhiaB?= MVzpcohq[mm2czDj[YxtKGe{b4f0bEB4cGmlaDDjZY4h[mVicH;0[Y51cWG2ZXSgZpkhdHmlb4DlcoU> NE\Od3czOzd2NkmzOC=>
PC-3  M{XueGFxd3C2b4Ppd{BCe3OjeR?= M2XDU|I2KM7:TR?= M1nORlQ5KGh? NHLrZpBqdmS3Y3XzJIFxd3C2b4Ppd{B4cGmlaDDjZY4h[mVicH;0[Y51cWG2ZXSgZpkhdHmlb4DlcoU> NXq2XHE1OjN5NE[5N|Q>
T98G NXj3THNxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk[2OVAuPDByIN88US=> NEnWZVcyPDRiaB?= M1PzTolvcGmkaYTzJINmdGxidnnhZoltcXS7IHnuJIEh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ NV35fFVWOjN5MUW0PVk>
U87-MG M2Pl[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTpNVAxKML3TR?= MmLBO|IhcA>? NI\E[ZVqdmirYnn0d{Bk\WyuIHfyc5d1cCC5aHnjbEBk[W5iYnWg[Y5p[W6lZXSgZpkhT1SE MXOyN|Y6Pjd6OB?=
U251-MG MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PrZ|ExOCEEtV2= NVW0Rm5UPzJiaB?= M2HGVIlvcGmkaYTzJINmdGxiZ4Lve5RpKHeqaXPoJINidiCkZTDlcohidmOnZDDifUBIXEJ? MXeyN|Y6Pjd6OB?=
LNT-229 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vFelMuOTByIN88US=> M1rHSVI1KGh? MonWbY5pcWKrdIOgZ4xwdm:pZX7pZ{B{fXK4aY\hcEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NV\rW5N1OjN4Nke2N|I>
T98G M3PtcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHzSIgyOC15MECg{txO NY\Qe5lKOjRiaB?= M{fPcYlvcGmkaYTzJINtd26xZ3XubYMhe3W{dnn2ZYwhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MoDsNlM3Pjd4M{K=
U87  MWXGeY5kfGmxbjDBd5NigQ>? NGjub3gyODBiwsXN M{[zNVMhcA>? M131doVt\X[jdHXzJJRp\SCuZY\lcJMhd2ZicFPob|Eh[W6mIIDDbIsz M2LvOlI{PjZ5NE[5
HCT116 NX\UN|VNTnWwY4Tpc44hSXO|YYm= M2TZN|ExOCEEtV2= NUXtVoF5OyCq NVHF[4FtcW6mdXPld{B1cGViQ3jrNUBRcG:|cHjvdplt[XSrb36= NHrlWYIzOzZ4N{S2PS=>
HCT3-6 MWrGeY5kfGmxbjDBd5NigQ>? MWixNFAhyrWP MXezJIg> MXnpcoR2[2W|IITo[UBEcGtzIGDoc5NxcG:{eXzheIlwdg>? MlvsNlM3Pjd2Nkm=
U-87  NVXvR|NlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXuwMVQxKM7:TR?= NYmzbVBLOTJiZB?= M4LDPIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NHv1fokzOzZ2NUeyPS=>
U-87  MVnBdI9xfG:|aYOgRZN{[Xl? NFfWdZoxNTRyIN88US=> MofxN{83KGR? MWPpcoR2[2W|IHHwc5B1d3OrczDpckBjd3SqIHTvd4UuKGGwZDD0bY1mNWSncHXu[IVvfCCvYX7u[ZI> MojPNlM3PDV5Mkm=
U-87  MWHGeY5kfGmxbjDBd5NigQ>? MnPDNE01OCEQvF2= NEf4co8{NzZiZB?= NGHLSGZqdmS3Y3XzJIF2fG:yaHHnfUBqdiCkb4ToJIRwe2VvIHHu[EB1cW2nLXTldIVv\GWwdDDtZY5v\XJ? NHH1WJIzOzZ2NUeyPS=>
GB-SCC010 M{DFSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfpeoVsPCCm NHXEdnlKSzVyPUKyOkDPxE1? NFnyVZozOzZzMke1OS=>
GB-SCC026 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;FdlQh\A>? NEDkNYVKSzVyPUWzMlEh|ryP MkjxNlM3OTJ5NUW=
GB-SCC028 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXi3PVZbPCCm MkjVTWM2OD1zNkeg{txO NX:zTYNTOjN4MUK3OVU>
U87 MknBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHxOEBl MYnJR|UxRTR3LkKg{txO M{LU[VI{PjF{N{W1
U87 stem cell Mln5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXO0JIQ> M1XpbGlEPTB;Nk[uO{DPxE1? NX65VZU{OjN4MUK3OVU>

... Click to View More Cell Line Experimental Data

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

PubMed: 24436439     


Cells were treated with TMZ (0.5 mM) time dependently, and Western blotting was used to analyze for phosphorylated ERK and p38 MAPK expression.

DR5 / c-FLIP / Survivin / XIAP; 

PubMed: 24436439     


Western blot analysis showing expressions in DR5 and antiapoptotic proteins (c-FLIP, survivin, and XIAP) in glioma cells treated with increasing doses of TMZ (0–2 mM) for 24 hours. 

24436439
Growth inhibition assay
Cell viability; 

PubMed: 25751281     


Distinct temozolomide-resistance for MGMT-expressing (SF767) and MGMT-negative (U87) GBM cells was assessed.

25751281
Immunofluorescence
Phalloidin / Phospho-H2A.X; 

PubMed: 27375225     


Immunofluorescence analysis of the level of phospho-H2A.X in nucleus which can reflect DNA damage response increased significantly at day 6, peaked during days 7-10 and decreased significantly at day 12 after treatment temozolomide (200 μM). 

cleaved caspase-3; 

PubMed: 25663820     


Representative Photomicrographs of cleaved caspase-3 immunoreactivity in control (DMSO treated) and treated group of U87 cells. Base line immunofluorescence was detected in control group. Significant Increase in immunofluorescence is detected in all treated groups with the highest observed intensity in combination treatment group (NA-2 + TMZ).

27375225 25663820
In vivo After a daily i.p. dose of 40 mg/kg for 5 consecutive days (days 1-5 after tumor transplant), methazolastone increases life-span by 86% in L-1210 and 22% in L-1210/BCNU. In L-1210/BCNU no effect is seen after 100 μM or 200 μM treatment; only 400 μM methazolastone produced an accumulation of cells in premitotic phase but much less than in L-1210. In L-1210/BCNU the maximum accumulation of cells in SL-G2-M is, after 48 hours-72 hours, approximately 30% as compared to 23% in untreated cells. Cells accumulates in SL-G2-M occurred too when L- 1210 leukemia-bearing mice are treated i.v. with methazola stone (40 mg/kg). No such effect is seen on L-1210/BCNU cells from mice given the same drug dose. [1]

Protocol

Cell Research:

[1]

- Collapse
  • Cell lines: L-1210 and L-1210/BCNU cells
  • Concentrations: 0 μM -100 μM
  • Incubation Time: l hours
  • Method:

    L-1210 and L-1210/BCNU cells are seeded at 0.2 × 104 cells/mL and incubated for 24 hours. The cultures are treated with Methazolastone for l hours at 37oC, then washed twice in PBS by centrifugation and resuspended in fresh medium. Controls and treated samples are diluted in fresh medium 1:4 at 48 hours and 1:2 at 96 hours. Using these dilutions cell concentrations throughout the experiments are between 3 × 105 and 8 × 105/mL. Control growth is logarithmic in this range.


    (Only for Reference)
Animal Research:

[1]

- Collapse
  • Animal Models: DBA/2 mice with L-1210 and L-1210/BCNU cells
  • Dosages: 40 mg/kg
  • Administration: Administered via i.v.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 38 mg/mL (195.72 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing.
2mg/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 194.15
Formula

C6H6N6O2

CAS No. 85622-93-1
Storage powder
in solvent
Synonyms CCRG81045, NSC 362856,TMZ
Smiles CN1N=NC2=C(N=C[N]2C1=O)C(N)=O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
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 MSDS / 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 MSDS / 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):
    C7=C6/X C7: LOG(C7):
    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
NCT04238819 Not yet recruiting Drug: Abemaciclib|Drug: Irinotecan|Drug: Temozolomide Relapsed Solid Tumor|Refractory Solid Tumor Eli Lilly and Company July 31 2020 Phase 1
NCT04388475 Not yet recruiting Drug: OKN-007|Drug: Temozolomide (TMZ) Recurrent Malignant Glioma|Brain Glioblastoma Oblato Inc. May 25 2020 Phase 2
NCT03796507 Not yet recruiting Drug: Temozolomide Glioma of Brain University of Rochester|National Institutes of Health (NIH) March 1 2020 Early Phase 1
NCT04200066 Not yet recruiting Drug: Temozolomide Tamoxifen Maprotiline Glioblastoma|Brain Tumor University of Rochester February 1 2020 Phase 1
NCT04091503 Not yet recruiting Drug: Intranasal Modified Temozolomide Glioma Malignant|Gliosarcoma|Astrocytoma of Brain Center Trials & Treatment Europe December 10 2019 Phase 1
NCT03932981 Recruiting Drug: Temozolomide Adult Brainstem Glioma Assistance Publique - Hôpitaux de Paris July 26 2019 Phase 2

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID