Temozolomide

Catalog No.S1237 Synonyms: CCRG81045, NSC 362856

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.

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In DMSO USD 64 In stock
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Cited by 43 Publications

Purity & Quality Control

Choose Selective DNA/RNA Synthesis Inhibitors

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.
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 M2XxfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVzadZY4PDhiaB?= NIfaVphKSzVyPUGzPU4zOOLCidMx5qCKPS57NTFOwG0> NY\FfXg{OjV7NkCyPFI>
KellyCis83 M4frOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYq0PEBp MX7JR|UxRTJ3MT6wNQKBkcLz4pEJNVUvPzVizszN NHvj[YEzPTl4MEK4Ni=>
SK-N-AS MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\zOFghcA>? M3rvPGlEPTB;MkK3Mlcx6oDLwsJihKkzOi5zNTFOwG0> M{m0PFI2QTZyMkiy
SK-N-ASCis24 NIKxPWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkX1OFghcA>? MoflTWM2OD12OECuOlDjiIoEsfMAjVExOS5zNTFOwG0> NYjGUFFvOjV7NkCyPFI>
CHP-212 M1\6N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFrqfGM1QCCq MoL5TWM2OD15Lkm35qCKyrIkgJmwMlY6KM7:TR?= NXrubGJUOjV7NkCyPFI>
CHP-212Cis100 M2f1Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkS5OFghcA>? NFPlVXRKSzVyPUmuOVXjiIoEsfMAjVAvQDhizszN MoniNlU6PjB{OEK=
U87  MlO0SpVv[3Srb36gRZN{[Xl? NH\EPG8yODBizszN MXmyOE04OiCq MmPmbY5lfWOnczDEZ3IyKGW6cILld5Nqd25? MVSyOVgxQDh4OB?=
LN229 M4jiT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVuwMVUxKM7:TR?= MoTrTWM2OD1zNjFOwG0> MVWyOVc2ODJ5Mx?=
TR-LN229 M1PJcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVGwMVUxKM7:TR?= Mn\wTWM2OD15NzFOwG0> NV2w[JRSOjV5NUCyO|M>
U87  M1SzN2Fxd3C2b4Ppd{BCe3OjeR?= MV:w5qCUOjBy4pEJxtVO NFLRbnAzPCCq NYTQXYRv\W6qYX7j[ZMhS1FiaX7keYNm\CCjcH;weI9{cXN? Ml\aNlU3QDF4Nki=
U251MG M3vaWmFxd3C2b4Ppd{BCe3OjeR?= MmrNNVAxyqEQvF2= MlT2OFghcA>? M3;iUnBDWw>? NWnTcIZMcW6mdXPld{BieG:ydH;zbZM> MlPINlU3QDB2NkS=
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U87 NVrxW4s{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;tOVAuOzVyIN88US=> MUW0POKhcMLi NYDhXHVscW6qaXLpeJMh[2WubDDndo94fGhic3zp[4h1dHl? MV2yOVU2PDJ{Mx?=
U118  NEWxfZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nSUlUxNTN3MDFOwG0> MkDQOFjDqGkEoB?= NUnleFdTcW6qaXLpeJMh[2WubDDndo94fGhic3zp[4h1dHl? M1G1c|I2PTV2MkKz
U87 Mn\HSpVv[3Srb36gRZN{[Xl? NEX4TlAzPTBxM{WwJO69VQ>? NH3VdG41QMLiaNMg NELvO2ZmdmijbnPld{BVVVhvaX7keYNm\CCyLWDLR{1x[W5iZHXjdoVie2V? M{PwN|I2PTV2MkKz
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A2058 MmPIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEn2O2k1QMLiaNMg MlH3TWM2OD1zMjFOwG0> Mlv3NlU2OjR3NUK=
M238 NHK0eVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHroPIY1QMLiaNMg MVTJR|UxRTRyIN88US=> NHjpSYwzPTV{NEW1Ni=>
M249 NFzPPJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU[0POKhcMLi MYHJR|UxRTJ3NDFOwG0> M1O1T|I2PTJ2NUWy
M21 M4PhXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUi1[|lVPDkEoHlCpC=> NWjQNXVsUUN3ME2yNlEh|ryP MXyyOVUzPDV3Mh?=
U251 MXzDfZRwfG:6aYT5JGF{e2G7 NInZOXczOCEQvF5CpC=> NXflfXhoPDkEoHlCpC=> NXrqT4JpemWmdXPl[JMhfGinIIDldoNmdnSjZ3XzJI9nKGOxbH;ubYV{KG[xcn3l[C=> NWDwZ4p5OjV2M{SzPFE>
LN229 MorwR5l1d3SxeHn0fUBCe3OjeR?= MV2yNEDPxE4EoB?= NEjPXms1QMLiaNMg NInreIRz\WS3Y3Xkd{B1cGVicHXyZ4VvfGGpZYOgc4Yh[2:ub37p[ZMh\m:{bXXk MWOyOVQ{PDN6MR?=
U373MG-LUC NFP0NWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fGc|czKGh? NFfyS45KSzVyPk[wNEDPxE1? NYm1NFNWOjV2M{G5OVM>
U87  NU\Xe|R[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml7HNlUuOjByIN88US=> Moi3OFjDqGkEoB?= NGTlXpZqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? Ml;xNlU1ODB5NEW=
U251 NHT3dIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4q5V|I2NTJyMDFOwG0> NXnPR3dSPDkEoHlCpC=> NVTuZm1bcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? Mn3KNlU1ODB5NEW=
U251 NEnLWoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TsR|ExOC12MECg{txO M2TWSFczNzl4IHi= Mn3keIhmKGGwdHmtdJJwdGmoZYLheIl3\SCnZn\lZ5Qh[2GwIHLlJIVvcGGwY3XkJIJ6KGexc4P5dI9tKGWwaHHuZ4VlKMLi MWeyOVM4PTJ5MR?=
U373 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1X3XFExOC12MECg{txO NYD0Tnc6PzJxOU[gbC=> MoGweIhmKGGwdHmtdJJwdGmoZYLheIl3\SCnZn\lZ5Qh[2GwIHLlJIVvcGGwY3XkJIJ6KGexc4P5dI9tKGWwaHHuZ4VlKMLi NVyzV3c5OjV|N{WyO|E>
U343 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDPbGk4OTByLUSwNEDPxE1? MknwO|IwQTZiaB?= NHH3WZN1cGViYX70bU1xem:uaX\ldoF1cX[nIHXm[oVkfCClYX6gZoUh\W6qYX7j[YQh[nliZ3;zd5lxd2xiZX7oZY5k\WRiwrC= MX:yOVM4PTJ5MR?=
U87MG-luc2 NWXaNldVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfhOGpxOTByLUSwNEDPxE1? MofoO|IwQTZiaB?= NW\CbmFtfGinIHHueIkueHKxbHnm[ZJifGm4ZTDl[oZm[3RiY3HuJIJmKGWwaHHuZ4VlKGK7IHfvd5N6eG:uIHXubIFv[2WmINMg NX3zRVhkOjV|N{WyO|E>
U87 MUPGeY5kfGmxbjDBd5NigQ>? NHW2cZAzODBizszN NX;rdohtPDhiaB?= M37IR4lv[3KnYYPld{BDWkOFMzDtVm5CKGW6cILld5Nqd25? MViyOVM{Pzd{MR?=
U251 MWrGeY5kfGmxbjDBd5NigQ>? NHnPdYUzODBizszN MkfOOFghcA>? NEToPGNqdmO{ZXHz[ZMhSlKFQ{OgcXJPSSCneIDy[ZN{cW:w MXuyOVM{Pzd{MR?=
A172 MXLGeY5kfGmxbjDBd5NigQ>? M3TQfVIxOCEQvF2= MlrjOFghcA>? NFXySGNqdmO{ZXHz[ZMhSlKFQ{OgcXJPSSCneIDy[ZN{cW:w MmrGNlU{Ozd5MkG=
U251 NF7vV5FHfW6ldHnvckBCe3OjeR?= M323ZVIxOCEQvF2= M1T0V|Q5KGh? Mln2bY5kemWjc3XzJJRp\SCneIDy[ZN{cW:wIH;mJGJTS0FzLDDCVmNCOixiUlHEOVEh[W6mIF\BUmNFOg>? NUX5S2N5OjV|M{e3NlE>
A172 MmnlSpVv[3Srb36gRZN{[Xl? MVOyNFAh|ryP M2K3WFQ5KGh? MnLabY5kemWjc3XzJJRp\SCneIDy[ZN{cW:wIH;mJGJTS0FzLDDCVmNCOixiUlHEOVEh[W6mIF\BUmNFOg>? NFXNUGYzPTN|N{eyNS=>
U87 NYHqUWQ5TnWwY4Tpc44hSXO|YYm= MoDINlAxKM7:TR?= NIH2SowzPC95Mj:xNlAhcA>? M1[3O4lv[3KnYYPld{DPu0h{QWig[o9kcSCob4LtZZRqd25idHnt[U1l\XCnbnTlcpRtgQ>? NYLSfJh2OjV|M{e3NlE>
U251 MULGeY5kfGmxbjDBd5NigQ>? MkfwNlAxKM7:TR?= NFmySHkzPC95Mj:xNlAhcA>? M1[wcIlv[3KnYYPld{DPu0h{QWig[o9kcSCob4LtZZRqd25idHnt[U1l\XCnbnTlcpRtgQ>? NXz4OVZxOjV|M{e3NlE>
A172 NHjTN4dHfW6ldHnvckBCe3OjeR?= NEm1[4UzODBizszN MkjENlQwPzJxMUKwJIg> MVzpcoNz\WG|ZYOg{tNJOkG[IH\vZ4kh\m:{bXH0bY9vKHSrbXWt[IVx\W6mZX70cJk> NULzUW5zOjV|M{e3NlE>
SNB19V Mn70S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmKwO{Bl NGHJNXFFVVOR NYPQNJpCT0l3ME2zOU44yrFzMjFOwG0> M3q1RVI2Ojd5NESx
SNB19M M1ixUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHyzZXY4KGR? MWjEUXNQ NFjr[ppIUTVyPUS2PU46yrF6ODFOwG0> MVmyOVI4PzR2MR?=
SNB19VR NF\3fY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDP[YdCPyCm MlvaSG1UVw>? NU[wc4VqT0l3ME2yPFAvOsLzMUig{txO MkiyNlUzPzd2NEG=
U373V MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\ucVE4KGR? M2TWcGROW09? MVfHTVUxRTZ6LkFCtVMzKM7:TR?= M2XmVVI2Ojd5NESx
U373M M3;YO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEO5Z4g4KGR? MXHEUXNQ MUnHTVUxRTN4OD63xtE5PiEQvF2= MmDBNlUzPzd2NEG=
U373VR Mn\mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\2O{Bl NWLsbIFtTE2VTx?= M{jGW2dKPTB;Mki4MljDuTN|IN88US=> M4XpRVI2Ojd5NESx
U87MG M3Ht[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfGc|I4KGR? M1PLVWROW09? Mk\ES2k2OD1|OD6zxtEzOCEQvF2= M4H2fVI2Ojd5NESx
HCT116 NYX5TG9xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXVWY84KGR? MW\EUXNQ NVXJdGx[T0l3ME21O|kvQcLzM{Kg{txO MkS5NlUzPzd2NEG=
DLD1 NYTCVmVFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUK3JIQ> M3r2bWROW09? MonxS2k2OD13MEGuOOKyQTNizszN M4TK[|I2Ojd5NESx
MRC5 MmK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4iyTVch\A>? MlixSG1UVw>? NXTGS5BVT0l3ME20OFkvPMLzODFOwG0> NYniSVN7OjV{N{e0OFE>
SNB19V  MV7GeY5kfGmxbjDBd5NigQ>? MmnoNVAxKM7:TdMgWG1b NF;TbGwxNTd{IHi= M2jvRYlv[3KnYYPld{DPu0h{QWig[ZhxemW|c3nvckBj\XS5ZXXuJFE3KGGwZDC3NkBp Ml7sNlUzPzd2NEG=
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U251 M2PTTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHwNVAxNTRyMDFOwG0> Mln4OFghcA>? NYjtOpo6TE2VTx?= M3nVZolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M1LJTlI1PjJ|N{O2
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MDA-MB-468 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVSwMVUxOCEQvF2= NUGzdo1MPDhiaB?= M2W1NmROW09? MVrpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NHHnflYzPDZ{M{ezOi=>
T47D NH\6bYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzQWFB1OC1zMECg{txO Ml3iOFghcA>? MYjEUXNQ MUTpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M3;FS|I1PjJ|N{O2
MCF7 NGjLVndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHGw[VMxNTFyMECg{txO M4jvcFQ5KGh? MUDEUXNQ NXfMdnlzcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NIjKRXIzPDZ{M{ezOi=>
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LNZ308 MknvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\4e4FlOC1zMECwJO69VQ>? NFfqXFk6PiCq Mn;BTWM2OD1|Mk[uO{DPxE1? MkjkNlQ1QTV7MEe=
U87 NWT6bYN{SXCxcITvd4l{KEG|c3H5 NVftZ|RGOTByIN88US=> Mli0OFghcA>? NIDrZ29FVVOR NXr0bXhNcW6lcnXhd4V{KHSqZTDjZZNx[XOnLUOvO{Bi[3Srdnn0fS=> M1:yWVI1PDhzNUi2
U251  MWPBdI9xfG:|aYOgRZN{[Xl? MorVNVAxKM7:TR?= M4DEcFQ5KGh? NH;hcGxFVVOR MUfpcoNz\WG|ZYOgeIhmKGOjc4Dhd4UuOy95IHHjeIl3cXS7 MYCyOFQ5OTV6Nh?=
U251 M1eySWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnfnNlQhcA>? MkLWTWM2OD16Nj6yPgKBkcLz4pEJNU42QCEQvF2= NIm4fJozPDN{Nkm1OC=>
U251 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWS0PEBp MYXJR|UxRTd3LkO05qCKyrIkgJmxMlAzKM7:TR?= MUGyOFMzPjl3NB?=
U251 M3fZeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFK5T|A4OiCq NHj6UG5KSzVyPUeyMlQz6oDLwsJihKkyNjR3IN88US=> MnS4NlQ{OjZ7NUS=
U251 NXfk[FhpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;SZVk3KGh? M{DubWlEPTB;NkmuPFLjiIoEsfMAjVMvODRizszN NU\0dYtpOjR|Mk[5OVQ>
T98G NFGyWYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXKwMVc2OCEQvF2= MmjhO|IwQTZiaB?= NGfBOGdqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDpckBiKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= MmTDNlQ{OjRyOEC=
U251-MG M{ixSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYj3VXVuOC16MECg{txO NX[5WW9IPzJiaB?= MoLnbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MWGyOFA6OzZ|MB?=
D54-MG NH;yc|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkniNE05ODBizszN NHvjS|k4OiCq NUTvemZ3cW6qaXLpeJMh[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK= MmHrNlQxQTN4M{C=
SHG-44 NVjMPZVET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPzNVAuOjByIN88US=> NFjrdno6PiCq M2ezbWlEPTB;OT63N{DDuSB{LkGyJO69VQ>? NV7tRYRROjRyNkW1Olk>
U373  MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jJ[|ExNTJyMDFOwG0> MWW5OkBp MmTyTWM2OD1zMD6xN{DDuSBzLkCyJO69VQ>? NXSwVpZ{OjRyNkW1Olk>
HT-29  MXLGeY5kfGmxbjDBd5NigQ>? MorEOVAxKM7:TR?= NXz5Uok2OjRxNEigbC=> NHvzXYtmdmijbnPld{B1cGVibHX2[Yx{KG:oIN8zMWgzSVkEoB?= M2KxWVI1ODN6ME[4
PC-3  Mlz1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVe4WpBzOC1{NTFOwG0> MVy0PEBp MkDSbY5pcWKrdIOgZ4VtdCCpcn;3eIghf2irY3igZ4FvKGKnIIDveIVvfGmjdHXkJIJ6KGy7Y3;w[Y5m MlqxNlM4PDZ7M{S=
PC-3  NY\FZWVnSXCxcITvd4l{KEG|c3H5 NILuZlAzPSEQvF2= M2PPWFQ5KGh? Mon0bY5lfWOnczDhdI9xfG:|aYOge4hq[2hiY3HuJIJmKHCxdHXueIlifGWmIHL5JIx6[2:yZX7l MmLpNlM4PDZ7M{S=
T98G M{LJS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXG1NE01ODBizszN Mlu3NVQ1KGh? M3rOTIlvcGmkaYTzJINmdGxidnnhZoltcXS7IHnuJIEh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ NX3abnc4OjN5MUW0PVk>
U87-MG NWXmPIJ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2iwd|ExOCEEtV2= NV\pVYZHPzJiaB?= NWnzV5UycW6qaXLpeJMh[2WubDDndo94fGhid3jpZ4gh[2GwIHLlJIVvcGGwY3XkJIJ6KEeWQh?= MkD0NlM3QTZ5OEi=
U251-MG NX3wbHdbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIT5dVUyODBiwsXN MXm3NkBp NU\1dGtscW6qaXLpeJMh[2WubDDndo94fGhid3jpZ4gh[2GwIHLlJIVvcGGwY3XkJIJ6KEeWQh?= NVXr[YtkOjN4OU[3PFg>
LNT-229 NX34WGxsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjZ[o4{NTFyMDFOwG0> NHPLVIMzPCCq NHfSbldqdmirYnn0d{BkdG:wb3flcolkKHO3co\peoFtKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NELOcZkzOzZ4N{[zNi=>
T98G MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\udlExNTdyMDFOwG0> NEjkV2wzPCCq MWnpcohq[mm2czDjcI9vd2enbnnjJJN2en[rdnHsJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MlvNNlM3Pjd4M{K=
U87  Mn;uSpVv[3Srb36gRZN{[Xl? MkfyNVAxKML3TR?= MVGzJIg> MX;lcIV3[XSnczD0bIUhdGW4ZXzzJI9nKHCFaHuxJIFv\CCyQ3jrNi=> Mn3wNlM3Pjd2Nkm=
HCT116 M1\UN2Z2dmO2aX;uJGF{e2G7 NUi5R242OTByINM1US=> M4KzPFMhcA>? MWLpcoR2[2W|IITo[UBEcGtzIGDoc5NxcG:{eXzheIlwdg>? NV7pbII1OjN4Nke0Olk>
HCT3-6 NH7l[lNHfW6ldHnvckBCe3OjeR?= NYm4VFdKOTByINM1US=> MnSzN{Bp MYTpcoR2[2W|IITo[UBEcGtzIGDoc5NxcG:{eXzheIlwdg>? MoHvNlM3Pjd2Nkm=
U-87  M33IV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF[2Z|YxNTRyIN88US=> MYKxNkBl MWHpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NXK2SXVIOjN4NEW3Nlk>
U-87  MYjBdI9xfG:|aYOgRZN{[Xl? Ml\HNE01OCEQvF2= NXnrWHB3Oy94IHS= NXj4O45pcW6mdXPld{BieG:ydH;zbZMhcW5iYn;0bEBld3OnLTDhcoQhfGmvZT3k[ZBmdmSnboSgcYFvdmW{ NV3W[4lMOjN4NEW3Nlk>
U-87  NFTqbXZHfW6ldHnvckBCe3OjeR?= MnjkNE01OCEQvF2= MorqN{83KGR? M{TV[4lv\HWlZYOgZZV1d3CqYXf5JIlvKGKxdHig[I9{\S1iYX7kJJRqdWVvZHXw[Y5l\W62IH3hco5meg>? NVXvZ45pOjN4NEW3Nlk>
GB-SCC010 MoHiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTBOEBl MoLXTWM2OD1{Mk[g{txO M4nnOFI{PjF{N{W1
GB-SCC026 NGXsdIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUm0JIQ> M1LifWlEPTB;NUOuNUDPxE1? MXGyN|YyOjd3NR?=
GB-SCC028 NIe1d2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXEXGdxPCCm NHLM[XZKSzVyPUG2O{DPxE1? M4\zfFI{PjF{N{W1
U87 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PoXFQh\A>? NHvYOpVKSzVyPUS1MlIh|ryP MkLWNlM3OTJ5NUW=
U87 stem cell Mk\1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH6zfGg1KGR? NWPhWG5vUUN3ME22Ok44KM7:TR?= MljCNlM3OTJ5NUW=

... 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
  • Formulation: 95% ethanol
  • 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

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
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*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
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* 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):
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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
NCT04091503 Not yet recruiting Drug: Intranasal Modified Temozolomide Glioma Malignant|Gliosarcoma|Astrocytoma of Brain Center Trials & Treatment Europe December 10 2019 Phase 1
NCT03796507 Not yet recruiting Drug: Temozolomide Glioma of Brain University of Rochester|National Institutes of Health (NIH) November 1 2019 Early Phase 1
NCT03932981 Recruiting Drug: Temozolomide Adult Brainstem Glioma Assistance Publique - Hôpitaux de Paris July 26 2019 Phase 2
NCT03709680 Recruiting Drug: Palbociclib|Drug: Temozolomide|Drug: Irinotecan Solid Tumors|Ewing Sarcoma|Rhabdoid Tumor|Rhabdomyosarcoma|Neuroblastoma|Medulloblastoma|Diffuse Intrinsic Pontine Glioma Pfizer May 24 2019 Phase 1
NCT03832621 Recruiting Drug: Temozolomide|Drug: Nivolumab|Drug: Ipilimumab Metastatic Colorectal Cancer Fondazione IRCCS Istituto Nazionale dei Tumori Milano March 25 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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID