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 28 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 NWLTXndPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYW0PEBp Mn\zTWM2OD1zM{muNlDjiIoEsfMAjVUvQTVizszN MkjsNlU6PjB{OEK=
KellyCis83 NWHHPGFTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPKbZQ1QCCq NYnJ[Wc2UUN3ME2yOVEvODEkgJpCtgKBkTF3Lke1JO69VQ>? NVWzeFVsOjV7NkCyPFI>
SK-N-AS MoHPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGixd2w1QCCq NWHtdotVUUN3ME2yNlcvPzEkgJpCtgKBkTJ{LkG1JO69VQ>? MlX1NlU6PjB{OEK=
SK-N-ASCis24 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TBVlQ5KGh? NIXwUWtKSzVyPUS4NE43OOLCidMx5qCKOTBzLkG1JO69VQ>? M4j3TFI2QTZyMkiy
CHP-212 NFfIPWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{L0PFQ5KGh? MY\JR|UxRTdwOUhihKnDueLCiUCuOlkh|ryP NWrQbo5FOjV7NkCyPFI>
CHP-212Cis100 M3POZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\mboFXPDhiaB?= NYjFS2g5UUN3ME25MlU26oDLwsJihKkxNjh6IN88US=> M1uyXFI2QTZyMkiy
U87  MX\GeY5kfGmxbjDBd5NigQ>? M3HHNlExOCEQvF2= MkPqNlQuPzJiaB?= NIS1Z3lqdmS3Y3XzJGRkWjFiZYjwdoV{e2mxbh?= MlWzNlU5ODh6Nki=
LN229 NEX0VmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF3kTnYxNTVyIN88US=> M3rNSGlEPTB;MU[g{txO M1jQS|I2PzVyMkez
TR-LN229 NEHtS|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXnNE02OCEQvF2= NWXZdGwxUUN3ME23O{DPxE1? NXL5WnRwOjV5NUCyO|M>
U87  NYTROY1wSXCxcITvd4l{KEG|c3H5 NYK4dmdjOOLCk{KwNQKBkcL3TR?= NGD5UHAzPCCq M{W4WoVvcGGwY3XzJGNSKGmwZIXj[YQh[XCxcITvd4l{ Moj4NlU3QDF4Nki=
U251MG MVvBdI9xfG:|aYOgRZN{[Xl? NUD4OmcxOTBywrFOwG0> MoK4OFghcA>? NYPJcZo2WEKV MXvpcoR2[2W|IHHwc5B1d3Orcx?= NYLLelI{OjV4OEC0OlQ>
U87MG M{XoV2Fxd3C2b4Ppd{BCe3OjeR?= MWGxNFDDqM7:TR?= NX\xcodHPDhiaB?= NYj0TolsWEKV MmPFbY5lfWOnczDhdI9xfG:|aYO= M3n5bVI2PjhyNE[0
U87 MmfCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXX2PWQ6PTBvM{WwJO69VQ>? MkLtOFjDqGkEoB?= NUOzZXJycW6qaXLpeJMh[2WubDDndo94fGhic3zp[4h1dHl? NWfRSZdQOjV3NUSyNlM>
U118  M2HpTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jHcVUxNTN3MDFOwG0> NGLu[ZQ1QMLiaNMg NILQTllqdmirYnn0d{Bk\WyuIHfyc5d1cCC|bHnnbJRtgQ>? M3ewNFI2PTV2MkKz
U87 NYnGOHhtTnWwY4Tpc44hSXO|YYm= NF25VFUzPTBxM{WwJO69VQ>? NUjjU|FQPDkEoHlCpC=> M2LPRYVvcGGwY3XzJHROYC2rbnT1Z4VlKHBvUFvDMZBidiCmZXPy[YF{\Q>? NVLiN2w3OjV3NUSyNlM>
U118  MmnFSpVv[3Srb36gRZN{[Xl? NGjqb3UzPTBxM{WwJO69VQ>? NF7jcXI1QMLiaNMg NUnTOpN4\W6qYX7j[ZMhXE2[LXnu[JVk\WRicD3QT2MueGGwIHTlZ5Jm[XOn NHT4SHAzPTV3NEKyNy=>
U87 NH3MSWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1vPU|I2OC9|NUCg{txO NVXz[HdQPDkEoHlCpC=> NF3VfZJqdmO{ZXHz[ZMhfGinIIDldoNmdnSjZ3Wgc4Yh[2WubIOgbY4hWyCjbnSgS|IwVcLiY3;0doVifGWmIIfpeIghXE2[ NH[2[owzPTV3NEKyNy=>
A375 NVnle5J1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnCOnVxPDkEoHlCpC=> M2foPWlEPTB;Mk[1JO69VQ>? M2O4SFI2PTJ2NUWy
A2058 NFXufYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlv6OFjDqGkEoB?= NX7ldFZXUUN3ME2xNkDPxE1? NHrlPZEzPTV{NEW1Ni=>
M238 NWHpXGNST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1ix[VQ5yqCqwrC= NHjhVYFKSzVyPUSwJO69VQ>? MYmyOVUzPDV3Mh?=
M249 NV7hVWlpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnnUOFjDqGkEoB?= M2TLWmlEPTB;MkW0JO69VQ>? M17VeVI2PTJ2NUWy
M21 NF;m[HNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV74W4R{PDkEoHlCpC=> Mn7jTWM2OD1{MkGg{txO M4XERlI2PTJ2NUWy
U251 MULDfZRwfG:6aYT5JGF{e2G7 MkfHNlAh|ryPwrC= NIXiSZk1QMLiaNMg NXvPWXBTemWmdXPl[JMhfGinIIDldoNmdnSjZ3XzJI9nKGOxbH;ubYV{KG[xcn3l[C=> M3nnNFI2PDN2M{ix
LN229 NVXyS3lrS3m2b4TvfIl1gSCDc4PhfS=> M{fmWVIxKM7:TdMg NEjaWXQ1QMLiaNMg M4niTJJm\HWlZXTzJJRp\SCyZYLj[Y51[WenczDv[kBkd2yxbnnld{Bnd3KvZXS= MkD4NlU1OzR|OEG=
U373MG-LUC NGiwdYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13pflczKGh? M4HSPWlEPTB-NkCwJO69VQ>? NELvZpozPTR|MUm1Ny=>
U87  MnfrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXaNlUuOjByIN88US=> M3u5ZVQ5yqCqwrC= M{LPcYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M1\wb|I2PDByN{S1
U251 NIT0WWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzwRoxbOjVvMkCwJO69VQ>? NGnOOWM1QMLiaNMg NFjGcnRqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NIj3UoUzPTRyMEe0OS=>
U251 M1G1RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVSxNFAuPDByIN88US=> MkDkO|IwQTZiaB?= NVHpb4RrfGinIHHueIkueHKxbHnm[ZJifGm4ZTDl[oZm[3RiY3HuJIJmKGWwaHHuZ4VlKGK7IHfvd5N6eG:uIHXubIFv[2WmINMg NIHIRo0zPTN5NUK3NS=>
U373 MnPZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXINVAxNTRyMDFOwG0> MkfCO|IwQTZiaB?= MWL0bIUh[W62aT3wdo9tcW[ncnH0bZZmKGWoZnXjeEBk[W5iYnWg[Y5p[W6lZXSgZpkh\2:|c4nwc4wh\W6qYX7j[YQhyqB? MXmyOVM4PTJ5MR?=
U343 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXKxNFAuPDByIN88US=> M2PKRlczNzl4IHi= NInNeop1cGViYX70bU1xem:uaX\ldoF1cX[nIHXm[oVkfCClYX6gZoUh\W6qYX7j[YQh[nliZ3;zd5lxd2xiZX7oZY5k\WRiwrC= NHHzc4QzPTN5NUK3NS=>
U87MG-luc2 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYL6XIVIOTByLUSwNEDPxE1? MkTzO|IwQTZiaB?= NGHBS2h1cGViYX70bU1xem:uaX\ldoF1cX[nIHXm[oVkfCClYX6gZoUh\W6qYX7j[YQh[nliZ3;zd5lxd2xiZX7oZY5k\WRiwrC= NVzKcFh[OjV|N{WyO|E>
U87 NXrv[Jd2TnWwY4Tpc44hSXO|YYm= NYq3WIVbOjByIN88US=> NGflUIE1QCCq NIHKO5dqdmO{ZXHz[ZMhSlKFQ{OgcXJPSSCneIDy[ZN{cW:w MYSyOVM{Pzd{MR?=
U251 NXm2T4JFTnWwY4Tpc44hSXO|YYm= MnO0NlAxKM7:TR?= MlfEOFghcA>? MmTMbY5kemWjc3XzJGJTS0N|IH3SUmEh\XiycnXzd4lwdg>? M4fsclI2OzN5N{Kx
A172 NGCyfpJHfW6ldHnvckBCe3OjeR?= NVW5b5BEOjByIN88US=> NV7iNmlXPDhiaB?= MkO0bY5kemWjc3XzJGJTS0N|IH3SUmEh\XiycnXzd4lwdg>? NX;RW4o2OjV|M{e3NlE>
U251 NVXIVmdoTnWwY4Tpc44hSXO|YYm= Mk\tNlAxKM7:TR?= MWi0PEBp MmTlbY5kemWjc3XzJJRp\SCneIDy[ZN{cW:wIH;mJGJTS0FzLDDCVmNCOixiUlHEOVEh[W6mIF\BUmNFOg>? MVmyOVM{Pzd{MR?=
A172 NWHabGU5TnWwY4Tpc44hSXO|YYm= MknkNlAxKM7:TR?= NWGx[o9DPDhiaB?= NFu4TItqdmO{ZXHz[ZMhfGinIHX4dJJme3Orb36gc4YhSlKFQUGsJGJTS0F{LDDSRWQ2OSCjbnSgSmFPS0R{ Mn;oNlU{Ozd5MkG=
U87 MlnCSpVv[3Srb36gRZN{[Xl? NH;6cpMzODBizszN NV;teWxIOjRxN{KvNVIxKGh? MoD2bY5kemWjc3XzJO6{UDKDWDDmc4NqKG[xcn3heIlwdiC2aX3lMYRmeGWwZHXueIx6 NXXDfJVSOjV|M{e3NlE>
U251 M3fDe2Z2dmO2aX;uJGF{e2G7 MoPMNlAxKM7:TR?= NHnTSlQzPC95Mj:xNlAhcA>? NH[xcFBqdmO{ZXHz[ZMh|rOKMlHYJIZw[2liZn;ycYF1cW:wIITpcYUu\GWyZX7k[Y51dHl? MUCyOVM{Pzd{MR?=
A172 MXTGeY5kfGmxbjDBd5NigQ>? MXOyNFAh|ryP MWCyOE84Oi9zMkCgbC=> MXrpcoNz\WG|ZYOg{tNJOkG[IH\vZ4kh\m:{bXH0bY9vKHSrbXWt[IVx\W6mZX70cJk> NH\GU2YzPTN|N{eyNS=>
SNB19V NH;aclRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHv3fpM4KGR? MWrEUXNQ MmDsS2k2OD1|NT63xtEyOiEQvF2= NIjVdmIzPTJ5N{S0NS=>
SNB19M NUfVXWJiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jLZ|ch\A>? MV3EUXNQ NV\qU25IT0l3ME20OlkvQcLzOEig{txO M{ftb|I2Ojd5NESx
SNB19VR NEG3bIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nzPFch\A>? MX;EUXNQ M3OxS2dKPTB;MkiwMlLDuTF6IN88US=> NEjwfHYzPTJ5N{S0NS=>
U373V M{G2UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPDU2NQPyCm NVjDdFFJTE2VTx?= M2\zSWdKPTB;NkiuNOKyOzJizszN MnrmNlUzPzd2NEG=
U373M NXXIS|FzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfLRZc4KGR? M{K4TWROW09? NFn2WFhIUTVyPUO2PE44yrF6NjFOwG0> M4f0N|I2Ojd5NESx
U373VR MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2DqbFch\A>? Ml3TSG1UVw>? MWjHTVUxRTJ6OD64xtE{OyEQvF2= NIfVUJYzPTJ5N{S0NS=>
U87MG MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUP4dVZSPyCm NHe0TmtFVVOR M3:wNGdKPTB;M{iuN:KyOjBizszN Ml;sNlUzPzd2NEG=
HCT116 NInNXYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY[3JIQ> Mlm3SG1UVw>? MXHHTVUxRTV5OT65xtE{OiEQvF2= MlXFNlUzPzd2NEG=
DLD1 MoXFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHDO{Bl NUjmWFdVTE2VTx?= M2TIWGdKPTB;NUCxMlTDuTl|IN88US=> M{L5elI2Ojd5NESx
MRC5 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnybGk4KGR? MnezSG1UVw>? NYfLVHA3T0l3ME20OFkvPMLzODFOwG0> NGr5TXAzPTJ5N{S0NS=>
SNB19V  Mni2SpVv[3Srb36gRZN{[Xl? NGXCToYyODBizszNxsBVVVp? Ml:4NE04OiCq MV;pcoNz\WG|ZYOg{tNJOkG[IHX4dJJme3Orb36gZoV1f2WnbjCxOkBidmRiN{KgbC=> NIfIXpozPTJ5N{S0NS=>
T98G  NWXkbHd5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlPnOU8yOC9zNTFOwG0> M{\nfFI1yqCq MmWybY5lfWOnczDj[YxtKGSnYYToJIRwe2VvZHXw[Y5l\W62bImgZYZ1\XJiY3;uZ49ucXSjboSteIVud3qxbH;tbYRmKHerdHigUnBmPi2SRGS= MofrNlUzPjJ7NkG=
U251  MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rWVVUwOTBxMUWg{txO M1q3SlI1yqCq NIO4O2NqdmS3Y3XzJINmdGxiZHXheIgh\G:|ZT3k[ZBmdmSnboTsfUBi\nSncjDjc45kd22rdHHueE11\W2xen;sc41q\GVid3n0bEBPWGV4LWDEWC=> NH7tOmUzPTJ4Mkm2NS=>
T98G  NYXwSpAxTnWwY4Tpc44hSXO|YYm= NU\Ub|h1OTVizszN M{fTbVI1yqCq M2flbIlv[3KnYYPld{BFVkFvZoLh[41mdnSjdHnvckBqdiCQUHW2MXBFXCC2cnXheIVlKGeuaX;tZUBk\Wyucx?= MnT0NlUzPjJ7NkG=
U251  MX\GeY5kfGmxbjDBd5NigQ>? NX;nfoxROTVizszN NEiyflMzPMLiaB?= NGLvbFlqdmO{ZXHz[ZMhTE6DLX\yZYdu\W62YYTpc44hcW5iTmDlOk1RTFRidILlZZRm\CCpbHnvcYEh[2WubIO= NVntWXZHOjV{NkK5OlE>
U-87 MG NXzDOGZoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWjLTZJvPzJiaB?= Mn\YTWM2OD1yLkmzJI1OyqB? MkjKNlUzPDV|M{K=
U-118 MG NWPM[3RRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEK3fIU4OiCq NFPvOmNKSzVyPUGuNFUhdU4EoB?= MnT1NlUzPDV|M{K=
U87 M{Tsb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\WNlQhcA>? MYXJR|UxRTJ4MD6zOEDPxE4EoB?= M{PjZ|I2OTd|MkOz
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U87MG NGK1VFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUC3NkBp NVjYTHRyUUN3ME2xOU43OjVizszNxsA> M{SySVI2ODVyOUG1
U251 M3\BT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVyxNFAuPDByIN88US=> MoX3OFghcA>? NHHPOoFFVVOR NHfkc|ZqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M1XDfFI1PjJ|N{O2
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MDA-MB-231-br M{TvNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGnkXXExNTFyIN88US=> MYS0PEBp NVzJ[HFMTE2VTx?= M321[4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NX3mVFJVOjR4MkO3N|Y>
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MDA-MB-231 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWj4bWlyOC12MDFOwG0> MYi0PEBp MmnnSG1UVw>? Mm\5bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MmrCNlQ3OjN5M{[=
MDA-MB-468 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrR[GwxNTVyMDFOwG0> MYm0PEBp Mn3rSG1UVw>? MknBbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MYiyOFYzOzd|Nh?=
T47D NX3Fe4x2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWe3dJB[OC1zMECg{txO NXS0UVN4PDhiaB?= NXHxdnhjTE2VTx?= MUfpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NUnaTnVyOjR4MkO3N|Y>
MCF7 NF20enJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnT3NE0yODByIN88US=> MWe0PEBp MmGxSG1UVw>? MoPZbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MVGyOFYzOzd|Nh?=
Hs683 MmLCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUP1Z48{OC1zMECwJO69VQ>? MnTIPVYhcA>? NWXN[WE2UUN3ME2xNlgvQSEQvF2= NFvEcXAzPDR7NUmwOy=>
U87 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTuNE0yODByIN88US=> MnvoPVYhcA>? MWjJR|UxRTF6LkS1JO69VQ>? Mn3ONlQ1QTV7MEe=
LNZ308 NIixUHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWH3b2pHOC1zMECwJO69VQ>? NGPZeXg6PiCq MVXJR|UxRTN{Nj63JO69VQ>? M2\ZeFI1PDl3OUC3
U87 NETZZW9CeG:ydH;zbZMhSXO|YYm= NFu4NocyODBizszN NFn3XWs1QCCq NXP1PJB7TE2VTx?= NEDseYdqdmO{ZXHz[ZMhfGinIHPhd5Bie2VvMz:3JIFkfGm4aYT5 Mn\yNlQ1QDF3OE[=
U251  NGLCSlVCeG:ydH;zbZMhSXO|YYm= MXmxNFAh|ryP MUS0PEBp NWHrRXdWTE2VTx?= NGrv[nBqdmO{ZXHz[ZMhfGinIHPhd5Bie2VvMz:3JIFkfGm4aYT5 MWqyOFQ5OTV6Nh?=
U251 M4j5SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUD1d2tUOjRiaB?= NIfjeppKSzVyPUi2MlI66oDLwsJihKkyNjV6IN88US=> NHXxPHczPDN{Nkm1OC=>
U251 MnTsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorUOFghcA>? M1\pfWlEPTB;N{WuN|TjiIoEsfMAjVEvODJizszN MWKyOFMzPjl3NB?=
U251 NGrOZ5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MorwO|IhcA>? NILLTZNKSzVyPUeyMlQz6oDLwsJihKkyNjR3IN88US=> NYLR[YhbOjR|Mk[5OVQ>
U251 NV\mcJMzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nJVVk3KGh? MWjJR|UxRTZ7Lkiy5qCKyrIkgJmzMlA1KM7:TR?= M3PWV|I1OzJ4OUW0
T98G MkfPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjyNWh6OC15NUCg{txO MmnqO|IwQTZiaB?= NHvkc2VqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDpckBiKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= MnLmNlQ{OjRyOEC=
U251-MG NGTxTXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnMeWwxNThyMDFOwG0> MUK3NkBp MonWbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NHTXNoYzPDB7M{[zNC=>
D54-MG NHfac5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFiyRpIxNThyMDFOwG0> MmLhO|IhcA>? Mmq0bY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? M1Oxb|I1ODl|NkOw
SHG-44 MorES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XIOlExNTJyMDFOwG0> MlzZPVYhcA>? NXWwOWx5UUN3ME25Mlc{KMLzIEKuNVIh|ryP M1T2blI1ODZ3NU[5
U373  NHTFPIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXWOJIyOC1{MECg{txO NYjLbphsQTZiaB?= M3XtO2lEPTB;MUCuNVMhyrFiMT6wNkDPxE1? MnfCNlQxPjV3Nkm=
HT-29  Mlz5SpVv[3Srb36gRZN{[Xl? NFfZSlg2ODBizszN NEOwXWMzPC92ODDo M{n0SIVvcGGwY3XzJJRp\SCuZY\lcJMhd2ZizsOtTFJCYMLi NX\CXW92OjRyM{iwOlg>
PC-3  Ml;qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnLmNE0zPSEQvF2= MnPPOFghcA>? MYjpcohq[mm2czDj[YxtKGe{b4f0bEB4cGmlaDDjZY4h[mVicH;0[Y51cWG2ZXSgZpkhdHmlb4DlcoU> Mny4NlM4PDZ7M{S=
PC-3  NV\sR4V6SXCxcITvd4l{KEG|c3H5 NX[1bmxuOjVizszN M3\JVlQ5KGh? MkjYbY5lfWOnczDhdI9xfG:|aYOge4hq[2hiY3HuJIJmKHCxdHXueIlifGWmIHL5JIx6[2:yZX7l NXPXW|VlOjN5NE[5N|Q>
T98G NFPXRY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljlOVAuPDByIN88US=> NHvDU|UyPDRiaB?= M1u4cYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHnuJIEh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ M{Pu[|I{PzF3NEm5
U87-MG MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTjO4pWOTByINM1US=> NUDkfHFXPzJiaB?= M4nWcolvcGmkaYTzJINmdGxiZ4Lve5RpKHeqaXPoJINidiCkZTDlcohidmOnZDDifUBIXEJ? NH3BNIozOzZ7Nke4PC=>
U251-MG Mon3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4T3VlExOCEEtV2= NXXZUoFrPzJiaB?= M4\WRYlvcGmkaYTzJINmdGxiZ4Lve5RpKHeqaXPoJINidiCkZTDlcohidmOnZDDifUBIXEJ? MYGyN|Y6Pjd6OB?=
LNT-229 MnTqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkDZN{0yODBizszN MnjmNlQhcA>? M4Xi[IlvcGmkaYTzJINtd26xZ3XubYMhe3W{dnn2ZYwhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MUmyN|Y3PzZ|Mh?=
T98G NVj1eFNlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXSNVAuPzByIN88US=> NH3UTG8zPCCq NYjlTJp1cW6qaXLpeJMh[2yxbn;n[Y5q[yC|dYL2bZZidCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NVXue4dxOjN4Nke2N|I>
U87  NFjDVppHfW6ldHnvckBCe3OjeR?= Ml3vNVAxKML3TR?= Mm\qN{Bp MU\lcIV3[XSnczD0bIUhdGW4ZXzzJI9nKHCFaHuxJIFv\CCyQ3jrNi=> M1H4R|I{PjZ5NE[5
HCT116 NV\yVIpMTnWwY4Tpc44hSXO|YYm= MUWxNFAhyrWP NWXZbFlMOyCq M4rPRolv\HWlZYOgeIhmKEOqa{GgVIhwe3Cqb4L5cIF1cW:w NYPpTWdYOjN4Nke0Olk>
HCT3-6 MUHGeY5kfGmxbjDBd5NigQ>? MVyxNFAhyrWP MUOzJIg> M{XwU4lv\HWlZYOgeIhmKEOqa{GgVIhwe3Cqb4L5cIF1cW:w NX\Wc2x[OjN4Nke0Olk>
U-87  MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\0WlcxNTRyIN88US=> NWm2NY9TOTJiZB?= NX36Zmw3cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NV\lOpI5OjN4NEW3Nlk>
U-87  M4W4SmFxd3C2b4Ppd{BCe3OjeR?= MkfSNE01OCEQvF2= NFLMb3A{NzZiZB?= MVfpcoR2[2W|IHHwc5B1d3OrczDpckBjd3SqIHTvd4UuKGGwZDD0bY1mNWSncHXu[IVvfCCvYX7u[ZI> MViyN|Y1PTd{OR?=
U-87  MYXGeY5kfGmxbjDBd5NigQ>? MUSwMVQxKM7:TR?= NWPrdohQOy94IHS= NYC1NlVucW6mdXPld{BifXSxcHjh[5khcW5iYn;0bEBld3OnLTDhcoQhfGmvZT3k[ZBmdmSnboSgcYFvdmW{ NUfqZXp{OjN4NEW3Nlk>
GB-SCC010 MofkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVO0JIQ> M3LyO2lEPTB;MkK2JO69VQ>? MWiyN|YyOjd3NR?=
GB-SCC026 NYDVb5U3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrnOEBl NGnpU3pKSzVyPUWzMlEh|ryP M3ey[lI{PjF{N{W1
GB-SCC028 NHXFXohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXrOEBl MYrJR|UxRTF4NzFOwG0> NIjOeHgzOzZzMke1OS=>
U87 NV;zcpZjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUHxc4VVPCCm NV36WnkxUUN3ME20OU4zKM7:TR?= NFX0XVAzOzZzMke1OS=>
U87 stem cell NV\tUIRLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWf2Wm9ZPCCm NFf5NVRKSzVyPU[2Mlch|ryP M32xPVI{PjF{N{W1

... 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]

+ Expand
  • 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]

+ Expand
  • 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 (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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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 )

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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)
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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
NCT03935685 Recruiting Drug: Mirtazapine (Remeron) Glioma of Brain University of California Irvine February 26 2019 Early 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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID