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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Cited by 18 Publications

7 Customer Reviews

  • C57BL/6 mice were implanted in the striatum with citrine-GL26-Cherry-HMGB1, which were stably transfected to express the YFP citrine and HMGB1 fused to red fluorescent protein cherry. Fourteen days later, they were treated with saline, Ad-TK+Ad-Flt3L, or Ad-TK+Ad-Flt3L+TMZ (temozolomide). Five days after treatment, the cellular location of cherry-HMGB1 in these cells was assessed by confocal microscopy. Arrows, tumor cells (green) with cytoplasmic HMGB1 (red).

    Clin Cancer Res 2014 20(6), 1555-65. Temozolomide purchased from Selleck.

  • D, Scramble (SCR), H82, H865, and H1836 cells were treated with AZD1775 (100 nmol/L) and temozolomide (1 μmol/L) for 24 hours; WEE1 KD cells were treated with just temozolomide (1 μmol/L) for 24 hours. The cells were lysed at 24 hours and subjected to Western blot analysis for phosphorylated WEE1 (pWEE1_S642), pCDC2_Y15 (WEE1 downstream effector), γH2AX (DNA damage marker), PH3 (mitotic marker), cleaved caspase-3 (apoptotic marker), and actin (loading control). E, SCR and WEE1 KD H82, H865, and H1836 cells were treated as described in D and subjected to Western blot analysis for DNA repair markers pATM_S1981, MRE11, RAD51, and E2F1. Actin was used as a loading control.

    Clin Cancer Res, 2017, 23(20):6239-6253. Temozolomide purchased from Selleck.

  • Talazoparib and temozolomide exhibit marked combinatorial efficacy in PDXs. A, Western blot against MGMT by near-infrared imaging in PDX models.

    Clin Cancer Res, 2017, 23(2):523-535. Temozolomide purchased from Selleck.

  • J Control Release, 2018, 269:245-257. Temozolomide purchased from Selleck.

  • Viability of U87 cells(A) assessed by the Alamar blue assay, 72 h after transfection with siRNA anti-survivin (siSURV) or with siMUT and/or cell incubation with the chemotherapeutical drugs temozolomide (TMZ) and Bliss interaction index (B) determined for the combined effects on cell viability of survivin silencing plus treatment with each drug. Cells were transfected, for 4 h, with (14Ser)2N5/siRNA/HL complexes and, after an additional period of 20 h, cells were incubated with 400 μM TMZ(A) for 48 h. Results, representative of at least three independent experiments, are expressed as a percentage of the nontreated control cells. Combined treatment (dotted bar) was compared with the single drug treatment (gray bar) (**p < 0.01, ***p < 0.001) and the Bliss interaction index of each combined treatment was compared with the theoretical value expected for an additive effect (1.0) (#p < 0.05, ns, non-significant).

    Eur J Pharm Biopharm, 2016, 104:7-18.. Temozolomide purchased from Selleck.

  • Cells were plated and 12 h after plating were treated with MMF (5 µM), FTY720 (50 nM), Temozolomide (TMZ, 3 µM) or in combination as indicated for 12 h. Cell viability was assessed by live / dead assay.

    Cancer Biol Ther, 2014, 15(12):1646-57. Temozolomide purchased from Selleck.

  • Establishment of TMZ-resistant (TR) GBM cell lines. a-d, Evaluation of temozolomide resistance in four glioblastoma cell lines. Cells were cultured in the presence of 5-600 μM of TMZ. A dose-dependent association between the survival rate of cells and TMZ concentration can be observed. Each group was cultured for 24 h in the presence of different concentrations of TMZ, followed by an evaluation of IC50 for TMZ inhibited growth in A172-TR/A172, U118-TR/U118, U251-TR/U251 and U87-TR/U87

    Neurochem Res, 2016, 41(12):3192-3205. Temozolomide purchased from Selleck.

Purity & Quality Control

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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.
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 NIjaclBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUC0PEBp NGPxe4FKSzVyPUGzPU4zOOLCidMx5qCKPS57NTFOwG0> MkfENlU6PjB{OEK=
KellyCis83 NIT5bmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17HfFQ5KGh? MU\JR|UxRTJ3MT6wNQKBkcLz4pEJNVUvPzVizszN NFrhXXgzPTl4MEK4Ni=>
SK-N-AS Mom0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mkm4OFghcA>? MVrJR|UxRTJ{Nz63NQKBkcLz4pEJNlIvOTVizszN NFPjWpMzPTl4MEK4Ni=>
SK-N-ASCis24 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILlWow1QCCq NYLBRmpJUUN3ME20PFAvPjEkgJpCtgKBkTFyMT6xOUDPxE1? MYqyOVk3ODJ6Mh?=
CHP-212 NYDPephUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1PGeFQ5KGh? MUjJR|UxRTdwOUhihKnDueLCiUCuOlkh|ryP NIHuW5gzPTl4MEK4Ni=>
CHP-212Cis100 NVvPXnN[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2n3bVQ5KGh? M{nSU2lEPTB;OT61OgKBkcLz4pEJNE45QCEQvF2= Ml\YNlU6PjB{OEK=
U87  MX;GeY5kfGmxbjDBd5NigQ>? NX\VXmFLOTByIN88US=> MVOyOE04OiCq M4H4eIlv\HWlZYOgSINTOSCneIDy[ZN{cW:w MUGyOVgxQDh4OB?=
LN229 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVGwMVUxKM7:TR?= NYHhWlFVUUN3ME2xOkDPxE1? NVzWNJRyOjV5NUCyO|M>
TR-LN229 NYXTb3dpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPYSWkxNTVyIN88US=> NYPxbok{UUN3ME23O{DPxE1? Ml3kNlU4PTB{N{O=
U87  M1zyU2Fxd3C2b4Ppd{BCe3OjeR?= M{XoNlDjiJN{MEFihKnDvU1? MUGyOEBp MVrlcohidmOnczDDVUBqdmS3Y3XkJIFxd3C2b4Ppdy=> MnzjNlU3QDF4Nki=
U251MG M3nmXmFxd3C2b4Ppd{BCe3OjeR?= NUPPepN3OTBywrFOwG0> NFvq[Jo1QCCq NUDoWHduWEKV M2j6Zolv\HWlZYOgZZBweHSxc3nz M3HJOFI2PjhyNE[0
U87MG MVHBdI9xfG:|aYOgRZN{[Xl? MUCxNFDDqM7:TR?= MXe0PEBp MoLNVGJU MU\pcoR2[2W|IHHwc5B1d3Orcx?= MWKyOVY5ODR4NB?=
U87 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnHrOVAuOzVyIN88US=> MXu0POKhcMLi M1f1RolvcGmkaYTzJINmdGxiZ4Lve5RpKHOuaXfoeIx6 M1;WRVI2PTV2MkKz
U118  MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\KNHI2OC1|NUCg{txO M1HtXlQ5yqCqwrC= MnrFbY5pcWKrdIOgZ4VtdCCpcn;3eIghe2yrZ3j0cJk> NWXvcYFtOjV3NUSyNlM>
U87 M4jG[WZ2dmO2aX;uJGF{e2G7 NX;FO3JlOjVyL{O1NEDPxE1? MXO0POKhcMLi MmrU[Y5p[W6lZYOgWG1ZNWmwZIXj[YQheC2SS1OtdIFvKGSnY4LlZZNm M2rWVFI2PTV2MkKz
U118  NVvNXIxuTnWwY4Tpc44hSXO|YYm= NI\YVY8zPTBxM{WwJO69VQ>? NH;xOmU1QMLiaNMg NFrnPGRmdmijbnPld{BVVVhvaX7keYNm\CCyLWDLR{1x[W5iZHXjdoVie2V? MXKyOVU2PDJ{Mx?=
U87 M{PoOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVGyOVAwOzVyIN88US=> MYq0POKhcMLi MXHpcoNz\WG|ZYOgeIhmKHCncnPlcpRi\2Vib3[gZ4VtdHNiaX6gV{BidmRiR{KvUeKh[2:2cnXheIVlKHerdHigWG1Z M334elI2PTV2MkKz
A375 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mkf6OFjDqGkEoB?= MkfhTWM2OD1{NkWg{txO MUCyOVUzPDV3Mh?=
A2058 NIC2fIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHTOHo1QMLiaNMg MW\JR|UxRTF{IN88US=> MmjBNlU2OjR3NUK=
M238 NGXjVGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXy0POKhcMLi MojkTWM2OD12MDFOwG0> Mn3HNlU2OjR3NUK=
M249 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1XUd|Q5yqCqwrC= M{Wy[GlEPTB;MkW0JO69VQ>? MmniNlU2OjR3NUK=
M21 M{PGTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mke4OFjDqGkEoB?= NYK2cpdxUUN3ME2yNlEh|ryP MXiyOVUzPDV3Mh?=
U251 MWfDfZRwfG:6aYT5JGF{e2G7 NGfrOIQzOCEQvF5CpC=> NYnrcGtWPDkEoHlCpC=> M37sfJJm\HWlZXTzJJRp\SCyZYLj[Y51[WenczDv[kBkd2yxbnnld{Bnd3KvZXS= NUHFcWhNOjV2M{SzPFE>
LN229 NGr2OmZEgXSxdH;4bZR6KEG|c3H5 M{jCe|IxKM7:TdMg Ml7pOFjDqGkEoB?= MmP4doVlfWOnZIOgeIhmKHCncnPlcpRi\2W|IH;mJINwdG:waXXzJIZwem2nZB?= NUPIdnB7OjV2M{SzPFE>
U373MG-LUC MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M36yeFczKGh? MmPxTWM2OD54MECg{txO MU[yOVQ{OTl3Mx?=
U87  M4TJNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfQcXNYOjVvMkCwJO69VQ>? M4nYZ|Q5yqCqwrC= MYHpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M1\xVFI2PDByN{S1
U251 NF;mWnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXOyOU0zODBizszN MXG0POKhcMLi MYfpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MXGyOVQxODd2NR?=
U251 NFPzNXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnabI1ROTByLUSwNEDPxE1? Mlv6O|IwQTZiaB?= Mn\6eIhmKGGwdHmtdJJwdGmoZYLheIl3\SCnZn\lZ5Qh[2GwIHLlJIVvcGGwY3XkJIJ6KGexc4P5dI9tKGWwaHHuZ4VlKMLi NEDWdJkzPTN5NUK3NS=>
U373 M33hbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkDSNVAxNTRyMDFOwG0> M1L6W|czNzl4IHi= NUT0NpY5fGinIHHueIkueHKxbHnm[ZJifGm4ZTDl[oZm[3RiY3HuJIJmKGWwaHHuZ4VlKGK7IHfvd5N6eG:uIHXubIFv[2WmINMg M3qwRVI2Ozd3Mkex
U343 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGD2eVAyODBvNECwJO69VQ>? NXjpSVNnPzJxOU[gbC=> MkLzeIhmKGGwdHmtdJJwdGmoZYLheIl3\SCnZn\lZ5Qh[2GwIHLlJIVvcGGwY3XkJIJ6KGexc4P5dI9tKGWwaHHuZ4VlKMLi MXSyOVM4PTJ5MR?=
U87MG-luc2 NWPBOI5KT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkTwNVAxNTRyMDFOwG0> MlKwO|IwQTZiaB?= MVX0bIUh[W62aT3wdo9tcW[ncnH0bZZmKGWoZnXjeEBk[W5iYnWg[Y5p[W6lZXSgZpkh\2:|c4nwc4wh\W6qYX7j[YQhyqB? MnzxNlU{PzV{N{G=
U87 NEPBUFBHfW6ldHnvckBCe3OjeR?= NVLQNJh1OjByIN88US=> MUW0PEBp MlzBbY5kemWjc3XzJGJTS0N|IH3SUmEh\XiycnXzd4lwdg>? M2HiZVI2OzN5N{Kx
U251 NH7lbotHfW6ldHnvckBCe3OjeR?= MXqyNFAh|ryP Mo[wOFghcA>? MmP3bY5kemWjc3XzJGJTS0N|IH3SUmEh\XiycnXzd4lwdg>? NX7lb4J6OjV|M{e3NlE>
A172 MnTrSpVv[3Srb36gRZN{[Xl? MoLGNlAxKM7:TR?= NEjrVno1QCCq NWLGd4RjcW6lcnXhd4V{KEKUQ1OzJI1TVkFiZYjwdoV{e2mxbh?= NGL4OWEzPTN|N{eyNS=>
U251 Mo[xSpVv[3Srb36gRZN{[Xl? NGewUG4zODBizszN MYm0PEBp NH;QPJRqdmO{ZXHz[ZMhfGinIHX4dJJme3Orb36gc4YhSlKFQUGsJGJTS0F{LDDSRWQ2OSCjbnSgSmFPS0R{ M3K3SFI2OzN5N{Kx
A172 NGq2OIRHfW6ldHnvckBCe3OjeR?= NEK1ZpozODBizszN M3jJSVQ5KGh? MXLpcoNz\WG|ZYOgeIhmKGW6cILld5Nqd25ib3[gRnJESTFuIFLSR2EzNCCUQVS1NUBidmRiRlHOR2Qz M2LIbFI2OzN5N{Kx
U87 M171RmZ2dmO2aX;uJGF{e2G7 NGexcmgzODBizszN MYeyOE84Oi9zMkCgbC=> M1f4NIlv[3KnYYPld{DPu0h{QWig[o9kcSCob4LtZZRqd25idHnt[U1l\XCnbnTlcpRtgQ>? MVqyOVM{Pzd{MR?=
U251 NILXXopHfW6ldHnvckBCe3OjeR?= MVWyNFAh|ryP MYeyOE84Oi9zMkCgbC=> MknvbY5kemWjc3XzJO6{UDKDWDDmc4NqKG[xcn3heIlwdiC2aX3lMYRmeGWwZHXueIx6 M4DSO|I2OzN5N{Kx
A172 MkPWSpVv[3Srb36gRZN{[Xl? MkPTNlAxKM7:TR?= NVnMRmp4OjRxN{KvNVIxKGh? M2ixRolv[3KnYYPld{DPu0h{QWig[o9kcSCob4LtZZRqd25idHnt[U1l\XCnbnTlcpRtgQ>? MXeyOVM{Pzd{MR?=
SNB19V NU\Rdok3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4npSFch\A>? NYr2cJB{TE2VTx?= MXfHTVUxRTN3LkhCtVEzKM7:TR?= MkPDNlUzPzd2NEG=
SNB19M NX7nU5dQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWO3JIQ> NVfKb2RVTE2VTx?= MWfHTVUxRTR4OT65xtE5QCEQvF2= NWC3cGJuOjV{N{e0OFE>
SNB19VR MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1q3NVch\A>? MmfCSG1UVw>? NYfEc5pRT0l3ME2yPFAvOsLzMUig{txO Mm\rNlUzPzd2NEG=
U373V M2DpOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{L0ZVch\A>? NWX6dGtoTE2VTx?= NGqzZppIUTVyPU[4MlDDuTN{IN88US=> NXnEWFVROjV{N{e0OFE>
U373M NVL2[YpDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrsO{Bl NGHoPGVFVVOR MVPHTVUxRTN4OD63xtE5PiEQvF2= NH7tWWgzPTJ5N{S0NS=>
U373VR MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PhS|ch\A>? NGG5bVNFVVOR NHvBUJBIUTVyPUK4PE45yrF|MzFOwG0> NYroN4tvOjV{N{e0OFE>
U87MG MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\6T|ch\A>? MXvEUXNQ M3SzN2dKPTB;M{iuN:KyOjBizszN MoPlNlUzPzd2NEG=
HCT116 NV\HPZY3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYm3JIQ> M{O0WWROW09? Mlz0S2k2OD13N{muPeKyOzJizszN MmfqNlUzPzd2NEG=
DLD1 MknLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXW3JIQ> NGTNSmRFVVOR NXXSemZsT0l3ME21NFEvPMLzOUOg{txO MV2yOVI4PzR2MR?=
MRC5 MmflS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LTb|ch\A>? M1SxTmROW09? MmrpS2k2OD12NEmuOOKyQCEQvF2= Mo\FNlUzPzd2NEG=
SNB19V  MVrGeY5kfGmxbjDBd5NigQ>? NVn4eY5POTByIN88UeKhXE2c M2LoSVAuPzJiaB?= NHP1UGVqdmO{ZXHz[ZMh|rOKMlHYJIV5eHKnc4Ppc44h[mW2d3XlckAyPiCjbnSgO|IhcA>? NXnMUYlUOjV{N{e0OFE>
T98G  NH3INY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVG1M|ExNzF3IN88US=> MXuyOOKhcA>? M1LDOIlv\HWlZYOgZ4VtdCCmZXH0bEBld3OnLXTldIVv\GWwdHz5JIFnfGW{IHPvcoNwdWm2YX70MZRmdW:8b3zvcYll\SC5aYToJG5R\TZvUFTU M{PsdFI2OjZ{OU[x
U251  M3\TWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYG1M|ExNzF3IN88US=> M4m4[VI1yqCq MoXjbY5lfWOnczDj[YxtKGSnYYToJIRwe2VvZHXw[Y5l\W62bImgZYZ1\XJiY3;uZ49ucXSjboSteIVud3qxbH;tbYRmKHerdHigUnBmPi2SRGS= M1nyZlI2OjZ{OU[x
T98G  MknpSpVv[3Srb36gRZN{[Xl? M1PYclE2KM7:TR?= Ml\3NlTDqGh? MXfpcoNz\WG|ZYOgSG5CNW[{YXft[Y51[XSrb36gbY4hVlCnNj3QSHQhfHKnYYTl[EBodGmxbXGgZ4VtdHN? MnfHNlUzPjJ7NkG=
U251  MV\GeY5kfGmxbjDBd5NigQ>? MV2xOUDPxE1? NHf3cFIzPMLiaB?= NYKzd|B5cW6lcnXhd4V{KESQQT3mdoFodWWwdHH0bY9vKGmwIF7Q[VYuWESWIITy[YF1\WRiZ3zpc41iKGOnbHzz MlPZNlUzPjJ7NkG=
U-87 MG NIn5VmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYrXcZJDPzJiaB?= M{XoV2lEPTB;MD65N{BuVcLi Mn7wNlUzPDV|M{K=
U-118 MG M3HJfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjDXoRyPzJiaB?= MUHJR|UxRTFwMEWgcW3DqA>? MXuyOVI1PTN|Mh?=
U87 NUTGN4J4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jYfVI1KGh? MkHwTWM2OD1{NkCuN|Qh|ryPwrC= MX2yOVE4OzJ|Mx?=
U87 GSLCs MmWzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFe1eo0zPCCq M2nzeWlEPTB;N{[2MlEyKM7:TdMg MkDtNlUyPzN{M{O=
U87MG MoG4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MneyO|IhcA>? MnHMTWM2OD1zNT62NlUh|ryPwrC= NUfjWoZXOjVyNUC5NVU>
U251 NVvmSZN6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjDfHUyODBvNECwJO69VQ>? MYq0PEBp NVH5W3ZtTE2VTx?= MYnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NYT2eWNuOjR4MkO3N|Y>
U87 MlXuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\Fb2QyODBvNECwJO69VQ>? NGW5bHo1QCCq MWHEUXNQ NGjB[FdqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MlH3NlQ3OjN5M{[=
MDA-MB-231-br M1TKWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPONE0yOCEQvF2= NWLJd29SPDhiaB?= MXrEUXNQ MVjpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M3vOXVI1PjJ|N{O2
HCC-1937 Mk\wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPyNE0{ODBizszN NYq5colEPDhiaB?= M3S2OmROW09? NVjFNVR5cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M3v0V|I1PjJ|N{O2
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U251  NXf5fodSSXCxcITvd4l{KEG|c3H5 NGmzNGYyODBizszN M4rKZlQ5KGh? NIjLc3lFVVOR MnK0bY5kemWjc3XzJJRp\SClYYPwZZNmNTNxNzDhZ5Rqfmm2eR?= MYSyOFQ5OTV6Nh?=
U251 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYeyOEBp MojjTWM2OD16Nj6yPgKBkcLz4pEJNU42QCEQvF2= NUHEWVZ7OjR|Mk[5OVQ>
U251 Ml;zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYG0PEBp NGjJ[29KSzVyPUe1MlM16oDLwsJihKkyNjB{IN88US=> MUeyOFMzPjl3NB?=
U251 M1rL[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkixO|IhcA>? MWHJR|UxRTd{LkSy5qCKyrIkgJmxMlQ2KM7:TR?= MXSyOFMzPjl3NB?=
U251 MmL1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPCWnprQTZiaB?= NEjPVVlKSzVyPU[5Mlgz6oDLwsJihKk{NjB2IN88US=> NYCwTWZwOjR|Mk[5OVQ>
T98G NGLFXoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPF[5kxNTd3MDFOwG0> NHHSeZY4Oi97NjDo MV3pcohq[mm2czDj[YxtKH[rYXLpcIl1gSCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MV6yOFMzPDB6MB?=
U251-MG MoXWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfZOY5IOC16MECg{txO MWG3NkBp NV71TpIzcW6qaXLpeJMh[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK= NEDX[ZYzPDB7M{[zNC=>
D54-MG MonKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XVcFAuQDByIN88US=> MXy3NkBp NEf4bnpqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDpckBiKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= MYGyOFA6OzZ|MB?=
SHG-44 M2fDWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17lXVExNTJyMDFOwG0> MkfCPVYhcA>? NH74Xo1KSzVyPUmuO|MhyrFiMj6xNkDPxE1? NHvneHEzPDB4NUW2PS=>
U373  MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFmzZmUyOC1{MECg{txO M1nxeFk3KGh? NGjr[Y5KSzVyPUGwMlE{KMLzIEGuNFIh|ryP MnrTNlQxPjV3Nkm=
HT-29  MUPGeY5kfGmxbjDBd5NigQ>? MX21NFAh|ryP NFntOoEzPC92ODDo Mk\X[Y5p[W6lZYOgeIhmKGyndnXsd{Bw\iEQsz3INmFZyqB? MlvCNlQxOzhyNki=
PC-3  MmDCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG[zdZIxNTJ3IN88US=> NUjW[JJCPDhiaB?= NFuwXFhqdmirYnn0d{Bk\WyuIHfyc5d1cCC5aHnjbEBk[W5iYnWgdI91\W62aXH0[YQh[nlibInjc5BmdmV? MmPlNlM4PDZ7M{S=
PC-3  M2P6dWFxd3C2b4Ppd{BCe3OjeR?= Mn;DNlUh|ryP M3\wTVQ5KGh? MXrpcoR2[2W|IHHwc5B1d3OrczD3bIlkcCClYX6gZoUheG:2ZX70bYF1\WRiYomgcJlkd3CnbnW= Mn;2NlM4PDZ7M{S=
T98G NEfKdnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYK1NE01ODBizszN M4e0b|E1PCCq NFi3[lRqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDpckBiKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= Mm\PNlM4OTV2OUm=
U87-MG MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfQS2YyODBiwsXN MUe3NkBp M4r6N4lvcGmkaYTzJINmdGxiZ4Lve5RpKHeqaXPoJINidiCkZTDlcohidmOnZDDifUBIXEJ? M1HNRVI{Pjl4N{i4
U251-MG NWrMeIN2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4XUfFExOCEEtV2= NWLleXozPzJiaB?= M4nhWolvcGmkaYTzJINmdGxiZ4Lve5RpKHeqaXPoJINidiCkZTDlcohidmOnZDDifUBIXEJ? MV2yN|Y6Pjd6OB?=
LNT-229 Mk\qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLaN{0yODBizszN Mn;uNlQhcA>? NGLpTlJqdmirYnn0d{BkdG:wb3flcolkKHO3co\peoFtKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M2LCV|I{PjZ5NkOy
T98G MmToS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jFbVExNTdyMDFOwG0> MYeyOEBp MX7pcohq[mm2czDjcI9vd2enbnnjJJN2en[rdnHsJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MkPnNlM3Pjd4M{K=
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HCT116 NHvQfZhHfW6ldHnvckBCe3OjeR?= MlrHNVAxKML3TR?= MXGzJIg> M3PiNYlv\HWlZYOgeIhmKEOqa{GgVIhwe3Cqb4L5cIF1cW:w NFTMW5czOzZ4N{S2PS=>
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U-87  MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\xflAuPDBizszN MkXGNVIh\A>? NVqxUZhIcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MWGyN|Y1PTd{OR?=
U-87  M1f2fWFxd3C2b4Ppd{BCe3OjeR?= MlrjNE01OCEQvF2= NFLlUoE{NzZiZB?= NGHEfnZqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCkb4ToJIRwe2VvIHHu[EB1cW2nLXTldIVv\GWwdDDtZY5v\XJ? NH\1ZmEzOzZ2NUeyPS=>
U-87  Moq3SpVv[3Srb36gRZN{[Xl? NELwO28xNTRyIN88US=> Mlq5N{83KGR? MlzxbY5lfWOnczDheZRweGijZ4mgbY4h[m:2aDDkc5NmNSCjbnSgeIlu\S2mZYDlcoRmdnRibXHucoVz NIK2ZXMzOzZ2NUeyPS=>
GB-SCC010 M2[3S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfVdoI1KGR? M2T6PWlEPTB;MkK2JO69VQ>? M1L4c|I{PjF{N{W1
GB-SCC026 NYHDU4VlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfYcG5RPCCm M1XNVmlEPTB;NUOuNUDPxE1? NILtTlMzOzZzMke1OS=>
GB-SCC028 NVL1ZWNWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV20JIQ> M3v5fWlEPTB;MU[3JO69VQ>? M33hfVI{PjF{N{W1
U87 M1qwbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rsUVQh\A>? MUDJR|UxRTR3LkKg{txO Mm\5NlM3OTJ5NUW=
U87 stem cell NHHtPYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXy0JIQ> M2fWeGlEPTB;Nk[uO{DPxE1? MoftNlM3OTJ5NUW=

... 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)

  • 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 )

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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 Conditions Sponsor/Collaborators Start Date Phases
NCT03687034 Not yet recruiting Glioblastoma Leaf Vertical Inc. June 1 2019 Phase 1
NCT03776071 Not yet recruiting Glioblastoma Denovo Biopharma LLC June 2019 Phase 2
NCT03776071 Not yet recruiting Glioblastoma Denovo Biopharma LLC June 2019 Phase 2
NCT03880019 Not yet recruiting Stage III Uterine Corpus Leiomyosarcoma AJCC v8|Stage IIIA Uterine Corpus Leiomyosarcoma AJCC v8|Stage IIIB Uterine Corpus Leiomyosarcoma AJCC v8|Stage IIIC Uterine Corpus Leiomyosarcoma AJCC v8|Stage IV Uterine Corpus Leiomyosarcoma AJCC v8|Stage IVA Uterine Corpus Leiomyosarcoma AJCC v8|Stage IVB Uterine Corpus Leiomyosarcoma AJCC v8 National Cancer Institute (NCI) June 7 2019 Phase 2
NCT03880019 Not yet recruiting Stage III Uterine Corpus Leiomyosarcoma AJCC v8|Stage IIIA Uterine Corpus Leiomyosarcoma AJCC v8|Stage IIIB Uterine Corpus Leiomyosarcoma AJCC v8|Stage IIIC Uterine Corpus Leiomyosarcoma AJCC v8|Stage IV Uterine Corpus Leiomyosarcoma AJCC v8|Stage IVA Uterine Corpus Leiomyosarcoma AJCC v8|Stage IVB Uterine Corpus Leiomyosarcoma AJCC v8 National Cancer Institute (NCI) June 7 2019 Phase 2
NCT03687034 Not yet recruiting Glioblastoma Leaf Vertical Inc. June 1 2019 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