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TMZ(Temozolomide)

别名: NSC 362856,CCRG 81045,Methazolastone 中文名称：替莫唑胺

此产品请避光密封保存。

TMZ(Temozolomide)是一种单功能的SN-1烷化剂，修饰DNA环上的氮原子以及环外氧基团。在生理pH值下，TMZ转化为活性产物MTIC、降解为methyldiazonium cation，后者再将甲基转移到DNA, 阻碍DNA复制启动，诱使细胞凋亡，是一种DNA损伤诱导剂。Temozolomide可诱导凋亡并具有抗肿瘤的活性。

TMZ(Temozolomide) Chemical Structure

TMZ(Temozolomide) Chemical Structure

CAS: 85622-93-1

规格 价格 库存 购买数量
10mM (1mL in DMSO) 647.01 现货
25mg 574.37 现货
100mg 1411.95 现货
1g 4668.3 现货
5g 13996.71 现货
10g 22416.03 现货
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TMZ(Temozolomide)相关产品

相关信号通路图

DNA/RNA Synthesis Signaling Pathways

DNA/RNA Synthesis信号通路图

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息(PMID)
U251  Function Assay 15 μM 24 h increases DNA-fragmentation in NPe6-PDT treated glioma cells 25262961
T98G  Function Assay 15 μM 24 h increases DNA-fragmentation in NPe6-PDT treated glioma cells 25262961
U251  Growth Inhibition Assay 5/10/15 μM 24 h induces cell death dose-dependently after concomitant-temozolomide with NPe6-PDT 25262961
T98G  Growth Inhibition Assay 5/10/15 μM 24 h induces cell death dose-dependently after concomitant-temozolomide with NPe6-PDT 25262961
SNB19V  Function Assay 100 μM TMZ 0-72 h increases γH2AX expression between 16 and 72 h 25277441
A172 Function Assay 200 μM 24/72/120 h increases γH2AX foci formation time-dependently 25337721
U251 Function Assay 200 μM 24/72/120 h increases γH2AX foci formation time-dependently 25337721
U87 Function Assay 200 μM 24/72/120 h increases γH2AX foci formation time-dependently 25337721
A172 Function Assay 200 μM 48 h increases the expression of BRCA1, BRCA2, RAD51 and FANCD2 25337721
U251 Function Assay 200 μM 48 h increases the expression of BRCA1, BRCA2, RAD51 and FANCD2 25337721
A172 Function Assay 200 μM 48 h increases BRCC3 mRNA expression 25337721
U251 Function Assay 200 μM 48 h increases BRCC3 mRNA expression 25337721
U87 Function Assay 200 μM 48 h increases BRCC3 mRNA expression 25337721
U87MG-luc2 Growth Inhibition Assay 100-400 μM 72/96 h the anti-proliferative effect can be enhanced by gossypol enhanced   25375271
U343 Growth Inhibition Assay 100-400 μM 72/96 h the anti-proliferative effect can be enhanced by gossypol enhanced   25375271
U373 Growth Inhibition Assay 100-400 μM 72/96 h the anti-proliferative effect can be enhanced by gossypol enhanced   25375271
U251 Growth Inhibition Assay 100-400 μM 72/96 h the anti-proliferative effect can be enhanced by gossypol enhanced   25375271
U251 Growth Inhibition Assay 25-200 μM 48 h  inhibits cell growth in a dose-dependent manner 25400745
U87  Growth Inhibition Assay 25-200 μM 48 h  inhibits cell growth in a dose-dependent manner 25400745
LN229 Cytotoxity Assay 20 μM  48 h  reduceds the percentages of colonies formed 25434381
U251 Cytotoxity Assay 20 μM  48 h  reduceds the percentages of colonies formed 25434381
U87 Growth Inhibition Assay 250/350 μM 48 h  increases the percentage of cells in S and G2/M cotreated with TMX 25554223
U118  Function Assay 250/350 μM 48 h  enhances TMX-induced p-PKC-pan decrease 25554223
U87 Function Assay 250/350 μM 48 h  enhances TMX-induced p-PKC-pan decrease 25554223
U118  Growth Inhibition Assay 50-350 μM 48 h  inhibits cell growth slightly 25554223
U87 Growth Inhibition Assay 50-350 μM 48 h  inhibits cell growth slightly 25554223
U87MG Apoptosis Assay 100 μM 48 h induces apoptosis 25680464
U251MG Apoptosis Assay 100 μM 48 h induces apoptosis 25680464
U87  Apoptosis Assay 0–200 µM 24 h enhances CQ induced apoptosis 25681668
U87  Function Assay 100 μM 24-72 h induces DcR1 expression 25808868
U251 Growth Inhibition Assay 100-400 μM 48 h inhibits cell growth in a dose-dependent manner 24623736
U87 Growth Inhibition Assay 100-400 μM 48 h inhibits cell growth in a dose-dependent manner 24623736
MDA-MB-231-br Growth Inhibition Assay 0-10 μM 48 h inhibits cell growth in a dose-dependent manner 24623736
HCC-1937 Growth Inhibition Assay 0-300 μM 48 h inhibits cell growth in a dose-dependent manner 24623736
MDA-MB-231 Growth Inhibition Assay 0-40 μM 48 h inhibits cell growth in a dose-dependent manner 24623736
MDA-MB-468 Growth Inhibition Assay 0-500 μM 48 h inhibits cell growth in a dose-dependent manner 24623736
T47D Growth Inhibition Assay 0-100 μM 48 h inhibits cell growth in a dose-dependent manner 24623736
MCF7 Growth Inhibition Assay 0-1000 μM 48 h inhibits cell growth in a dose-dependent manner 24623736
Hs683 Growth Inhibition Assay 0-1000 μM 96 h IC50=128.9 μM 24495907
U87 Growth Inhibition Assay 0-1000 μM 96 h IC50=18.45 μM 24495907
LNZ308 Growth Inhibition Assay 0-1000 μM 96 h IC50=326.7 μM 24495907
U87 Apoptosis Assay 100 μM 48 h increases the caspase-3/7 activity 24481586
U251  Apoptosis Assay 100 μM 48 h increases the caspase-3/7 activity 24481586
T98G Growth Inhibition Assay 0-750 μM 72/96 h inhibits cell viability in a dose dependent manner 24324080
U251-MG Growth Inhibition Assay 0-800 μM 72 h inhibits cell viability in a dose dependent manner 24093630
D54-MG Growth Inhibition Assay 0-800 μM 72 h inhibits cell viability in a dose dependent manner 24093630
SHG-44 Growth Inhibition Assay 10-200 μM 96 h IC50=9.73 ± 2.12 μM 24065569
U373  Growth Inhibition Assay 10-200 μM 96 h IC50=10.13 ± 1.02 μM 24065569
HT-29  Function Assay 500 μM 24/48 h enhances the levels of γ-H2AX  24038068
PC-3  Growth Inhibition Assay 0-25 μM 48 h inhibits cell growth which can be potentiated by lycopene 23746934
PC-3  Apoptosis Assay 25 μM 48 h induces apoptosis which can be potentiated by lycopene 23746934
T98G Growth Inhibition Assay 50-400 μM 144 h inhibits cell viability in a dose dependent manner 23715499
U87-MG Growth Inhibition Assay 100 µM 72 h inhibits cell growth which can be enhanced by GTB 23696788
U251-MG Growth Inhibition Assay 100 µM 72 h inhibits cell growth which can be enhanced by GTB 23696788
LNT-229 Growth Inhibition Assay 3-100 μM 24 h inhibits clonogenic survival in a dose-dependent manner 23667632
T98G Growth Inhibition Assay 10-700 μM 24 h inhibits clonogenic survival in a dose-dependent manner 23667632
U87  Function Assay 100 µM 3 h elevates the levels of pChk1 and pChk2 23667469
HCT116 Function Assay 100 µM 3 h induces the Chk1 Phosphorylation 23667469
HCT3-6 Function Assay 100 µM 3 h induces the Chk1 Phosphorylation 23667469
U-87  Growth Inhibition Assay 0-40 μM 12 d inhibits cell growth in a dose-dependent manner 23645729
U-87  Apoptosis Assay 0-40 μM 3/6 d induces apoptosis in both dose- and time-dependent manner 23645729
U-87  Function Assay 0-40 μM 3/6 d induces autophagy in both dose- and time-dependent manner 23645729
SNB75 Antiproliferative assay 10 uM 24 hrs Antiproliferative activity against human SNB75 cells at 10 uM after 24 hrs by SRB assay 22268526
C6 Antiproliferative assay 100 uM 48 hrs Antiproliferative activity against rat C6 cells at 100 uM after 48 hrs by neutral red incorporation assay 22268526
SF295 Antiproliferative assay 10 uM 24 hrs Antiproliferative activity against human SF295 cells at 10 uM after 24 hrs by SRB assay 22268526
M8 Apoptosis assay 50 to 100 uM 48 hrs Induction of apoptosis in human M8 cells assessed as apoptotic/necrotic cells at 50 to 100 uM after 48 hrs by APC-labeled annexin V and 7-AAD staining-based flow cytometric analysis 24125877
SK-MEL-30 Apoptosis assay 100 uM 48 hrs Induction of apoptosis in human SK-MEL-30 cells assessed as apoptotic/necrotic cells at 100 uM after 48 hrs by APC-labeled annexin V and 7-AAD staining-based flow cytometric analysis relative to control 24125877
SK-MEL-30 Apoptosis assay 50 uM 48 hrs Induction of apoptosis in human SK-MEL-30 cells assessed as apoptotic/necrotic cells at 50 uM after 48 hrs by APC-labeled annexin V and 7-AAD staining-based flow cytometric analysis relative to control 24125877
MNT1 Apoptosis assay 100 uM 48 hrs Induction of apoptosis in human MNT1 cells assessed as apoptotic/necrotic cells at 100 uM after 48 hrs by APC-labeled annexin V and 7-AAD staining-based flow cytometric analysis relative to control 24125877
MNT1 Apoptosis assay 50 uM 48 hrs Induction of apoptosis in human MNT1 cells assessed as apoptotic/necrotic cells at 50 uM after 48 hrs by APC-labeled annexin V and 7-AAD staining-based flow cytometric analysis relative to control 24125877
GBM 047T Antitumor assay 20 uM 1 to 2 weeks Tumoricidal effect in patient derived GBM 047T cells assessed as reduction in neurosphere formation at 20 uM after 1 to 2 weeks by 3D tumor clonogenic assay 26355532
GBM 464T Antitumor assay 20 uM 1 to 2 weeks Tumoricidal effect in patient derived GBM 464T cells assessed as reduction in neurosphere formation at 20 uM after 1 to 2 weeks by 3D tumor clonogenic assay 26355532
U373 Function assay 100 uM 72 hrs Induction of double stranded DNA break in empty vector transfected human U373 cells assessed as increase in gamma-H2AX level at 100 uM after 72 hrs by flow cytometry ChEMBL
TR-LN229 Growth Inhibition Assay 0-50 μM IC50=77 μM 25750273
LN229 Growth Inhibition Assay 0-50 μM IC50=16 μM 25750273
MRC5 Growth Inhibition Assay 7 d GI50=449.4±8 μM 25277441
DLD1 Growth Inhibition Assay 7 d GI50=501.4±93 μM 25277441
HCT116 Growth Inhibition Assay 7 d GI50=579.9±32 μM 25277441
U87MG Growth Inhibition Assay 7 d GI50=38.3±20 μM 25277441
U373VR Growth Inhibition Assay 7 d GI50=288.8±33 μM 25277441
U373M Growth Inhibition Assay 7 d GI50=368.7±86 μM 25277441
U373V Growth Inhibition Assay 7 d GI50=68.0±32 μM 25277441
SNB19VR Growth Inhibition Assay 7 d GI50=280.2±18 μM 25277441
SNB19M Growth Inhibition Assay 7 d GI50=469.9±88 μM 25277441
SNB19V Growth Inhibition Assay 7 d GI50=35.7±12 μM 25277441
U373MG-LUC Growth Inhibition Assay 72 h IC50>600 μM 25431953
M21 Growth Inhibition Assay 48 h  IC50=221 μM 25524552
M249 Growth Inhibition Assay 48 h  IC50=254 μM 25524552
M238 Growth Inhibition Assay 48 h  IC50=40 μM 25524552
A2058 Growth Inhibition Assay 48 h  IC50=12 μM 25524552
A375 Growth Inhibition Assay 48 h  IC50=265 μM 25524552
CHP-212Cis100 Growth Inhibition Assay 48 h IC50=9.55 ± 0.88 μM 25960282
CHP-212 Growth Inhibition Assay 48 h IC50=7.97 ± 0.69 μM 25960282
SK-N-ASCis24 Growth Inhibition Assay 48 h IC50=480.60 ± 101.15 μM 25960282
SK-N-AS Growth Inhibition Assay 48 h IC50=227.70 ± 22.15 μM 25960282
KellyCis83 Growth Inhibition Assay 48 h IC50=251.00 ± 15.75 μM 25960282
Kelly Growth Inhibition Assay 48 h IC50=139.20 ± 5.95 μM 25960282
U-87 MG Growth Inhibition Assay 72 h IC50=0.93 mM  25245332
U-118 MG Growth Inhibition Assay 72 h IC50=1.05 mM  25245332
U87 Growth Inhibition Assay 24 h IC50=260.34 μM  25173233
U87 GSLCs Growth Inhibition Assay 24 h IC50=766.11 μM  25173233
U87MG Growth Inhibition Assay 72 h IC50=15.625 μM  25050915
U251 Growth Inhibition Assay 24 h IC50=86.29 ± 1.58 μM 24326954
U251 Growth Inhibition Assay 48 h IC50=75.34 ± 1.02 μM 24326954
U251 Growth Inhibition Assay 72 h IC50=72.42 ± 1.45 μM 24326954
U251 Growth Inhibition Assay 96 h IC50=69.82 ± 3.04 μM 24326954
GB-SCC010 Growth Inhibition Assay 4 d IC50=226 μM 23612755
GB-SCC026 Growth Inhibition Assay 4 d IC50=53.1 μM 23612755
GB-SCC028 Growth Inhibition Assay 4 d IC50=167 μM 23612755
U87 Growth Inhibition Assay 4 d IC50=45.2 μM 23612755
U87 stem cell Growth Inhibition Assay 4 d IC50=66.7 μM 23612755
HCT116 Cytotoxicity assay 4 days IC50 = 4.34 μM 19800803
U87 Antiproliferative assay 5 days IC50 = 49 μM 22608389
U138MG Cytotoxicity assay 48 hrs IC50 = 26 μM 23069682
C6 Cytotoxicity assay 48 hrs IC50 = 34 μM 23069682
A2780 Antitumor assay 5 days IC50 = 8.5 μM 23895620
A2058 Antitumor assay 5 days IC50 = 35.5 μM 23895620
SNB19 Antitumor assay 5 days IC50 = 37 μM 23895620
A2780 Cytotoxicity assay 5 days Cytotoxicity against human A2780 cells after 5 days by MTT assay 24900418
A2780/CP70 Cytotoxicity assay 5 days Cytotoxicity against MMR-deficient human A2780/CP70 cells after 5 days by MTT assay 24900418
U87MG Function assay 3 hrs Induction of DNA alkylation in human U87MG cells assessed as increase in N7-MedG formation after 3 hrs by LC-MS/MS analysis 27614414
MDCK Cytotoxicity assay 24 hrs Cytotoxicity against MDCK cells expressing carbonic anhydrase 9 assessed as reduction in cell viability incubated for 24 hrs measured after 7 days under normoxic condition by methylene blue staining based clonogenic survival assay 27823879
MDCK Cytotoxicity assay 24 hrs Cytotoxicity against MDCK cells expressing carbonic anhydrase 9 assessed as reduction in cell viability incubated for 24 hrs measured after 7 days under hypoxic condition by methylene blue staining based clonogenic survival assay 27823879
C6 Cytotoxicity assay 4 days EC50 = 16.5 μM ChEMBL
U87 Cytotoxicity assay 72 hrs IC50 = 19.38 μM ChEMBL
SNB19 Growth inhibition assay 7 days GI50 = 35.7 μM ChEMBL
SNB19 Growth inhibition assay 7 days GI50 = 45.6 μM ChEMBL
TLX5 lymphoma Cytotoxicity assay IC50 = 5 μM 7739008
GM892 A Cytotoxicity assay IC50 = 7.6 μM 7739008
TLX5 lymphoma Cytotoxicity assay IC50 = 5 μM 12459014
U87MG Antitumor assay Antitumor activity against human U87MG cells orthotopically xenografted in Harlan nude mouse brain assessed as induction of slow tumor growth at 50 umol/kg, iv administered once daily for 5 days 27614414
U87MG Antitumor assay Antitumor activity against human U87MG cells orthotopically xenografted in Harlan nude mouse brain assessed as increase in mouse survival at 50 umol/kg, iv administered once daily for 5 days 27614414
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
Glioma Antitumor assay Antitumor activity against Homo sapiens (human) Glioma cells xenografted in transgenic mouse assessed as mouse survival ChEMBL
点击查看更多细胞系数据

生物活性

产品描述 TMZ(Temozolomide)是一种单功能的SN-1烷化剂，修饰DNA环上的氮原子以及环外氧基团。在生理pH值下，TMZ转化为活性产物MTIC、降解为methyldiazonium cation，后者再将甲基转移到DNA, 阻碍DNA复制启动，诱使细胞凋亡，是一种DNA损伤诱导剂。Temozolomide可诱导凋亡并具有抗肿瘤的活性。
特性 Methazolastone是第二代烷化剂。
靶点
DNA replication [1]
(L-1210, L-1210/BCNU cells)
体外研究(In Vitro)
体外研究活性

Methazolastone引起DNA碱不稳定位点的形成，其在L-1210和L-1210/BCNU细胞系中以相似数量存在，并且以相似比率修复。在L-1210中，methazolastone诱导细胞阻滞在SL-G2-M期，但在L-1210/BCNU中无此作用。[1]对化疗敏感与耐受的细胞(D54-R 和 U87-R)对Methazolastone的敏感性在高氧情况下被显著增强。Methazolastone和高氧均与ERK p44/42 MAPK (Erk1/2)磷酸化的增加相关，但是在D54-R细胞中增加程度较低，表明Erk1/2可能参与高氧与Methazolastone介导的细胞死亡的调节。高氧增强Methazolastone诱导细胞凋亡在GBM细胞中产生的细胞毒性，可能是通过MAPK相关的途径发挥作用。[2] Methazolastone诱导单核细胞中DNA损伤应答通路ATM-Chk2 和ATR-Chk1，导致p53活化。[3]长期Methazolastone暴露导致获得性Methazolastone耐药，并提高miR-21表达。[4] Methazolastone治疗引起内质网(ER)应激，增加GADD153和GRP78蛋白质表达，并减少caspase 12前体蛋白质。Methazolastone通过线粒体损伤和内质网应激依赖机制诱导自吞噬，以保护神经胶质瘤细胞。[5]
细胞实验 细胞系 L-1210 和 L-1210/BCNU 细胞
浓度 0 μM -100 μM
孵育时间 1小时
方法

L-1210和L-1210/ BCNU细胞以0.2×104 cells/mL接种，并培养24小时。培养基用Methazolastone在37℃下处理1小时，然后用PBS洗涤两次，离心并重新悬浮在新鲜培养基中。对照组和处理试样在48小时时以1:4在新鲜培养基中稀释，第96小时时，以1:2稀释。整个实验中使用这些稀释的细胞浓度介于3×105和8×105/mL之间。该范围内对照组呈对数生长。
实验图片 检测方法 检测指标 实验图片 PMID
Western blot DR5 / c-FLIP / Survivin / XIAP pERK / ERK / p-p38 / p38 24436439
Growth inhibition assay Cell viability 25751281
Immunofluorescence Phalloidin / Phospho-H2A.X cleaved caspase-3 27375225
体内研究(In Vivo)
体内研究活性

每天腹腔注射40 mg/kg，连续5天(肿瘤移植后1-5天)后，在L-1210 和L-1210/BCNU中，methazolastone分别增加86%和22%的寿命。在L-1210/BCNU中，100 μM 或200 μM治疗后没有作用，仅400 μM methazolastone使细胞在有丝分裂前期产生积聚，但是在L-1210中效果较弱。在L-1210/BCNU中，SL-G2-M期细胞的最大积聚在48-72小时后，大约为30%，未处理的细胞为23%。患有L- 1210白血病的小鼠静脉注射methazolastone (40 mg/kg)时，也会使细胞在SL-G2-M期积聚。而给予相同剂量药物的小鼠L-1210/BCNU细胞中，没有此作用。[1]
动物实验 Animal Models 负荷L-1210 和 L-1210/BCNU细胞的DBA/2小鼠
Dosages 40 mg/kg
Administration 静脉注射给药
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05128734 Not yet recruiting
Breast Cancer Triple Negative
AHS Cancer Control Alberta
 July 1 2024 Phase 2
NCT06161974 Not yet recruiting
High Grade Glioma|Astrocytoma|Astrocytoma Grade III|Astrocytoma Grade IV|Diffuse Intrinsic Pontine Glioma|WHO Grade III Glioma|WHO Grade IV Glioma|Metastatic Brain Tumor|Diffuse Midline Glioma H3 K27M-Mutant|Thalamus Tumor|Spinal Tumor|IDH1 Mutation|IDH1 R132|IDH1 R132C|IDH1 R132H|IDH1 R132S|IDH1 R132G|IDH1 R132L|Oligodendroglioma
Rigel Pharmaceuticals|Nationwide Children''s Hospital
 June 2024 Phase 2
NCT04967690 Not yet recruiting
Newly Diagnosed Glioblastoma
Double Bond Pharmaceutical AB
 January 2024 Phase 1
NCT05698524 Recruiting
Recurrent High Grade Glioma|Anaplastic Astrocytoma|Anaplastic Oligodendroglioma|Glioblastoma|Gliosarcoma
University of Nebraska|Xynomic Pharmaceuticals Inc.
 June 26 2023 Phase 1
NCT04945148 Not yet recruiting
Glioblastoma IDH-wildtype
Hopital Foch|National Cancer Institute France
 May 2023 Phase 2
  • https://pubmed.ncbi.nlm.nih.gov/3621181/
  • https://pubmed.ncbi.nlm.nih.gov/22763762/
  • https://pubmed.ncbi.nlm.nih.gov/22768182/
  • https://pubmed.ncbi.nlm.nih.gov/22753745/
  • https://pubmed.ncbi.nlm.nih.gov/22745676/
  • https://pubmed.ncbi.nlm.nih.gov/22627392/

化学信息&溶解度

分子量 194.15 分子式

C6H6N6O2
CAS号 85622-93-1 SDF Download TMZ(Temozolomide) SDF
Smiles CN1C(=O)N2C=NC(=C2N=N1)C(=O)N
储存条件(自收到货起) 3年 -20°C(避光) 粉状

体外溶解度
批次：

DMSO : 39 mg/mL ( (200.87 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : 7 mg/mL (36.05 mM)

Ethanol : Insoluble

摩尔浓度计算器

体内溶解配方
批次：

现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂

 动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

mg/kg g μL 只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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