TMZ(Temozolomide)
别名: NSC 362856,CCRG 81045,Methazolastone 中文名称：替莫唑胺
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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
CAS: 85622-93-1
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纯度：
99.99%
99.99
TMZ(Temozolomide)相关产品
相关信号通路图
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 |
|---|---|---|---|---|---|
| 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 |
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| 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] |
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|---|---|---|---|---|
| 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。 |
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| 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] |
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|---|---|---|
| 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 |
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 | ||
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体外溶解度 |
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 |
|
体内溶解度 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
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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