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別名: NSC 362856,CCRG 81045,Methazolastone 中文名稱:替莫唑胺
此產品請避光密封保存。
TMZ(Temozolomide)是一種單功能的SN-1烷化劑,修飾DNA環(huán)上的氮原子以及環(huán)外氧基團。在生理pH值下,TMZ轉化為活性產物MTIC、降解為methyldiazonium cation,后者再將甲基轉移到DNA, 阻礙DNA復制啟動,誘使細胞凋亡,是一種DNA損傷誘導劑。Temozolomide可誘導凋亡并具有抗腫瘤的活性。
TMZ(Temozolomide) Chemical Structure
CAS: 85622-93-1
細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
---|---|---|---|---|---|
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 | ||
點擊查看更多細胞系數據 |
產品描述 | TMZ(Temozolomide)是一種單功能的SN-1烷化劑,修飾DNA環(huán)上的氮原子以及環(huán)外氧基團。在生理pH值下,TMZ轉化為活性產物MTIC、降解為methyldiazonium cation,后者再將甲基轉移到DNA, 阻礙DNA復制啟動,誘使細胞凋亡,是一種DNA損傷誘導劑。Temozolomide可誘導凋亡并具有抗腫瘤的活性。 | |
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特性 | Methazolastone是第二代烷化劑。 | |
靶點 |
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體外研究(In Vitro) | ||||
體外研究活性 | Methazolastone引起DNA堿不穩(wěn)定位點的形成,其在L-1210和L-1210/BCNU細胞系中以相似數量存在,并且以相似比率修復。在L-1210中,methazolastone誘導細胞阻滯在SL-G2-M期,但在L-1210/BCNU中無此作用。[1]對化療敏感與耐受的細胞(D54-R 和 U87-R)對Methazolastone的敏感性在高氧情況下被顯著增強。Methazolastone和高氧均與ERK p44/42 MAPK (Erk1/2)磷酸化的增加相關,但是在D54-R細胞中增加程度較低,表明Erk1/2可能參與高氧與Methazolastone介導的細胞死亡的調節(jié)。高氧增強Methazolastone誘導細胞凋亡在GBM細胞中產生的細胞毒性,可能是通過MAPK相關的途徑發(fā)揮作用。[2] Methazolastone誘導單核細胞中DNA損傷應答通路ATM-Chk2 和ATR-Chk1,導致p53活化。[3]長期Methazolastone暴露導致獲得性Methazolastone耐藥,并提高miR-21表達。[4] Methazolastone治療引起內質網(ER)應激,增加GADD153和GRP78蛋白質表達,并減少caspase 12前體蛋白質。Methazolastone通過線粒體損傷和內質網應激依賴機制誘導自吞噬,以保護神經膠質瘤細胞。[5] |
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細胞實驗 | 細胞系 | L-1210 和 L-1210/BCNU 細胞 | ||
濃度 | 0 μM -100 μM | |||
孵育時間 | 1小時 | |||
方法 | L-1210和L-1210/ BCNU細胞以0.2×104 cells/mL接種,并培養(yǎng)24小時。培養(yǎng)基用Methazolastone在37℃下處理1小時,然后用PBS洗滌兩次,離心并重新懸浮在新鮮培養(yǎng)基中。對照組和處理試樣在48小時時以1:4在新鮮培養(yǎng)基中稀釋,第96小時時,以1:2稀釋。整個實驗中使用這些稀釋的細胞濃度介于3×105和8×105/mL之間。該范圍內對照組呈對數生長。 |
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實驗圖片 | 檢測方法 | 檢測指標 | 實驗圖片 | 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 |
體內研究(In Vivo) | ||
體內研究活性 | 每天腹腔注射40 mg/kg,連續(xù)5天(腫瘤移植后1-5天)后,在L-1210 和L-1210/BCNU中,methazolastone分別增加86%和22%的壽命。在L-1210/BCNU中,100 μM 或200 μM治療后沒有作用,僅400 μM methazolastone使細胞在有絲分裂前期產生積聚,但是在L-1210中效果較弱。在L-1210/BCNU中,SL-G2-M期細胞的最大積聚在48-72小時后,大約為30%,未處理的細胞為23%。患有L- 1210白血病的小鼠靜脈注射methazolastone (40 mg/kg)時,也會使細胞在SL-G2-M期積聚。而給予相同劑量藥物的小鼠L-1210/BCNU細胞中,沒有此作用。[1] |
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動物實驗 | Animal Models | 負荷L-1210 和 L-1210/BCNU細胞的DBA/2小鼠 |
Dosages | 40 mg/kg | |
Administration | 靜脈注射給藥 |
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 |
分子量 | 194.15 | 分子式 | C6H6N6O2 |
CAS號 | 85622-93-1 | SDF | Download TMZ(Temozolomide) SDF |
Smiles | CN1C(=O)N2C=NC(=C2N=N1)C(=O)N | ||
儲存條件(自收到貨起) | 3年 -20°C(避光) 粉狀 | ||
體外溶解度 |
DMSO : 39 mg/mL ( (200.87 mM) ;DMSO吸濕會降低化合物溶解度,請使用新開封DMSO) Water : 7 mg/mL (36.05 mM) Ethanol : Insoluble |
摩爾濃度計算器 |
體內溶解度 現(xiàn)配現(xiàn)用,請按從左到右的順序依次添加,澄清后再加入下一溶劑 |
動物體內配方計算器 |
動物體內配方計算器(澄清溶液)
第一步:請輸入基本實驗信息(考慮到實驗過程中的損耗,建議多配一只動物的藥量)
第二步:請輸入動物體內配方組成(配方適用于不溶于水的藥物;不同批次藥物配方比例不同,請聯(lián)系Selleck為您提供正確的澄清溶液配方)
計算結果:
工作液濃度: mg/ml;
DMSO母液配制方法: mg 藥物溶于μL DMSO溶液(母液濃度mg/mL,注:如該濃度超過該批次藥物DMSO溶解度,請先聯(lián)系Selleck);
體內配方配制方法:取μL DMSO母液,加入μL PEG300,混勻澄清后加入μL Tween 80,混勻澄清后加入μL ddH2O,混勻澄清。
體內配方配制方法:取μL DMSO母液,加入μL Corn oil,混勻澄清。
注意:1. 首先保證母液是澄清的;
2.一定要按照順序依次將溶劑加入,進行下一步操作之前必須保證上一步操作得到的是澄清的溶液,可采用渦旋、超聲或水浴加熱等物理方法助溶。
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