Inhibitors•Agonists•Screening Librarieswww.MedChemExpress.cnTemozolomideCat. No.:CAS No.:Synonyms:HY-1736485622-93-1NSC 362856; CCRG 81045; TMZC₆H₆N₆O₂194.15Autophagy; DNA Alkylator/CrosslinkerAutophagy; Cell Cycle/DNA Damage-20°C, stored under nitrogen*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)分⼦式:分⼦量:作⽤靶点:作⽤通路:储存⽅式:溶解性数据体外实验DMSO : 20.83 mg/mL (107.29 mM; Need ultrasonic)H2O : 2.86 mg/mL (14.73 mM; Need ultrasonic)Mass1 mg5.1507 mL1.0301 mL0.5151 mL5 mg25.7533 mL5.1507 mL2.5753 mL10 mg51.5066 mL10.3013 mL5.1507 mLSolventConcentration制备储备液1 mM5 mM10 mM请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存⽅式和期限。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案，配制前请先配制澄清的储备液，再依次添加助溶剂 (为保证实验结果的可靠性，体内实验的⼯作液，建议您现⽤现配，当天使⽤；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分⽐是指该溶剂在您配制终溶液中的体积占⽐)：1.请依序添加每种溶剂： 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline Solubility: ≥ 2.08 mg/mL (10.71 mM); Clear solutionSolubility: ≥ 2.08 mg/mL (10.71 mM); Clear solution2.请依序添加每种溶剂： 10% DMSO >> 90% (20% SBE-β-CD in saline)3.请依序添加每种溶剂： 10% DMSO >> 90% corn oil1/3Master of Small Molecules —您⾝边的抑制剂⼤师
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Solubility: ≥ 2.08 mg/mL (10.71 mM); Clear solutionBIOLOGICAL ACTIVITY⽣物活性IC50 & TargetTemozolomide (NSC 362856; CCRG 81045) 是可⼝服的⽤于治疗某些脑癌的DNA烷基化剂。DNA alkylator [1]Temozolomide (TZM) is a methylating agent that crosses the blood-brain barrier and is indicated for malignant gliomas and metastatic melanomas. Temozolomide is effective against tumor cells that are characterized by low levels of O6-alkylguanine DNA alkyltransferase (OGAT) and a functional mismatch repair system (MR) [1]. Determination of the IC50 for Temozolomide (TZM) in different cell lines gave values ranging from 14.1 to 234.6 μM that fell into two clearly differentiated groups: cell lines with low IC50 values (50 values (>100 μM), which include SF268 (147.2±2.1 μM) and SK-N-SH cells (234.6±2.3 μM) [2].体内研究Temozolomide (TZM), as a single agent, does not significantly increase mdian survival time (MST) with respect to control. Noteworthy, intracranial injection of NU1025, immediately before the administration of 100 or 200 mg/kg Temozolomide, significantly increases lifespans with respect to controls or to groups treated with Temozolomide only. When Temozolomide is fractionated, the increase in lifespan (ILS) obtained with this schedule is higher than that observed when NU1025 is combined with a single injection of Temozolomide (statistical comparison of survival curves: NU1025 intracranially+Temozolomide 100 mg/kg×2 vs NU1025+Temozolomide 200 mg/kg; P=0.023) [1]. 体外研究PROTOCOLCell Assay [1]The murine lymphoma cell line L5178Y of DBA/2 (H-2d/H-2d) origin is cultured in RPMI-1640 containing 10% fetal calf serum and antibiotics. Inhibition of PARP is obtained by treating cells (105 cells/mL) with 8-hydroxy-2-methylquinazolin-4[3H]-1 (NU1025), at a concentration (25 μM) that abrogates PARP activity. Cells are then exposed to Temozolomide (7.5-125 μM) and are cultured for 3 days. Cell growth is evaluated by counting viable cells in quadruplicate, and apoptosis is assessed by flow cytometry analysis of DNA content. Long-term survival is analyzed by colony-formation assay [1].MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Administration [1]Mice [1] Male B6D2F1 (C57BL/6×DBA/2) mice are anesthetized with ketamine (100 mg/kg) and xylazine (5 mg/kg) in 0.9% NaCl solution (10 mL/kg intraperitoneally). L5178Y cells (104 in 0.03 mL RPMI-1640) are then injected intracranially, through the center-middle area of the frontal bone to a 2-mm depth, using a 0.1-mL glass microsyringe and a 27-gauge disposable needle. To evaluate tumor cell growth, brains are fixed in 10% phosphate-buffered formaldehyde, and histologic sections (5 μm) are cut along the axial plane, stained with hematoxylin-eosin, and analyzed by light microscopy. Temozolomide is dissolved in DMSO (40 mg/mL), diluted in saline (5 mg/mL), and administered intraperitoneally on day 2 after tumor injection at 100 mg/kg or 200 mg/kg, doses commonly used for in vivo preclinical studies. Because cytotoxicity induced by 2/3Master of Small Molecules —您⾝边的抑制剂⼤师
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Temozolomide and PARP inhibitors can be improved by fractionated modality of treatment, in selected groups a total dose of 200 mg/kg Temozolomide is divided in 2 doses of 100 mg/kg given on days 2 and 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only. 客户使⽤本产品发表的科研⽂献• J Pineal Res. 2016 Sep;61(2):208-17.• Neuro Oncol. 2019 Jun 21. pii: noz107• Cell Physiol Biochem. 2018;48(4):1694-1702.• Cell Physiol Biochem. 2018;45(2):819-831.• J Mol Med (Berl). 2019 Jun 14. See more customer validations on www.MedChemExpress.cn REFERENCES[1]. Tentori L, et al. Combined treatment with temozolomide and poly(ADP-ribose) polymerase inhibitor enhances survival of mice bearing hematologic malignancy at the central nervous system site. Blood. 2002 Mar 15;99(6):2241-4.[2]. Perazzoli G, et al. Temozolomide Resistance in Glioblastoma Cell Lines: Implication of MGMT, MMR, P-Glycoprotein and CD133 Expression. PLoS One. 2015 Oct 8;10(10):e0140131.McePdfHeightCaution: Product has not been fully validated for medical applications.
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