卡莫司汀作用机制- Medchemexpress- MCE中国 - 图文

Product Data?SheetCarmustineCat. No.:CAS No.:分?式:分?量:作?靶点:作?通路:储存?式:HY-13585154-93-8C?H?Cl?N?O?214.05DNA Alkylator/CrosslinkerCell Cycle/DNA Damage-20°C, protect from light* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)Inhibitors?Agonists?Screening Libraries溶解性数据体外实验DMSO : ≥ 35 mg/mL (163.51 mM)* \Mass1 mg5 mg10 mgSolventConcentration制备储备液1 mM5 mM10 mM4.6718 mL0.9344 mL0.4672 mL23.3590 mL4.6718 mL2.3359 mL46.7181 mL9.3436 mL4.6718 mL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；?旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存?式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时，请在 6 个?内使?，-20°C 储存时，请在 1 个?内使?。体内实验请根据您的实验动物和给药?式选择适当的溶解?案。以下溶解?案都请先按照 In Vitro ?式配制澄清的储备液，再依次添加助溶剂： 为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的?作液，建议您现?现配，当天使?； 以下溶剂前显?的百分?是指该溶剂在您配制终溶液中的体积占?；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的?式助溶1. 请依序添加每种溶剂：?10% DMSO ?? 40% PEG300 ?? 5% Tween-80 ?? 45% salineSolubility: ≥ 2.5 mg/mL (11.68 mM); Clear solution此?案可获得 ≥ 2.5 mg/mL (11.68 mM，饱和度未知) 的澄清溶液。 以 1 mL ?作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加? 50 μL Tween-80，混合均匀；然后继续加? 450 μL ?理盐?定容? 1 mL。2. 请依序添加每种溶剂：?10% DMSO ?? 90% (20% SBE-β-CD in saline)Solubility: ≥ 2.5 mg/mL (11.68 mM); Clear solution此?案可获得 ≥ 2.5 mg/mL (11.68 mM，饱和度未知) 的澄清溶液。 以 1 mL ?作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD ?理盐??溶液中，混合Page 1 of 2 www.MedChemExpress.cn

均匀。3. 请依序添加每种溶剂：?10% DMSO ?? 90% corn oilSolubility: ≥ 2.5 mg/mL (11.68 mM); Clear solution此?案可获得 ≥ 2.5 mg/mL (11.68 mM，饱和度未知) 的澄清溶液，此?案不适?于实验周期在半个?以上的实验。 以 1 mL ?作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL ??油中，混合均匀。BIOLOGICAL ACTIVITY?物活性IC?? & Target体外研究Carmustine 是?种抗肿瘤化疗剂，为 DNA 和 RNA 的烷化剂 (alkylator)。DNA Alkylator[1]Carmustine is an antitumor chemotherapeutic agent. Carmustine (8, 80, and 800 μM) decreases N-acetyltransferase (NAT) activities for 2-aminofluorene (AF) and p-aminobenzoic acid (PABA) in rat glial tumor cytosol and intact cells. In rat glial tumor cells, the DNA-AF adduct increases, and carmustine decreases the formation of DNA-AF adduct[1].体内研究Carmustine (BCNU; 25 mg/kg, i.p.) causes higher levels of the rhe ratio of liver weight to body weight and plasma conjugated bilirubin, and lower biliary flow, oxidised glutation levels (GSSG) and reduced glutation (GSH)/GSSG values compared with control rats[2].PROTOCOLKinase Assay [1]The determination of Acetyl-CoAdependent N-acetylation of 2-aminofluorene (AF) and p-aminobenzoic acid (PABA) are performed. Incubation mixtures in the assay system consists of a total volume of 90 μL: glial tumor cells cytosols, diluted as required, in 50 μL of lysis buffer (20 mM Tris/HCl, pH 7.5, 1 mM DTT and 1 mM EDTA), 20 μL of an Acetyl-CoA recycling mixture of 50 mM Tris-HCl (pH7.5), 0.2 mM EDTA, 2 mM DTT, 15 mM acetylcamitine, 2U/mL carnitine acetyltransferase, and AF or PABA at specific concentrations. The reactions are started by addition of 20 μL of Acetyl-CoA. The control reactions have 20 μL distilled water in place of Acetyl-CoA. For the single point activity measurements, the final concentration of AF or PABA is 0.1 mM and AcCoA is 0.5 mM. The reaction mixtures with or without specific concentrations of Carmustine and lomustine are incubated at 37°C for 10 min and stopped with 50 μL of 20% trichloroacetic acid for the PABA reactions, and 100 μL of acetonitrile for the AF reactions. All of the reactions (experiments and controls) are run in triplicate[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Administration [2]Rats[2] Individual rats are weighted prior to enter the study; their weights are recorded, and they are randomLy assigned to four groups. Group I (saline group); This group consists of 12 rats. These rats are injected with 2 mL/kg of saline intraperitoneally (IP) 48 h before the study, being included by the study 48 h later. Group II (corn oil group) consists of 15 rats. These rats are injected with 2 mL/kg of corn oil (vehicle) IP 48 h before the study. Group III (Carmustine group) consists of 16 rats. These rats are injected with 1 mL per day of saline IP, administered at the same hour of the day as a single-dose for 3 days. Twelve hours after the first dose of saline, corn oil 2 mL/kg + Carmustine 25 mg/kg IP are injected, and the rats are included in the study 48 h after the administration of corn oil + Carmustine. Group IV (trimetazidine group) consists of 12 rats. These rats are injected with 2.5 mg/kg per day of trimetazidine (TMZ) IP, administered at the same hour of the day as a single-dose for 3 days. 12 h after the first dose of TMZ, corn oil 2 mL/kg + Carmustine 25 mg/kg IP are injected, and the rats are included in the study 48 h after the administration of corn oil + Carmustine[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.Page 2 of 3

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????Ann Rheum Dis. 2020 May 14;annrheumdis-2019-216911.????J Mol Med (Berl). 2019 Aug;97(8):1183-1193.????Acta Pharmacol Sin. 2020 May 12.????Mol Imaging Biol.?2019 Apr 15.

See more customer validations on www.MedChemExpress.cnREFERENCES

[1].?Hung CF. Effects of carmustine and lomustine on arylamine N-acetyltransferase activity and 2-aminofluorene-DNA adducts in rat glial tumor cells. Neurochem Res. 2000 Jun;25(6):845-51.

[2].?Demir A, et al. The effect of trimetazidine on intrahepatic cholestasis caused by carmustine in rats. Hepatol Res. 2001 May 1;20(1):133-143.

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