卡莫司汀作用机制 - Medchemexpress - MCE中国

1、Product Data SheetCarmustineCat. No.: HY-13585CAS No.: 154-93-8分式: CHClNO分量: 214.05作靶点: DNA Alkylator/Crosslinker作通路: Cell Cycle/DNA Damage储存式: -20C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect from light)溶解性数据体外实验 DMSO : 35 mg/mL (163.51 mM)* means soluble, but saturatio

2、n unknown.SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 4.6718 mL 23.3590 mL 46.7181 mL5 mM 0.9344 mL 4.6718 mL 9.3436 mL10 mM 0.4672 mL 2.3359 mL 4.6718 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：-80C, 6 months; -20C, 1 month (protect from light)。-80C 储存时，请在 6 个内使，-20C 储存

3、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 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 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

4、 mg/mL (11.68 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-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 L 2

5、5.0 mg/mL 的澄 DMSO 储备液加到 900 L 20% 的 SBE-CD 理盐溶液中，混合Page 1 of 2 www.MedChemE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 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 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。BIOLOGICAL ACTIVITY物活性

6、 Carmustine种抗肿瘤化疗剂，为 DNA 和 RNA 的烷化剂 (alkylator)。IC & Target DNA Alkylator1体外研究 Carmustine is an antitumor chemotherapeutic agent. Carmustine (8, 80, and 800 M) decreases N-acetyltransferase(NAT) activities for 2-aminofluorene (AF) and p-aminobenzoic acid (PABA) in rat glial tumor cytosol and intact

7、cells. Inrat glial tumor cells, the DNA-AF adduct increases, and carmustine decreases the formation of DNA-AF adduct1.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 plasmaconjugated bilirubin, and lower biliary flow, oxidised glutation

8、 levels (GSSG) and reduced glutation (GSH)/GSSG values compared with control rats2.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

9、90 L: glial tumor cellscytosols, diluted as required, in 50 L of lysis buffer (20 mM Tris/HCl, pH 7.5, 1 mM DTT and 1 mM EDTA), 20 L of anAcetyl-CoA recycling mixture of 50 mM Tris-HCl (pH7.5), 0.2 mM EDTA, 2 mM DTT, 15 mM acetylcamitine, 2U/mLcarnitine acetyltransferase, and AF or PABA at specific

10、concentrations. The reactions are started by addition of 20 Lof Acetyl-CoA. The control reactions have 20 L distilled water in place of Acetyl-CoA. For the single point activitymeasurements, the final concentration of AF or PABA is 0.1 mM and AcCoA is 0.5 mM. The reaction mixtures with orwithout spe

11、cific concentrations of Carmustine and lomustine are incubated at 37C for 10 min and stopped with 50 L of 20% trichloroacetic acid for the PABA reactions, and 100 L of acetonitrile for the AF reactions. All of thereactions (experiments and controls) are run in triplicate1.MCE has not independently c

12、onfirmed the accuracy of these methods. They are for reference only.Animal Rats2Administration 2 Individual rats are weighted prior to enter the study; their weights are recorded, and they are randomLy assigned tofour groups. Group I (saline group); This group consists of 12 rats. These rats are inj

13、ected with 2 mL/kg of salineintraperitoneally (IP) 48 h before the study, being included by the study 48 h later. Group II (corn oil group) consistsof 15 rats. These rats are injected with 2 mL/kg of corn oil (vehicle) IP 48 h before the study. Group III (Carmustinegroup) consists of 16 rats. These

14、rats are injected with 1 mL per day of saline IP, administered at the same hour of theday as a single-dose for 3 days. Twelve hours after the first dose of saline, corn oil 2 mL/kg + Carmustine 25 mg/kgIP are injected, and the rats are included in the study 48 h after the administration of corn oil

15、+ 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 2mL/kg + Carmustine 25 mg/kg IP are injected, and

16、 the rats are included in the study 48 h after the administration ofcorn oil + Carmustine2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Page 2 of 3 www.MedChemE户使本产品发表的科研献 Ann Rheum Dis. 2020 May 14;annrheumdis-2019-216911. J Mol Med (Berl). 2019 Aug

17、;97(8):1183-1193. Acta Pharmacol Sin. 2020 May 12. Mol Imaging Biol. 2019 Apr 15.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. 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 ra