卡莫司汀作用機(jī)制 - Medchemexpress - MCE中國

1、Product Data SheetCarmustineCat. No.: HY-13585CAS No.: 154-93-8分式: CHClNO分量: 214.05作靶點(diǎn): DNA Alkylator/Crosslinker作通路: Cell Cycle/DNA Damage儲存式: -20C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect from light)溶解性數(shù)據(jù)體外實驗 DMSO : 35 mg/mL (163.51 mM)* means soluble, but saturatio

2、n unknown.SolventMass1 mg 5 mg 10 mgConcentration制備儲備液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請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存式和期限：-80C, 6 months; -20C, 1 month (protect from light)。-80C 儲存時，請在 6 個內(nèi)使，-20C 儲存

3、時，請在 1 個內(nèi)使。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍浮Ｒ韵氯芙獍付颊埾劝凑?In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實驗結(jié)果的可靠性，澄 的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的式助溶1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (11.68 mM); Clear solution此案可獲得 2.5

4、 mg/mL (11.68 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (11.68 mM); Clear solution此案可獲得 2.5 mg/mL (11.68 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 2

5、5.0 mg/mL 的澄 DMSO 儲備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合Page 1 of 2 www.MedChemE均勻。3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (11.68 mM); Clear solution此案可獲得 2.5 mg/mL (11.68 mM，飽和度未知) 的澄 溶液，此案不適于實驗周 期在半個以上的實驗。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性

6、 Carmustine種抗腫瘤化療劑，為 DNA 和 RNA 的烷化劑 (alkylator)。IC & Target DNA Alkylator1體外研究 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.體內(nèi)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戶使本產(chǎn)品發(fā)表的科研獻(xiàn) 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