苯丁酸氮芥作用機制 - Medchemexpress - MCE中國

1、Product Data SheetChlorambucilCat. No.: HY-13593CAS No.: 305-03-3分式: CHClNO分量: 304.21作靶點: DNA Alkylator/Crosslinker作通路: Cell Cycle/DNA Damage儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 24 mg/mL (78.89 mM)* means soluble, but saturation unknown.SolventMass1

2、mg 5 mg 10 mgConcentration制備儲備液1 mM 3.2872 mL 16.4360 mL 32.8720 mL5 mM 0.6574 mL 3.2872 mL 6.5744 mL10 mM 0.3287 mL 1.6436 mL 3.2872 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。-80C 儲存時，請在 6 個內(nèi)使，-20C 儲存時，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?shù)娜芙獍浮Ｒ韵氯芙獍付颊?/p>

3、先按照 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，適當保存；體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當天使； 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 (8.22 mM); Clear solution此案可獲得 2.5 mg/mL (8.22 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 10

4、0 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 (8.22 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 2.5 mg/mL (8.22 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

5、900 L 20% 的 SBE-CD 理鹽溶液中，混合均勻。3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (8.22 mM); Clear solution此案可獲得 2.5 mg/mL (8.22 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 Chlorambucil種烷化劑 (alkylator)，具有抗腫瘤活性。IC & Target

6、DNA Alkylator1體外研究 Chlorambucil can deprive the function of complementary strands of DNA molecules via alkalization-induced crossinteraction, and then inhibits tumor cell proliferation. Chlorambucil (0, 2.5, 5, 10 M) exhibits slight inhibitory effect onRaji cell apoptosis, but potently increases DR4

7、 and DR5 mRNA expression in Raji cells. Chlorambucil (10 M) incombination with Tumor necrosis factor (TNF) related apoptosis inducing ligand (TRAIL, 80 ng/ml) has synergisticeffect on Raji cell apoptosis and inhibition on proliferation1.體內(nèi)研究 Chlorambucil (0.2 mg/kg, p.o.) in combination with levamis

8、ole (5 mg/kg) has enhanced anti-cancer effect on Ehrlich ascites carcinoma which elevates apoptosis of Ehrlich ascites carcinoma and the survival rate of the mice. However, Chlorambucil exhibits adverse effects on the liver and kidneys of mice2.PROTOCOLCell Assay 1 Cultured cells at log-growth phase

9、 are digested by trypsin into single cell suspension and are seeded into 96-wellplate at 1000 per well density. The plate is placed in a 37C chamber with 5% CO2. After attached growth for 24 h,cells are treated with TRAIL at 0, 20, 40 and 80 ng/mL or Chlorambucil at 0, 2.5, 5 and 10 M for 48 h. 10 L

10、 CCK-8reagent is added to each well, followed by incubation at 37C for 4 h. Absorbance values at 450 nm are thenmeasured by a micro-plate reader. Six parallel samples are performed in each treatment group. Cell proliferation rate(%) = mean value of experimental group/mean value of control group 100%

11、1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice2Administration 2 Female Swiss mice are divided randomly into five group (20 mice per group). Group 1 is kept as the control group, Group 2 receives intraperitoneal injection of by 2.5 106 Ehr

12、lich ascites carcinoma cell, Gropu 3 is treated orallywith Chlorambucil 0.2 mg/kg body weight, Group 4 is treated orally with levamisole (5 mg/kg body weight) andGroup 5 is treated orally with a combination of Chlorambucil and levamisole each day, using a bent stainless steelstomach tube2.MCE has no

13、t independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻Page 2 of 3 www.MedChemE J Autoimmun. 2020 Apr 21:102465. J Mol Med (Berl). 2019 Aug;97(8):1183-1193.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Guo JX, et al. Synergi

14、stic effects of chlorambucil and TRAIL on apoptosis and proliferation of Raji cells. Eur Rev Med Pharmacol Sci. 2017Oct;21(20):4703-4710.2. Salem FS, et al. Biochemical and pathological studies on the effects of levamisole and chlorambucil on Ehrlich ascites carcinoma-bearing mice. Vet Ital.2011 Jan-Mar;47(1):89-95.McePdfHeigh