環(huán)磷酰胺水合物作用機制 - Medchemexpress - MCE中國

1、Product Data SheetCyclophosphamide hydrateCat. No.: HY-17420ACAS No.: 6055-19-2分式: CHClNOP分量: 279.1作靶點: DNA Alkylator/Crosslinker作通路: Cell Cycle/DNA Damage儲存式: Powder -20C 3 years4C 2 years* 該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)現(xiàn)配，即刻使。溶解性數(shù)據(jù)體外實驗 H2O : 50 mg/mL (179.15 mM)DMSO : 38 mg/mL (136.15 mM)* means soluble, but sa

2、turation unknown.SolventMass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 3.5829 mL 17.9147 mL 35.8295 mL5 mM 0.7166 mL 3.5829 mL 7.1659 mL10 mM 0.3583 mL 1.7915 mL 3.5829 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；該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)現(xiàn)配，即刻使.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?。以下溶解案都請先按?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

3、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 (8.96 mM); Clear solution此案可獲得 2.5 mg/mL (8.96 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；

4、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 (8.96 mM); Clear solution此案可獲得 2.5 mg/mL (8.96 mM，飽和度未知) 的澄清溶液。Page 1 of 2 www.MedChemE以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄均勻。DMSO 儲備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合3. 請依序添加每種溶劑： 10% DM

5、SO 90% corn oilSolubility: 2.5 mg/mL (8.96 mM); Clear solution此案可獲得 2.5 mg/mL (8.96 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 Cyclophosphamide hydrate種合成的 DNA Alkylator，在化學(xué)上與氮芥類有關(guān)，具有抗腫瘤及免疫抑制活性。體外研究 Cyclophosphamide induces ou

6、ter membrane blebbing, leads to DNA fragmentation, as revealed by TUNEL staining offree 3-OH DNA ends, and induces cleavage of the caspase 3 and caspase 7 substrate PARP in 9L/P450 cells. Bcl-2expression fully blocks the activation of both initiator caspases as well as the effector caspase 3 in cell

7、s treated withactivated Cyclophosphamide. Bcl-2 inhibits the cytotoxic effects but not the cytostatic effects of activatedCyclophosphamide1. Cyclophosphamide inhibits the AChE reversibly with an IC50 of 511 M2. Carbon tetrachloridedoes not affect the direct cytotoxicity of cyclophosphamide or 4-hydr

8、oxycyclophosphamide to cells in culture3.體內(nèi)研究 Cyclophosphamide (injected i.p.;2mg/mouse in 0.1 mL PBS, in C3H mice bearing SW1 tumors) increases thepercentage of cells that stained for CD3, CD4 or CD8 in both spleens and tumors4.Animal Model: Six to eight-week old female C3H/HeN mice bearing SW1 tum

9、ors4Dosage: 2 mg/mouseAdministration: Injected i.p.; 2mg/mouse in 0.1 mL PBS; Four daysResult: Increased the percentage of cells that stained for CD3, CD4 or CD8 in both spleensand tumors.戶使本產(chǎn)品發(fā)表的科研獻 J Mol Med (Berl). 2019 Aug;97(8):1183-1193. Life Sci. 2020 Mar.See more customer validations on HYPE

10、RLINK www.MedChemE www.MedChemEREFERENCES1. Schwartz PS, et al. Cyclophosphamide induces caspase 9-dependent apoptosis in 9L tumor cells. Mol Pharmacol. 2001 Dec;60(6):1268-1279.2. al-Jafari AA, et al. Inhibition of human acetylcholinesterase by cyclophosphamide. Toxicology. 1995 Jan 19;96(1):1-6.3.

11、 Harris RN, et al. Carbon tetrachloride-induced increase in the antitumor activity of cyclophosphamide in mice: a pharmacokineticstudy. CancerChemother Pharmacol. 1984;12(3):167-72.4. Liu P, et al. Administration of cyclophosphamide changes the immune profile of tumor-bearing mice. J Immunother. 2010 Jan;33(1):53-9.Page 2 of 3 www.MedChemEMcePdfHeightCaution: Product has not been fully validat