依托泊苷作用機(jī)制 - Medchemexpress - MCE中國

1、Product Data SheetEtoposideCat. No.: HY-13629CAS No.: 33419-42-0分式: CHO分量: 588.56作靶點: Topoisomerase; Autophagy; Mitophagy; Bacterial; Apoptosis作通路: Cell Cycle/DNA Damage; Autophagy; Anti-infection; Apoptosis儲存式: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect from light)溶

2、解性數(shù)據(jù)體外實驗 DMSO : 39 mg/mL (66.26 mM)* means soluble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 1.6991 mL 8.4953 mL 16.9906 mL5 mM 0.3398 mL 1.6991 mL 3.3981 mL10 mM 0.1699 mL 0.8495 mL 1.6991 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 mont

3、hs; -20C, 1 month (protect from light)。-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(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

4、45% salineSolubility: 2.5 mg/mL (4.25 mM); Clear solution此案可獲得 2.5 mg/mL (4.25 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% corn oilSolubility: 2.5 mg/mL (4.25 mM); Clear solution此案可獲得 2.5

5、mg/mL (4.25 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。Page 1 of 2 www.MedChemEBIOLOGICAL ACTIVITY物活性 Etoposide (VP-16; VP-16-213) 種常的抗腫瘤化療劑。Etoposide 抑制拓?fù)洚悩?gòu)酶 II (topoisomerase-II)，從抑 制 DNA 復(fù)制。Etoposide 誘導(dǎo)細(xì)胞周 期停滯，凋亡 (apoptosis) 和噬 (autophagy)。IC & T

6、arget Topoisomerase II體外研究 Etoposide is capable of causing cytotoxicity on pancreatic -cells by inducing apoptosis through the JNK/ERK-mediated GSK-3 downstream-triggered mitochondria-dependent signaling pathway in RIN-m5F cells1.Etoposide and Bevacizumab significantly abolish P1 sphere-forming abil

7、ity, an effect associated with apoptosis of thissubset of cells2.Etoposide phosphate (0-1M; 72 hours) inhibits HCT116 FBXW+/+, FBXW-/- and p53-/- as a dose-dependent manner,exhibits IC50s of 0.945 M; 0.375 M; and 1.437 M, respectively5.Etoposide (25 M; 6 hours) delays p53 recover in FBXW7-deficient

8、cells. In addition, FBXW7 expression is disappearedin FBXW7-/- cells5.Cell Viability Assay5Cell Line: HCT116 FBXW+/+, FBXW-/- and p53-/- cellsConcentration: 0.025 M, 0.05 M, 0.075 M, 0.1 M, 0.2 M, 0.4 M, 0.6 M, 0.8 M, 1 MIncubation Time: 72 hoursResult: Inhibits HCT116 FBXW+/+p, FBXW-/- and p53-/- c

9、ell growth as a concentrationmanner.Western Blot Analysis5Cell Line: HCT116 FBXW7+/+ or FBXW7-/- cellsConcentration: 25 MIncubation Time: 6 hoursResult: Exhibited that the recovery of p53 levels after DNA damage is mediated by FBXW7.體內(nèi)研究 Etoposide (50 M) and Bevacizumab-treated hypoxic cells injecte

10、d intravenously into immunodeficient mice reveals a reduced capacity to induce lung colonies, which also appear with a longer latency period2. Etoposide (10 mg/kg/day, i.v.) with ifosfamide and carboplatin, reduces the tumor volume in the hepatoblastoma cell injected NMRI nude mice3.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Hepa

11、tology. 2019 Sep 11. Cell Syst. 2019 Jul 24;9(1):35-48.e5. Cell Syst. 2018 Apr 25;6(4):424-443.e7. Cell Rep. 2020 Jan 14;30(2):497-509.e4. Cancer Lett. 2017 Nov 1;408:43-54.Page 2 of 3 www.MedChemESee more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Lee KI, et al. Etoposi

12、de induces pancreatic -cells cytotoxicity via the JNK/ERK/GSK-3 signaling-mediated mitochondria-dependent apoptosis pathway.Toxicol In Vitro. 2016 Jul 26. pii: S0887-2333(16)30147-3.2. Calvani M, det al. Etoposide-Bevacizumab a new strategy against human melanoma cells expressing stem-like traits. O

13、ncotarget. 2016 Jun 9. doi:10.18632/oncotarget.9939.3. Fuchs, J., et al. Comparative activity of cisplatin, ifosfamide, doxorubicin, carboplatin, and etoposide in heterotransplanted hepatoblastoma. Cancer, 1998.83(11): p. 2400-7.4. Hande KR, et al. The Importance of Drug Scheduling in Cancer Chemotherapy: Etoposide as an Example. Oncologist. 1996;1(4):234-239.5. Cui D, et al. FBXW7 Confers Radiation Survival by Targeting p53 for Degradation.Cell Rep. 2020 Jan 14;30(2):497-509.e4.McePdfHeightCautio