依托泊苷作用机制- Medchemexpress- MCE中国

Product Data?SheetEtoposideCat. No.:CAS No.:分?式:分?量:作?靶点:作?通路:储存?式:HY-1362933419-42-0C??H??O??588.56Topoisomerase; Autophagy; Mitophagy; Bacterial; ApoptosisCell Cycle/DNA Damage; Autophagy; Anti-infection; Apoptosis4°C, protect from light* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)Inhibitors?Agonists?Screening Libraries溶解性数据体外实验DMSO : ≥ 39 mg/mL (66.26 mM)* \Mass1 mg5 mg10 mgSolventConcentration制备储备液1 mM5 mM10 mM1.6991 mL0.3398 mL0.1699 mL8.4953 mL1.6991 mL0.8495 mL16.9906 mL3.3981 mL1.6991 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：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时，请在 6 个?内使?，-20°C 储存时，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，澄清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?是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 (4.25 mM); Clear solution此?案可获得 ≥ 2.5 mg/mL (4.25 mM，饱和度未知) 的澄清溶液。 以 1 mL ?作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加? 50 μL Tween-80，混合均匀；然后继续加? 450 μL ?理盐?定容? 1 mL。2. 请依序添加每种溶剂：?10% DMSO ?? 90% corn oilSolubility: ≥ 2.5 mg/mL (4.25 mM); Clear solution此?案可获得 ≥ 2.5 mg/mL (4.25 mM，饱和度未知) 的澄清溶液，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 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL ??油中，混合均匀。Page 1 of 2 www.MedChemExpress.cn

BIOLOGICAL ACTIVITY?物活性Etoposide (VP-16; VP-16-213) 是?种常?的抗肿瘤化疗剂。Etoposide 抑制拓扑异构酶 II (topoisomerase-II)，从?抑制 DNA 复制。Etoposide 诱导细胞周期停滞，凋亡 (apoptosis) 和?噬 (autophagy)。IC?? & Target体外研究Topoisomerase IIEtoposide is capable of causing cytotoxicity on pancreatic β-cells by inducing apoptosis through the JNK/ERK-mediated GSK-3 downstream-triggered mitochondria-dependent signaling pathway in RIN-m5F cells[1]. Etoposide and Bevacizumab significantly abolish P1 sphere-forming ability, an effect associated with apoptosis of this subset of cells[2]. Etoposide phosphate (0-1μM; 72 hours) inhibits HCT116 FBXW+/+, FBXW-/- and p53-/- as a dose-dependent manner, exhibits IC50s of 0.945 μM; 0.375 μM; and 1.437 μM, respectively[5]. Etoposide (25 μM; 6 hours) delays p53 recover in FBXW7-deficient cells. In addition, FBXW7 expression is disappeared in FBXW7-/- cells[5]. Cell Viability Assay[5]Cell Line:Concentration:Incubation Time:Result:HCT116 FBXW+/+, FBXW-/- and p53-/- cells0.025 μM, 0.05 μM, 0.075 μM, 0.1 μM, 0.2 μM, 0.4 μM, 0.6 μM, 0.8 μM, 1 μM72 hoursInhibits HCT116 FBXW+/+p>, FBXW-/- and p53-/- cell growth as a concentration manner.Western Blot Analysis[5]Cell Line:Concentration:Incubation Time:Result:HCT116 FBXW7+/+ or FBXW7-/- cells25 μM6 hoursExhibited that the recovery of p53 levels after DNA damage is mediated by FBXW7.体内研究Etoposide (50 μM) and Bevacizumab-treated hypoxic cells injected intravenously into immunodeficient mice reveals a reduced capacity to induce lung colonies, which also appear with a longer latency period[2]. Etoposide (10 mg/kg/day, i.v.) with ifosfamide and carboplatin, reduces the tumor volume in the hepatoblastoma cell injected NMRI nude mice[3].客户使?本产品发表的科研?献????Hepatology.?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.MedChemExpress.cn

See more customer validations on www.MedChemExpress.cnREFERENCES

[1].?Lee KI, et al. Etoposide induces pancreatic β-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. Oncotarget. 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.

McePdfHeightCaution: Product has not been fully validated for medical applications. For research use only.

Tel: 400-820-3792; 021-58955995 Fax: 021-53700325 E-mail: tech@MedChemExpress.cn

Master of Small Molecules — 您?边的抑制剂?师

Page 3 of 3 www.MedChemExpress.cn