Etoposide-VP-16-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEEtoposideCat. No.: HY-13629CAS No.: 33419-42-0Synonyms: VP-16; VP-16-213分式: CHO分量: 588.56作靶點(diǎn): Topoisomerase; Autophagy; Mitophagy; Apoptosis作通路: Cell Cycle/DNA Damage; Autophagy; Apoptosis儲(chǔ)存式: 4C, protect from light* In solvent

2、: -80C, 6 months; -20C, 1 month (protect fromlight)溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 39 mg/mL (66.26 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)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(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑

3、配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn) 請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (4.25 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2

4、.5 mg/mL (4.25 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 Etoposide (VP-16; VP-16-213)于治療多種癌癥的化療藥物，通過(guò)與拓?fù)洚悩?gòu)酶 II 和 DNA 形成復(fù)合物來(lái)抑制DNA合成。Etoposide 阻斷細(xì)胞周 期 G2 期并誘導(dǎo)細(xì)胞凋亡。IC50 & Target Topoisomerase II體外研究 Etoposide is capable of causing cytotoxicity on pancreat

5、ic -cells by inducing apoptosis through theJNK/ERK-mediated GSK-3 downstream-triggered mitochondria-dependent signaling pathway in RIN-m5Fcells 1. Etoposide and Bevacizumab significantly abolish P1 sphere-forming ability, an effect associatedwith apoptosis of this subset of cells 2.體內(nèi)研究 Etoposide (5

6、0 M) and Bevacizumab-treated hypoxic cells injected intravenously into immunodeficient micereveals 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 thehepatoblastom

7、a cell injected NMRI nude mice 3.PROTOCOLKinase Assay 1 RIN-m5F cells are seeded and treated with Etoposide (10-50 M) in the absence or presence of Z-DEVD-FMK (20 M). At the end of treatments (for 24 h), the cell lysates are incubated at 37C with 10 M Ac-DEVD-AMC, a caspase-3/CPP32 substrate, for 1

8、h. The fluorescence of the cleaved substrate is measuredby a spectrofluorometer with an excitation wavelength at 380 nm and an emission wavelength at 460 nm.Protein levels of cell lysate samples are determined using the bicinchoninic acid protein assay kit with anabsorption band of 570 nm to normali

9、ze the cell numbers between control and etoposide-treated groups.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Cell Assay 1 RIN-m5F cell is a rat pancreatic -cell line, and cultured in a humidified chamber with a 5% CO2-95% airmixture at 37C and maint

10、ained in RPIM 1640 medium supplemented with 10% fetal bovine serum (FBS)and antibiotics (100 U/mL of penicillin and 100 g/mL of streptomycin). RIN-m5F cells are seeded (2 104cells/well) in 96-well plates and allowed to adhere and recover overnight. The cells are changed to freshmedia and then incuba

11、ted with Etoposide (1-100 M) in the absence or presence of the pharmacologicalinhibitors (lithium chloride (LiCl)-50 M; SP600125-20 M; PD98059-20 M) for 24 h.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal The in vivo model for nude mice HB (NMHB

12、) has been established. Only HB cells with embryonalAdministration 3 components are grafted and reproduced successfully in this model. Each NMHB subsequently istransplanted into 50 mice for treatment groups. Treatment is initiated when the majority of the tumors reach avolume of 50-100 mm3. The mice

13、 are stratified according to their tumor volume and randomLy assigned togroups of ten animals each. The animals injected with tumor are given ifosfamide, cisplatin, doxorubicin,etoposide (10 mg/kg/day, i.v.), and carboplatin as single agents in two blocks. One group of ten animals foreach original x

14、enograft served as a control group. After initiation of treatment, the tumor growth is recorded at5-day intervals for 25-30 days and the relative tumor volumes are calculated. Twenty-four hours before theanimals are sacrificed, bromodeoxyuridine (BrdU) is injected intraperitoneally for the semiquant

15、itative2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEdetermination of proliferation activity of the tumor cells (50 g of BrdU/g body weight).MCE has not 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(xiàn) Cell Syst. 2019 Jul 5. pii: S2405-4712(19)30200-5

16、. Cell Syst. 2018 Apr 25;6(4):424-443.e7. Cancer Lett. 2017 Nov 1;408:43-54. J Mol Med (Berl). 2019 Jun 14. J Cell Physiol. 2019 Mar;234(3):2683-2692.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Lee KI, et al. Etoposide induces pancreatic -cells cytotoxicity via the JNK/ERK/

17、GSK-3 signaling-mediated mitochondria-dependentapoptosis 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. 2016Jun 9. doi: 10.18632/oncotarget.9939.3. Fuchs, J., et al. Comparative activity of cisplatin, ifosfamide, doxorubicin, carboplatin, and etoposide in heterotransplantedhepatoblastoma. Cancer, 1998. 83(11): p. 2400-7.4. Hande KR, et al. The Importance of Drug Scheduling in Cancer C