Etoposide (Synonyms: VP-16; VP-16-213) |
Catalog No.GC15617
One-Click Copy Product Info
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Etoposide (VP-16) es un inhibidor no específico de la topoisomerasa II con un valor de IC50 de 59,2 μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 33419-42-0
Sample solution is provided at 25 µL, 10mM.
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Etoposide (VP-16) es un inhibidor no específico de la topoisomerasa II con un valor de IC50 de 59,2 μM[1]. El etopósido inhibe la síntesis de ADN al inhibir la actividad de la topoisomerasa II, y puede inducir arresto del ciclo celular, apoptosis y autofagia[2].
In vitro, el tratamiento de células HCT116 FBXW7+/+, FBXW7−/− y p53−/− con etopósido (0-1 μM) durante 72 horas inhibió el crecimiento celular de manera dependiente de la dosis, con valores de IC50 de 0,945 μM, 0,375 μM y 1,437 μM, respectivamente[3]. El tratamiento de células adherentes C33a con etopósido (5 μM) durante 48 horas indujo una apoptosis celular marginal y arresto del ciclo celular en G2/M[4].
In vivo, se inyectó etopósido (80 mg/kg) por vía intraperitoneal en ratones adultos Smc5 flox/del, Stra8-Cre cKO. Después de 8 días de exposición, se observaron defectos en los espermatocitos, con un aumento en el número de espermátidas redondas agrandadas con dos acrosomas y cromosomas adicionales[5]. El etopósido (50 mg/kg) se inyectó por vía intraperitoneal en ratones inoculados con células de cáncer de pulmón 3LL, lo que indujo al sistema inmunológico del huésped a reconocer las células 3LL y aumentó la tasa de supervivencia de los ratones al 60%[6].
References:
[1] Sudo K, Konno K, Shigeta S, et al. Inhibitory effects of podophyllotoxin derivatives on herpes simplex virus replication[J]. Antiviral Chemistry and Chemotherapy, 1998, 9(3): 263-267.
[2] Xu D, Cao J, Qian S, et al. 5k, a novel β-O-demethyl-epipodophyllotoxin analogue, inhibits the proliferation of cancer cells in vitro and in vivo via the induction of G2 arrest and apoptosis[J]. Investigational new drugs, 2011, 29: 786-799.
[3] Cui D, Xiong X, Shu J, et al. FBXW7 confers radiation survival by targeting p53 for degradation[J]. Cell reports, 2020, 30(2): 497-509. e4.
[4] Bristol M L, Wang X, Smith N W, et al. DNA damage reduces the quality, but not the quantity of human papillomavirus 16 E1 and E2 DNA replication[J]. Viruses, 2016, 8(6): 175.
[5] Hwang G, Verver D E, Handel M A, et al. Depletion of SMC5/6 sensitizes male germ cells to DNA damage[J]. Molecular biology of the cell, 2018, 29(25): 3003-3016.
[6] Slater L M, Stupecky M, Sweet P, et al. Etoposide induction of tumor immunity in Lewis lung cancer[J]. Cancer chemotherapy and pharmacology, 2001, 48: 327-332.
| Experimentos celulares [1]: | |
Líneas celulares | Células HCT116 FBXW7+/+, FBXW7−/−, p53−/− |
Método de preparación | Las células HCT116 FBXW7+/+, FBXW7−/− y p53−/− fueron sembradas en placas de 96 pocillos a una densidad de 2×10³ células por pocillo en triplicado. Las células fueron tratadas con etopósido a concentraciones de 0-1 μM durante 72 horas. |
Condiciones de reacción | 0-1 μM; 72h |
Áreas de aplicación | El etopósido inhibió el crecimiento de las células HCT116 FBXW7+/+, FBXW7−/− y p53−/− de manera dependiente de la dosis con valores de IC50 de 0,945 μM, 0,375 μM y 1,437 μM, respectivamente. |
| Experimentos con animales [2]: | |
Modelos animales | Ratones adultos Smc5 flox/del, Stra8-Cre cKO |
Método de preparación | Los ratones adultos Smc5 flox/del, Stra8-Cre cKO y los ratones control fueron inyectados intraperitonealmente con una única dosis de etopósido (80 mg/kg de peso corporal). Después de la inyección, los ratones fueron monitoreados diariamente antes de ser sacrificados a los 3, 5 o 8 días después del tratamiento. |
Forma de dosificación | 80 mg/kg; i.p. |
Áreas de aplicación | Tras 8 días de exposición al etopósido, se observó un aumento en el número de espermátidas agrandadas, a menudo con dos acrosomas, en los ratones Smc5 flox/del, Stra8-Cre cKO. |
Referencias: [1] Cui D, Xiong X, Shu J, et al. FBXW7 confers radiation survival by targeting p53 for degradation[J]. Cell reports, 2020, 30(2): 497-509. e4. [2] Hwang G, Verver D E, Handel M A, et al. Depletion of SMC5/6 sensitizes male germ cells to DNA damage[J]. Molecular biology of the cell, 2018, 29(25): 3003-3016. | |
| Cas No. | 33419-42-0 | SDF | |
| Sinónimos | VP-16; VP-16-213 | ||
| Chemical Name | (5S,5aR,8aR,9R)-5-[[(2R,4aR,6R,7R,8R,8aS)-7,8-dihydroxy-2-methyl-4,4a,6,7,8,8a-hexahydropyrano[3,2-d][1,3]dioxin-6-yl]oxy]-9-(4-hydroxy-3,5-dimethoxyphenyl)-5a,6,8a,9-tetrahydro-5H-[2]benzofuro[6,5-f][1,3]benzodioxol-8-one | ||
| Canonical SMILES | CC1OCC2C(O1)C(C(C(O2)OC3C4COC(=O)C4C(C5=CC6=C(C=C35)OCO6)C7=CC(=C(C(=C7)OC)O)OC)O)O | ||
| Formula | C29H32O13 | M.Wt | 588.56 |
| Solubility | ≥ 29.45mg/mL in DMSO | Storage | -20°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.6991 mL | 8.4953 mL | 16.9906 mL |
| 5 mM | 339.8 μL | 1.6991 mL | 3.3981 mL |
| 10 mM | 169.9 μL | 849.5 μL | 1.6991 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 15 reference(s) in Google Scholar.)