Etoposide (Synonyms: VP-16; VP-16-213) |
Catalog No.GC15617
One-Click Copy Product Info
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Etoposide (VP-16)는 토포이소머효소II를 비록이적으로 억제제로 IC50 값이 59.2μM이다.
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)는 토포이소머효소II를 비록이적으로 억제제로 IC50 값이 59.2μM이다.Etoposide는 토포이소머효소II활동을 억제하고DNA 합성을 억제하고 세포주기 중단,세포 사멸 그리고 자포시를 유도할 수 있다.
체외 실험에서 HCT116 FBXW7+/+, FBXW7−/− 및p53−/− 세포에 Etoposide (0-1μM)을 72시간 처리하여 세포 성장을 용량 의존적으로 억제했고 각각의 IC50 값이 0.945μM, 0.375μM및 1.437μM이었다. Etoposide (5μM)을 48시간 동안 부착된 C33a 세포에 처리하고 변두리 세포 사멸과 세포주기 G2/M 중지를 유도했다[4].
체내 실험에서 Etoposide (80mg/kg)가 성체 Smc5 flox/del, Stra8-Cre cKO쥐에게 복강 주사되었다.노출 8일 후 쥐에서 정자 결함이 관찰되었고 두개의 아크로좀과 추가로 있는 염색체를 가진 켜진 둥근 정자의 수가 증가했다[5]. Etoposide (50mg/kg)가 3LL 폐암 세포를 이식 받은 쥐에게 복강 주사되었고 호스트 면역 체계를 유도하고 3LL 세포를 인식하고 쥐의 생존률을 60%로 증가시켰다[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.
| 세포 실험 [1]: | |
세포 라인 | HCT116 FBXW7+/+, FBXW7−/−, p53−/− 세포 |
제조 방법 | HCT116 FBXW7+/+, FBXW7−/−, p53−/− 세포는 96웰 판에 2×103 세포/웰의 밀도로 세척하여 3회복으로 심었습니다. 세포는 0-1μM의 Etoposide로 72시간 동안 처리되었습니다. |
반응 조건 | 0-1μM; 72시간 동안 |
응용 분야 | Etoposide는 HCT116 FBXW+/+, FBXW-/-및 p53-/- 세포를 농도 의존적인 방식으로 억제하고 그 IC50 값은 각각 0.945 μM, 0.375 μM, 1.437 μM입니다. |
| 동물 실험 [2]: | |
동물 모형 | 성체 Smc5 flox/del, Stra8-Cre cKO 쥐 |
제조 방법 | 성체 Smc5 flox/del, Stra8-Cre cKO 및대조 쥐는 Etoposide 단일 투여로 복강 내 주입을 받았습니다 (80mg/kg 체중). 주입 후 쥐는 치료 후 3, 5 또는 8일에 사멸되기 전 매일 관찰했습니다. |
제형 | 80mg/kg; i.p. |
응용 분야 | Etoposide 노출 8일 후 Smc5 flox/del, Stra8-Cre cKO에서 두 개의 아크로졸을 가진 팽창된 정자의 수가 증가하는 것을 관찰했습니다. |
References: | |
| Cas No. | 33419-42-0 | SDF | |
| Synonyms | 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 | |||
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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 |
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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.
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 15 reference(s) in Google Scholar.)