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Arenobufagin
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Arenobufagin图片
CAS NO:464-74-4
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议

产品介绍
沙蟾蜍精(Arenobufagin)是由蟾蜍毒液提取的蟾蜍甾烯,具有抗癌活性。
Cas No.464-74-4
别名沙蟾毒精
Canonical SMILESC[C@]([C@@H](C(C=C1)=COC1=O)CC2)(C3=O)[C@]2([C@@](CC[C@@]4([H])[C@@]5(CC[C@H](O)C4)C)([H])[C@]5([H])[C@@H]3O)O
分子式C24H32O6
分子量416.51
溶解度Ethanol : 10 mg/mL (24.01 mM)
储存条件Store at 2-8°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Arenobufagin is a natural bufadienolide from toad venom; has potent antineoplastic activity against HCC HepG2 cells as well as corresponding multidrug-resistant HepG2/ADM cells.IC50 value: Target: in vitro: arenobufagin induced mitochondria-mediated apoptosis in HCC cells, with decreasing mitochondrial potential, as well as increasing Bax/Bcl-2 expression ratio, Bax translocation from cytosol to mitochondria. Arenobufagin also induced autophagy in HepG2/ADM cells. Autophagy-specific inhibitors (3-methyladenine, chloroquine and bafilomycin A1) or Beclin1 and Atg 5 small interfering RNAs (siRNAs) enhanced arenobufagin-induced apoptosis, indicating that arenobufagin-mediated autophagy may protect HepG2/ADM cells from undergoing apoptotic cell death [1]. arenobufagin inhibited vascular endothelial growth factor (VEGF)-induced viability, migration, invasion and tube formation in human umbilical vein endothelial cells (HUVECs) in vitro [2]. Arenobufagin blocked the Na+/K+ pump current in a dose-dependent manner with a half-maximal concentration of 0.29 microM and a Hill coefficient of 1.1 [3].in vivo: arenobufagin inhibited the growth of HepG2/ADM xenograft tumors, which were associated with poly (ADP-ribose) polymerase cleavage, light chain 3-II activation and mTOR inhibition [1]. Arenobufagin also suppressed sprouting formation from VEGF-treated aortic rings in an ex vivo model [2].

[1]. Zhang DM, et al. Arenobufagin, a natural bufadienolide from toad venom, induces apoptosis and autophagy in human hepatocellular carcinoma cells through inhibition of PI3K/Akt/mTOR pathway. Carcinogenesis. 2013 Jun;34(6):1331-42. [2]. Li M, et al. Arenobufagin, a bufadienolide compound from toad venom, inhibits VEGF-mediated angiogenesis through suppression of VEGFR-2 signaling pathway. Biochem Pharmacol. 2012 May 1;83(9):1251-60. [3]. Cruz Jdos S, et al. Arenobufagin, a compound in toad venom, blocks Na(+)-K+ pump current in cardiac myocytes. Eur J Pharmacol. 1993 Aug 3;239(1-3):223-6.