Appearance:Solid powderPurity: > 98%
| Cat No: | I003611 |
| Cas No: | 464-74-4 |
| Product-Name: | Arenobufagin |
| InChI: | InChI=1S/C24H32O6/c1-22-9-7-15(25)11-14(22)4-5-17-19(22)20(27)21(28)23(2)16(8-10-24(17,23)29)13-3-6-18(26)30-12-13/h3,6,12,14-17,19-20,25,27,29H,4-5,7-11H2,1-2H3/t14-,15+,16-,17-,19-,20+,22+,23+,24+/m1/s1 |
| InChIKey: | JGDCRWYOMWSTFC-AZGSIFHYSA-N |
| SMILES: | O=C(C=C1)OC=C1[[email protected]]([[email protected]]23C)CC[[email protected]]2(O)[[email protected]]4([H])CC[[email protected]]5([H])C[[email protected]@H](O)CC[[email protected]]5(C)[[email protected]@]4([H])[[email protected]](O)C3=O |
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:Arenobufagin activates p53 to trigger esophageal squamous cell carcinoma cell apoptosis in vitro and in vivo. Lv J, Lin S, Peng P, Cai C, Deng J, Wang M, Li X, Lin R, Lin Y, Fang A, Li Q.Onco Targets Ther. 2017 Feb 28;10:1261-1267. doi: 10.2147/OTT.S104767. eCollection 2017. PMID: 28280360 Free PMC Article2:Proteasome Inhibition Contributed to the Cytotoxicity of Arenobufagin after Its Binding with Na, K-ATPase in Human Cervical Carcinoma HeLa Cells. Yue Q, Zhen H, Huang M, Zheng X, Feng L, Jiang B, Yang M, Wu W, Liu X, Guo D.PLoS One. 2016 Jul 18;11(7):e0159034. doi: 10.1371/journal.pone.0159034. eCollection 2016. PMID: 27428326 Free PMC Article3:Arenobufagin intercalates with DNA leading to G2 cell cycle arrest via ATM/ATR pathway. Deng LJ, Peng QL, Wang LH, Xu J, Liu JS, Li YJ, Zhuo ZJ, Bai LL, Hu LP, Chen WM, Ye WC, Zhang DM.Oncotarget. 2015 Oct 27;6(33):34258-75. doi: 10.18632/oncotarget.5545. PMID: 26485758 Free PMC Article4:Quantitative determination of arenobufagin in rat plasma by ultra fast liquid chromatography-tandem mass spectrometry and its application in a pharmacokinetic study. Li G, Han W, Jiang W, Zhang D, Ye W, Chen X, Ma A.J Chromatogr B Analyt Technol Biomed Life Sci. 2013 Nov 15;939:86-91. doi: 10.1016/j.jchromb.2013.09.019. Epub 2013 Sep 23. PMID: 24113236 5:Arenobufagin, a natural bufadienolide from toad venom, induces apoptosis and autophagy in human hepatocellular carcinoma cells through inhibition of PI3K/Akt/mTOR pathway. Zhang DM, Liu JS, Deng LJ, Chen MF, Yiu A, Cao HH, Tian HY, Fung KP, Kurihara H, Pan JX, Ye WC.Carcinogenesis. 2013 Jun;34(6):1331-42. doi: 10.1093/carcin/bgt060. Epub 2013 Feb 7. PMID: 23393227 6:Arenobufagin, a bufadienolide compound from toad venom, inhibits VEGF-mediated angiogenesis through suppression of VEGFR-2 signaling pathway. Li M, Wu S, Liu Z, Zhang W, Xu J, Wang Y, Liu J, Zhang D, Tian H, Li Y, Ye W.Biochem Pharmacol. 2012 May 1;83(9):1251-60. doi: 10.1016/j.bcp.2012.01.023. Epub 2012 Jan 24. PMID: 22305746 7:[Anti-angiogenetic effect of arenobufagin in vitro and in vivo]. Liu JS, Zhang DM, Chen MF, Li MM, Luo QD, Kurihara H, Ye WC.Yao Xue Xue Bao. 2011 May;46(5):527-33. Chinese. PMID: 21800539 8:[Analysis on competitive interaction between arenobufagin and verapamil hydrochloride with serum albumin]. Lu GD, Zhou J, Ma HY, Wu DK, Qian DW, Tang YP, Hong M, Hua YQ, Duan JA.Zhong Xi Yi Jie He Xue Bao. 2011 Jul;9(7):768-74. Chinese. PMID: 21749828 Free Article9:Depressive effects of arenobufagin on the delayed rectifier K+ current of guinea-pig cardiac myocytes. Cruz Jdos S, Matsuda H.Eur J Pharmacol. 1994 Feb 15;266(3):317-25. PMID: 8174614 10:Arenobufagin, a compound in toad venom, blocks Na(+)-K+ pump current in cardiac myocytes. Cruz Jdos S, Matsuda H.Eur J Pharmacol. 1993 Aug 3;239(1-3):223-6. PMID: 8223897
Your information is safe with us.