Arenobufagin

Arenobufagin is a cardiotonic steroid that has been found in the skin secretions of the toad B. gargarizans and has anticancer activity. It inhibits Na+/K+-ATPase activity in isolated guinea pig ventricular myocytes with an IC50 value of 290 nM. Arenobufagin (20-500 nM) induces cleavage of poly(ADP-ribose) polymerase (PARP), caspase-3, and caspase-9, as well as induces apoptosis in HepG2 hepatocellular carcinoma cells. It inhibits proliferation of HepG2, Hep3B, BEL-7402, and MCF-7 cancer cells (IC50s = 101.9, 39.8, 416.3, and 143.7 nM, respectively), as well as multidrug-resistant HepG2/adm and MCF-7/adr cancer cells (IC50s = 730 and 67.5 nM, respectively). Arenobufagin (1 mg/kg once per day, i.v.) reduces tumor growth, the number and size of lung metastases, and tumor levels of the epithelial-to-mesenchymal transition (EMT) markers vimentin and beta-catenin in a PC3 mouse xenograft model. Arenobufagin (5 and 10 µM/plug) inhibits VEGF-induced angiogenesis in a Matrigel(TM) plug assay in mice.Formal Name: (3beta,5beta,11alpha)-3,11,14-trihydroxy-12-oxo-bufa-20,22-dienolide. CAS Number: 464-74-4. Molecular Formula: C24H32O6. Formula Weight: 416.5. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 20 mg/ml, DMSO:PBS (pH 7.2) (1:8): 0.11 mg/ml. lambdamax: 299 nm. SMILES: O[C@H]1CC[C@@]2(C)[C@@](CC[C@]([C@]3(O)[C@@]4(C)[C@](C5=COC(C=C5)=O)([H])CC3)([H])[C@]2([H])[C@H](O)C4=O)([H])C1. InChi Code: 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. InChi Key: JGDCRWYOMWSTFC-AZGSIFHYSA-N. Origin: Plant/Bufonis Venenum.