A cardiotonic steroid with anticancer activity; inhibits Na+/K+-ATPase activity in isolated guinea pig ventricular myocytes (IC50 = 290 nM); increases cleavage of PARP

Arenobufagin – 10 mg

Brand:
Cayman
CAS:
464-74-4
Storage:
-20
UN-No:
Non-Hazardous - /

Arenobufagin is a cardiotonic steroid that has been found in the skin secretions of the toad B. gargarizans and has anticancer activity.{52655,52656,42766,52657} It inhibits Na+/K+-ATPase activity in isolated guinea pig ventricular myocytes with an IC50 value of 290 nM.{52655} 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.{52656} 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 β-catenin in a PC3 mouse xenograft model.{42766} Arenobufagin (5 and 10 µM/plug) inhibits VEGF-induced angiogenesis in a Matrigel™ plug assay in mice.{52657}  

 

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Description

A cardiotonic steroid with anticancer activity; inhibits Na+/K+-ATPase activity in isolated guinea pig ventricular myocytes (IC50 = 290 nM); increases cleavage of 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); reduces tumor growth, the number and size of lung metastases, and tumor levels of the EMT markers vimentin and β-catenin in a PC3 mouse xenograft model at 1 mg/kg; inhibits VEGF-induced angiogenesis in a Matrigel™ plug assay in mice at 5 and 10 µM/plug

Formal name: (3β,5β,11α)-3,11,14-trihydroxy-12-oxo-bufa-20,22-dienolide

Synonyms: 

Molecular weight: 416.5

CAS: 464-74-4

Purity: ≥95%

Formulation: A crystalline solid

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