Cinobufagin

SKU: orb1222235

Description

Cinobufagin is a cardiotoxic bufanolide steroid secreted by the Asiatic toad Bufo gargarizans. It has similar effects to digitalis and is used in traditional Chinese medicine. Cinobufagin has been shown to have clinical applications in cancer treatment as well as immunomodulatory and analgesic properties. Cinobufagin induces apoptosis of osteosarcoma cells through inactivation of Notch signaling. Cinobufagin induces autophagy-mediated cell death in human osteosarcoma U2OS cells through the ROS/JNK/p38 signaling pathway.

Key Properties

• CAS Number: 470-37-1
• MW: 442.55
• Purity: >98% (HPLC)
• Formula: C₂₆H₃₄O₆
• SMILES: CC(=O)O[C@@H]1[C@@H]([C@]2(CC[C@H]3[C@H]([C@]42[C@@H]1O4)CC[C@H]1[C@@]3(CC[C@@H](C1)O)C)C)c1coc(=O)cc1
• Target: Antifungal
• Solubility: DMSO : ≥ 43 mg/mL; 97.17 mM

Bioactivity

• In Vivo:
  Animal model: OCM1 cells tumor xenograft in Nu/Nu nude mice. Dosage: 5 mg/kg. Administration: Intraperitoneal injection (i.p.), once a day for 10 days. Result: Made the tumors grew more slowly than those treated with intraperitoneal injection of saline or untreated. Increased the expression of caspase-3 and PARP in tumor tissues and decreased Bcl-2 and Bcl-xl expression in mouse tumor tissues and increased expression of Bad and Bax. Animal model: U87MG-EGFR subcutaneous and intracranial xenograft model. Dosage: 5 mg/kg. Administration: Intraperitoneal injection (i.p.), once a day for 10 days. Result: Decreased the luminescence intensity of brain tumor about 70%. Decreased p-EGFR, p-STAT3, and p-Akt levels in the intracranial tumors as compared with the vehicles. Decreased Ki67 and active caspase-3 immunostaining of intracranial tumors.
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• In Vitro:
  Cell Proliferation Assay Cell line: OCM1 cell. Concentration: 30, 100, 300 nM. Incubation time: 7 days. Result: Exerted potent cytotoxic in OCM1 cells with an IC50 of 8.023 nM. Apoptosis Analysis Cell line: OCM1 cell. Concentration: 30, 100, 300 nM. Incubation time: 24 hours. Result: Induced cell apoptosis and upregulate the expression levels of cleaved caspase-3, cleaved poly(ADP-ribose) polymerase (PARP), and cleaved caspase-9. Activated the intrinsic mitochondrial apoptosis pathway, which was demonstrated by increased cell apoptosis with increased expression of Bad and Bax, decreased expression of Bcl-2 and Bcl-xl, and reduced mitochondrial membrane potential (MMP).
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Cinobufagin | Cinobufagine | Cino-bufagin

Quick Database Links

Gene Symbol

Antifungal