Bufalin is a potent Na+/K+-ATPase inhibitor, binds to the subunit α1, α2 and α3, with Kd of 42.5, 45 and 40 nM respectively, it has anti-cancer activity. Bufalin (2 μM) increases caspae-3, Endo G and GADD153 mRNA expression, but decreases the GRP78 mRNA expression.
In vivo, Bufalin (0.1, 0.2, or 0.4 mg/kg, i.p., daily for 14 days) shows significant anti-tumor activity in mice bearing NCI-H460 cells.
Molecular Weight | 386.52 |
Formula | C24H34O4 |
CAS Number | 465-21-4 |
Solubility (25°C) | DMSO 30 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[1] Lei Dou, et al. Bufalin suppresses ovarian cancer cell proliferation via EGFR pathway
[3] Shan Su, et al. Bufalin inhibits ovarian carcinoma via targeting mTOR/HIF-α pathway
[4] Min Li, et al. Bufalin-induced cardiotoxicity: new findings into mechanisms
[5] Yu-Long Lan, et al. A research update on the anticancer effects of bufalin and its derivatives
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