Ingenol Mebutate is a diterpenoid derived from Euphorbia plant and a modulator of PKC with Ki values of 0.3, 0.105, 0.162, 0.376 and 0.171 nM for PKC-α, PKC-β, PKC-γ, PKC-δ and PKC-ε, respectively.In addition, Ingenol Mebutate is a cell death inducer with anticancer activity.Ingenol Mebutate has been shown to be an anticancer agent. Ingenol Mebutate is also an inducer of cell death and has anticancer activity.
Cell Experiment | |
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Cell lines | T7 cell |
Preparation method | Tumours were treated topically (on days 4 and 5 post tumour inoculation) with 30 μl of 0.25 % (w/v) ingenol mebutate or placebo gel (supplied by LEO Pharma A/S) using a positive displacement pipette, with the gel then spread over the tumour site. |
Concentrations | 30 μl of 0.25 % (w/v) |
Incubation time | 48 h |
Animal Experiment | |
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Animal models | BALB/c nu−/nu− mice |
Formulation | isopropanol-based gel |
Dosages | 18 μg/kg |
Administration | i.v. |
Molecular Weight | 430.53 |
Formula | C25H34O6 |
CAS Number | 75567-37-2 |
Solubility (25°C) | 41 mg/ml in CHCl3 |
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.
[2] Lebwohl M,et.al. N Engl J Med. Ingenol mebutate gel for actinic keratosis.
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