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Ingenol Mebutate

Cat. No. M5030
Ingenol Mebutate Structure
Synonym:

Ingenol 3-angelate; PEP005

Size Price Availability Quantity
1mg USD 80  USD80 In stock
5mg USD 250  USD250 In stock
10mg USD 410  USD410 In stock
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Quality Control & Documentation
Biological Activity

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.

Customer Product Validations & Biological Datas
Source Mol Cancer Ther (2015). Figure 4. Ingenol Mebutate
Method qPCR
Cell Lines SCC cells
Concentrations 100 nmol/L
Incubation Time 24 h
Results In addition, we used either the PKC inhibitor AEB071 or a knockdown of PKCd, either alone or in combination with ingenol mebutate and analyzed the expression of ERK target genes. Either inhibition of PKC or knockdown of PKCd could prevent the upregulation of ERK target gene expression after ingenol mebutate treatment
Source Mol Cancer Ther (2015). Figure 3. Ingenol Mebutate
Method Western blotting
Cell Lines SCC13 cells
Concentrations 100 nmol/L
Incubation Time 24 h
Results Similar to our findings with the PKC inhibitor, we detected a rescue of cell viability upon ingenol mebutate treatment when PKCd was knocked down. A knockdown PKCa followed by ingenol mebutate treatment led only to a partial rescue, while PKCd knockdown could rescue the ingenol mebutate–treated cells completely
Protocol (for reference only)
Cell Experiment
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
Animal models BALB/c nu−/nu− mice
Formulation isopropanol-based gel
Dosages 18 μg/kg
Administration i.v.
Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Cozzi SJ, et al. Arch Dermatol Res. Effective treatment of squamous cell carcinomas with ingenol mebutate gel in immunologically intact SKH1 mice.

[2] Lebwohl M,et.al. N Engl J Med. Ingenol mebutate gel for actinic keratosis.

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Keywords: Ingenol Mebutate, Ingenol 3-angelate; PEP005 supplier, PKC, inhibitors, activators


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