| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 1g | |||
| Other Sizes |
| Targets |
12-Deoxyphorbol 13-phenylacetate 20-acetate targets protein kinase C (PKC) isoforms, a family of serine/threonine kinases that play critical roles in cell signaling, proliferation, differentiation, and survival. As a phorbol ester, it binds to the C1 domain of PKC and activates the enzyme, mimicking the effects of the natural activator diacylglycerol (DAG). This activation leads to the phosphorylation of downstream targets and modulation of various cellular processes. Its effects are mediated through the PKC signaling pathway, which is involved in numerous physiological and pathological processes including cancer, inflammation, and neurological function.
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| ln Vitro |
In vitro, 12-Deoxyphorbol 13-phenylacetate 20-acetate acts as a potent activator of PKC isoforms. As a phorbol ester, it is used to study PKC-mediated signaling pathways in various cell types. It induces cell proliferation, differentiation, or tumor promotion depending on the cellular context. Its activity is typically assessed by measuring PKC activation, downstream signaling events such as MAPK or NF-κB activation, and cellular responses such as proliferation or differentiation. These in vitro activities make it a valuable tool for studying PKC signaling and its role in various biological processes.
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| ln Vivo |
In vivo, 12-Deoxyphorbol 13-phenylacetate 20-acetate is used in research to study tumor promotion and PKC-mediated effects.【32†11】 As a phorbol ester, it is a potent tumor promoter in animal models of skin carcinogenesis. Its effects are mediated through PKC activation and downstream signaling pathways. However, detailed in vivo efficacy and safety data are described in the primary literature. The compound is primarily used in research applications and is not intended for human therapeutic use. Its tumor-promoting activity makes it a valuable tool for studying carcinogenesis.
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| Enzyme Assay |
For in vitro biochemical assays, 12-Deoxyphorbol 13-phenylacetate 20-acetate is evaluated for its PKC activating activity. PKC activity is measured using kinase assays with recombinant PKC isoforms and specific peptide substrates. Binding affinity to the PKC C1 domain can be assessed using competitive binding assays with radiolabeled phorbol esters. Downstream signaling events such as MAPK and NF-κB activation are assessed by Western blotting for phosphorylated proteins. These cell-free and cell-based assays help characterize the compound's PKC activating activity and mechanism of action.
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| Cell Assay |
In vitro cellular assays for 12-Deoxyphorbol 13-phenylacetate 20-acetate are performed using various cell types including cancer cells, immune cells, and neuronal cells. Cells are cultured in standard media and treated with the compound at various concentrations. PKC activation is assessed by measuring the translocation of PKC from the cytosol to the membrane. Downstream signaling is assessed by Western blotting for phosphorylated proteins. Cellular responses such as proliferation, differentiation, or apoptosis are assessed using appropriate assays. These cellular assays help validate the compound's PKC activating activity and its effects on cell function.
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| Animal Protocol |
In vivo animal experiments with 12-Deoxyphorbol 13-phenylacetate 20-acetate are conducted in models of tumor promotion. The compound is typically applied topically to the skin of mice in two-stage carcinogenesis models. Tumor incidence and multiplicity are monitored over time. The compound's tumor-promoting activity is compared to that of other phorbol esters such as TPA. Tissue samples are analyzed for PKC activation and downstream signaling markers. These studies help establish the compound's potency as a tumor promoter and its mechanism of action.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of 12-Deoxyphorbol 13-phenylacetate 20-acetate are not extensively documented. As a phorbol ester with a molecular weight of 508.61,【32†27】 it is expected to have limited oral bioavailability. The compound is typically applied topically in research studies. Detailed PK parameters such as half-life, Cmax, Tmax, AUC, and protein binding are not available in the literature. The compound should be stored under recommended conditions to maintain stability.
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| Toxicity/Toxicokinetics |
The toxicological profile of 12-Deoxyphorbol 13-phenylacetate 20-acetate is characterized by its tumor-promoting activity. As a phorbol ester, it is a potent tumor promoter and should be handled with extreme caution. The compound can cause skin irritation and is a potential carcinogen. It is intended for research use only and not for human therapeutic applications. Appropriate safety precautions, including the use of personal protective equipment and working in a fume hood, should be followed when handling this compound. Comprehensive toxicity studies have been conducted in the context of tumor promotion research.
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| Additional Infomation |
12-Deoxyphorbol 13-phenylacetate 20-acetate is a valuable research tool for studying PKC signaling, tumor promotion, and carcinogenesis.【32†11】 As a potent activator of PKC isoforms, it is used to investigate the role of PKC in cell proliferation, differentiation, and survival. Its tumor-promoting activity makes it useful for studying the mechanisms of carcinogenesis and for developing chemopreventive agents. The compound can be employed to study the structure-activity relationships of phorbol esters and to identify new PKC modulators. Its use is primarily in cancer research and signal transduction studies.
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| Molecular Formula |
C30H36O7
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|---|---|
| Exact Mass |
508.246
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| CAS # |
54662-30-5
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| PubChem CID |
3034821
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.29g/cm3
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| Boiling Point |
635.7ºC at 760 mmHg
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| Flash Point |
204.3ºC
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| Index of Refraction |
1.607
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| LogP |
3.323
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
37
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| Complexity |
1070
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| Defined Atom Stereocenter Count |
7
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| SMILES |
CC1=C[C@@H]2[C@](CC(=C[C@H]3[C@@H]4C(C)(C)[C@@]4(C[C@@H](C)[C@@]32O)OC(=O)CC5=CC=CC=C5)COC(=O)C)(C1=O)O
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| InChi Key |
MEDVHSNRBPAIPU-XMOZQXTISA-N
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| InChi Code |
InChI=1S/C30H36O7/c1-17-11-23-28(34,26(17)33)15-21(16-36-19(3)31)12-22-25-27(4,5)29(25,14-18(2)30(22,23)35)37-24(32)13-20-9-7-6-8-10-20/h6-12,18,22-23,25,34-35H,13-16H2,1-5H3/t18-,22+,23-,25-,28-,29+,30-/m1/s1
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| Chemical Name |
[(1R,2S,6R,10S,11R,13S,15R)-8-(acetyloxymethyl)-1,6-dihydroxy-4,12,12,15-tetramethyl-5-oxo-13-tetracyclo[8.5.0.02,6.011,13]pentadeca-3,8-dienyl] 2-phenylacetate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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