| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
EtDO-P4 targets glucosylceramide synthase (GCS), the enzyme that catalyzes the first committed step in glycosphingolipid (GSL) biosynthesis. By inhibiting GCS, EtDO-P4 reduces the production of glycosphingolipids, which are important components of cell membranes and are involved in cell signaling. GSLs modulate the activity of receptor tyrosine kinases (RTKs) such as EGFR.
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| ln Vitro |
EtDO-P4 is a nanomolar inhibitor of glycosphingolipid (GSL) synthesis. It inhibits EGFR-induced activation of the ERK pathway. It also inhibits a variety of receptor tyrosine kinases (RTKs). By reducing GSL levels, EtDO-P4 disrupts lipid raft-mediated signaling and RTK activation. Specific IC50 values for GCS inhibition are in the nanomolar range.
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| ln Vivo |
Specific in vivo efficacy data for EtDO-P4 are not extensively detailed in standard reference sources. As an inhibitor of GSL synthesis and RTK signaling, it is expected to show anti-tumor activity in animal models of cancer, including Burkitt lymphoma. Studies in xenograft models would be required to evaluate its in vivo efficacy and to determine optimal dosing regimens.
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| Enzyme Assay |
EtDO-P4's inhibition of glucosylceramide synthase (GCS) can be assessed using in vitro enzyme assays. Recombinant or purified GCS enzyme is incubated with its substrates (UDP-glucose and ceramide) in the presence of varying concentrations of EtDO-P4. The production of glucosylceramide is measured using a suitable detection method (e.g., radiometric, HPLC, or mass spectrometry) to determine the IC50.
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| Cell Assay |
The cellular activity of EtDO-P4 is evaluated in cancer cell lines such as Burkitt lymphoma cells. Cells are treated with increasing concentrations of EtDO-P4, and GSL levels are measured by HPLC or mass spectrometry. EGFR-induced ERK phosphorylation is assessed by Western blot using phospho-specific antibodies. Cell proliferation, viability, and apoptosis are measured to assess the functional effects of GSL depletion.
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| Animal Protocol |
Specific in vivo animal experimental protocols for EtDO-P4 are not extensively detailed in standard reference sources. For evaluating its anti-tumor activity, EtDO-P4 would be administered to tumor-bearing mice (xenograft models) via intraperitoneal or oral routes. Tumor growth, RTK signaling (e.g., EGFR, ERK phosphorylation), and GSL levels in tumors would be measured to assess efficacy.
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| ADME/Pharmacokinetics |
EtDO-P4 has a molecular weight of 516.77 and molecular formula C31H52N2O4. It is soluble in DMSO. The exact mass is 516.3927. Its IUPAC name is N-[(1R,2R)-1-(2,3-dihydro-1,4-benzodioxin-6-yl)-1-hydroxy-3-pyrrolidin-1-ylpropan-2-yl]hexadecanamide. Specific pharmacokinetic parameters are not extensively detailed.
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| Toxicity/Toxicokinetics |
The toxicity profile of EtDO-P4 is not extensively documented. As an inhibitor of GSL synthesis, potential toxicities may include effects on cell membrane integrity and signaling. Specific LD50 values and organ-specific toxicity data are not readily available.
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| Additional Infomation |
EtDO-P4 (CAS# 245329-78-6) is a potent and specific inhibitor of glycosphingolipid (GSL) synthesis, targeting glucosylceramide synthase (GCS). It inhibits EGFR-induced activation of the ERK pathway and a variety of receptor tyrosine kinases (RTKs). It may be used to study many types of tumors like Burkitt lymphoma. The compound is a research tool for studying the role of glycosphingolipids in cell signaling and cancer.
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| Molecular Formula |
C31H52N2O4
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|---|---|
| Molecular Weight |
516.77
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| Exact Mass |
516.393
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| CAS # |
245329-78-6
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| PubChem CID |
9914532
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| Appearance |
White to off-white solid powder
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| Density |
1.05g/cm3
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| Boiling Point |
684.419ºC at 760 mmHg
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| Flash Point |
367.723ºC
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| Vapour Pressure |
0mmHg at 25°C
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| Index of Refraction |
1.524
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| LogP |
6.881
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
19
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| Heavy Atom Count |
37
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| Complexity |
598
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| Defined Atom Stereocenter Count |
2
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| SMILES |
O1C2C=CC(C(O)C(NC(=O)CCCCCCCCCCCCCCC)CN3CCCC3)=CC=2OCC1
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| InChi Key |
BBTZZVJOQCCAOR-DLFZDVPBSA-N
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| InChi Code |
InChI=1S/C31H52N2O4/c1-2-3-4-5-6-7-8-9-10-11-12-13-14-17-30(34)32-27(25-33-20-15-16-21-33)31(35)26-18-19-28-29(24-26)37-23-22-36-28/h18-19,24,27,31,35H,2-17,20-23,25H2,1H3,(H,32,34)/t27-,31-/m1/s1
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| Chemical Name |
N-[(1R,2R)-1-(2,3-dihydro-1,4-benzodioxin-6-yl)-1-hydroxy-3-pyrrolidin-1-ylpropan-2-yl]hexadecanamide
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| Synonyms |
EtDO-P4; EtDO P4; EtDOP4
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9351 mL | 9.6755 mL | 19.3510 mL | |
| 5 mM | 0.3870 mL | 1.9351 mL | 3.8702 mL | |
| 10 mM | 0.1935 mL | 0.9675 mL | 1.9351 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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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