Edelfosine (Synonyms: ET-18-OCH3)

Name: Edelfosine
Brand: MedChemExpress
SKU: HY-108610A
Rating: 4.5 (1 reviews)

Cat. No.: HY-108610A Purity: 99.0%: Data Sheet
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Edelfosine (ET-18-OCH3) is an orally active lipid raft modulator and apoptosis inducer that alters membrane fluidity and preferentially inserts into tumor cell membranes. Edelfosine recruits death receptor ligands (FasL/CD95L, TRAIL) and Bid to lipid rafts to form death-inducing signaling complexes, thereby initiating mitochondria-dependent apoptosis and inducing cytochrome c release. Edelfosine also exerts anti-inflammatory effects, promotes L-Selectin shedding, and causes no gastrointestinal or organ toxicity. In addition, Edelfosine inhibits nucleic acid and protein synthesis in Leishmania donovani and exhibits antiproliferative activity. Edelfosine can be used in research on multiple myeloma, inflammatory bowel diseases (such as ulcerative colitis and Crohn's disease), and visceral leishmaniasis.

For research use only. We do not sell to patients.

Edelfosine Chemical Structure

CAS No. : 70641-51-9

Size	Stock	Quantity
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

Other Forms of Edelfosine:

(R)-Edelfosine In-stock
(S)-Edelfosine In-stock

1 Publications Citing Use of MCE Edelfosine

•Sci Rep. 2026 Mar 25.

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Biological Activity
Purity & Documentation
References
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Description

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	13.5 μM Compound: Edelfosine	Antiproliferative activity of compound was measured on human tumor cell line A431. Antiproliferative activity of compound was measured on human tumor cell line A431.	[PMID: 7707324]
A549	IC₅₀	3.5 μM Compound: 3, ET-18-OMe	Inhibition of Akt phosphorylation in human insulin-stimulated A549 cells incubated for 2 hrs prior to insulin-induction measured after 30 mins by ELISA Inhibition of Akt phosphorylation in human insulin-stimulated A549 cells incubated for 2 hrs prior to insulin-induction measured after 30 mins by ELISA	[PMID: 23415083]
A549	IC₅₀	7.4 μM Compound: 3, ET-18-OMe	Cytotoxicity against human A549 cells by flow cytometric analysis Cytotoxicity against human A549 cells by flow cytometric analysis	[PMID: 23415083]
BXPC-3	IC₅₀	18.8 μM Compound: EDLF	Growth inhibition of human BxPC3 cells after 72 hrs by XTT assay Growth inhibition of human BxPC3 cells after 72 hrs by XTT assay	[PMID: 29547833]
CEM-SS	IC₅₀	4 mM Compound: 10	Concentration of compound required to 50% growth inhibition of HIV-1 in CEM-SS cells Concentration of compound required to 50% growth inhibition of HIV-1 in CEM-SS cells	[PMID: 1901911]
CEM-SS	IC₅₀	4 μM Compound: ET-18-OMe	In vitro inhibition of CEM-SS cell growth by 50 % In vitro inhibition of CEM-SS cell growth by 50 %	[PMID: 2016713]
FHC	IC₅₀	45 μM Compound: Edelfosine	In vitro inhibition of FHC normal human colon cell proliferation In vitro inhibition of FHC normal human colon cell proliferation	10.1016/S0960-894X(97)00433-2
HL-60	IC₅₀	1 μM Compound: Edelfosine	Antiproliferative activity of compound was measured on human tumor cell line HL-60. Antiproliferative activity of compound was measured on human tumor cell line HL-60.	[PMID: 7707324]
HL-60	IC₅₀	12 μM Compound: ET-18-oMe	Inhibition of Protein Kinase C (PKC) isolated from HL-60 human promyelocytic leukemia cells Inhibition of Protein Kinase C (PKC) isolated from HL-60 human promyelocytic leukemia cells	[PMID: 2342075]
HL-60	IC₅₀	2 μM Compound: Edelfosine	In vitro inhibition of HL-60 human promyelocytic leukemia cell proliferation In vitro inhibition of HL-60 human promyelocytic leukemia cell proliferation	10.1016/S0960-894X(97)00433-2
HL-60	IC₅₀	6.1 μM Compound: Edelfosine	Cytotoxicity measured in HL-60 leukemic cells after a 24 hr incubation period. Cytotoxicity measured in HL-60 leukemic cells after a 24 hr incubation period.	[PMID: 7707324]
HT-29	IC₅₀	2 μM Compound: Edelfosine	In vitro inhibition of the HT-29 transformed human colon cell proliferation In vitro inhibition of the HT-29 transformed human colon cell proliferation	10.1016/S0960-894X(97)00433-2
Jurkat	IC₅₀	12.2 μM Compound: Edelfosine	Cytotoxicity against human Jurkat cells assessed as live cells in neubauer chamber after 24 hrs by trypan blue assay Cytotoxicity against human Jurkat cells assessed as live cells in neubauer chamber after 24 hrs by trypan blue assay	[PMID: 21571403]
K562	IC₅₀	6.1 μM Compound: Edelfosine	Antiproliferative activity of compound was measured on human tumor cell line K-562. Antiproliferative activity of compound was measured on human tumor cell line K-562.	[PMID: 7707324]
MCF7	IC₅₀	9.3 μM Compound: 3, ET-18-OMe	Cytotoxicity against human MCF7 cells by flow cytometric analysis Cytotoxicity against human MCF7 cells by flow cytometric analysis	[PMID: 23415083]
MDA-MB-231	IC₅₀	5 μM Compound: Edelfosine	In vitro inhibition of estrogen receptor negative MDA-MB-231 human breast cancer cell proliferation In vitro inhibition of estrogen receptor negative MDA-MB-231 human breast cancer cell proliferation	10.1016/S0960-894X(97)00433-2
MDA-MB-435	IC₅₀	12 μM Compound: ET-18-OCH3	Cytotoxicity against human MDA-MB-435 cells after 3 days in serum free conditions by MTT assay Cytotoxicity against human MDA-MB-435 cells after 3 days in serum free conditions by MTT assay	[PMID: 16279790]
MDA-MB-435	IC₅₀	3 μM Compound: ET-18-OCH3	Inhibition of Akt phosphorylation in MDA-MB-435 cells after 2 hrs Inhibition of Akt phosphorylation in MDA-MB-435 cells after 2 hrs	[PMID: 16279790]
PANC-1	IC₅₀	25.7 μM Compound: EDLF	Growth inhibition of human PANC1 cells after 72 hrs by XTT assay Growth inhibition of human PANC1 cells after 72 hrs by XTT assay	[PMID: 29547833]
THP-1	CC₅₀	12.9 μM Compound: Edelfosine	Cytotoxicity against human THP-1 cells Cytotoxicity against human THP-1 cells	[PMID: 36944273]
THP-1	EC₅₀	1 μM Compound: Edelfosine	Cytotoxicity against human THP1 cells assessed as reduction in cell viability after 24 hrs by propidium iodide staining based fluorescence microscopic analysis Cytotoxicity against human THP1 cells assessed as reduction in cell viability after 24 hrs by propidium iodide staining based fluorescence microscopic analysis	[PMID: 29501944]
THP-1	IC₅₀	3.1 μM Compound: Edelfosine	Leishmanicidal activity against amastigote stage of Leishmania infantum expressing GFP infected in human THP1 cells after 48 hrs by flow cytometric analysis Leishmanicidal activity against amastigote stage of Leishmania infantum expressing GFP infected in human THP1 cells after 48 hrs by flow cytometric analysis	[PMID: 24448421]
THP-1	IC₅₀	4.9 μM Compound: Edelfosine	Cytotoxicity against human THP1 cells after 24 hrs by propidium iodide staining-based flow cytometric analysis Cytotoxicity against human THP1 cells after 24 hrs by propidium iodide staining-based flow cytometric analysis	[PMID: 24448421]
THP-1	IC₅₀	4.96 μM Compound: Edelfosine	Cytotoxicity against human THP1 cells assessed as live cells in neubauer chamber after 24 hrs by trypan blue assay Cytotoxicity against human THP1 cells assessed as live cells in neubauer chamber after 24 hrs by trypan blue assay	[PMID: 21571403]
THP-1	IC₅₀	4.96 μM Compound: Edelfosine	Cytotoxicity against human THP1 cells assessed as reduction in cell viability measured after 24 hrs by propidium iodide staining based flow cytometry Cytotoxicity against human THP1 cells assessed as reduction in cell viability measured after 24 hrs by propidium iodide staining based flow cytometry	[PMID: 32223141]
THP-1	IC₅₀	4.96 μM Compound: Edelfosine	Cytotoxicity against human THP-1 cells assessed as reduction in cell viability incubated for 24 hrs Cytotoxicity against human THP-1 cells assessed as reduction in cell viability incubated for 24 hrs	[PMID: 32738977]

In Vitro

Edelfosine (10 μM; 24-48 h) induces apoptosis in human multiple myeloma (MM) cell lines (MM144, MM1S, MM1R, RPMI-8226, OPM-2), leukemic Jurkat T lymphoid cells and JY B lymphoid cells, with MM144 cells showing the highest sensitivity; however, it does not induce apoptosis in Fas/CD95-deficient human OPM-2 MM cells^[1].
Edelfosine (10 μM; 15 h) induces the translocation of Fas/CD95, DR4, DR5, FADD, procaspase-8, activated caspase-8 and Bid to lipid rafts in human MM144 cells, thereby promoting the formation of the death-inducing signaling complex (DISC), which consists of Fas/CD95, FADD and caspase-8^[1].
Edelfosine (10 μM; 3-24 h) induces apoptosis in human MM144 cells, with this effect emerging after 15 h of incubation. Activation of caspase-3 and PARP is detectable at this time point, and over 50% of cell apoptosis is observed after 24 h of incubation^[1].
Edelfosine (5 μg/mL; 12 h, 18 h) delays spontaneous apoptosis of neutrophils compared with the medium-only control group^[2].
Edelfosine (0.01-5 μg/mL; 15 min) downregulates cell surface L-selectin, CD43 and CD44 (but not CD11a, CD11b or HLA) in a concentration-dependent manner, with an IC₅₀ of 0.29 μM for L-selectin downregulation^[2].
Edelfosine (1.9-95 μM; 4 h) inhibits Leishmania donovani amastigotes in J774A.1 macrophages. After 4 hours of treatment, its ED₅₀ value is 19.47 μM as detected by light microscopy and 23.16 μM as detected by flow cytometry^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis^[1]

Cell Line:	Human multiple myeloma (MM) cell lines (MM144, MM1S, MM1R, RPMI-8226, OPM-2)
Concentration:	10 μM
Incubation Time:	24 h, 48 h
Result:	Induced potent apoptotic responses in all tested MM cell lines. Showed higher sensitivity in MM144 cells (higher cell-surface Fas/CD95 content). Produced similar apoptotic cell death rates in dexamethasone-sensitive MM1S cells and dexamethasone-resistant MM1R cells.

Immunofluorescence^[1]

Cell Line:	Human MM144 cells and primary MM cells from patients
Concentration:	10 μM
Incubation Time:	12 h
Result:	Potentiated coclustering of lipid rafts and Fas/CD95 in MM144 cells, as shown by yellow colocalization areas in merged confocal images. Induced similar coclustering in primary MM cells from patients.

Western Blot Analysis^[1]

Cell Line:	Human MM144 cells
Concentration:	10 μM
Incubation Time:	15 h
Result:	Induced translocation of Fas/CD95, DR4, DR5, FADD, procaspase-8, cleaved active caspase-8 forms, and Bid into lipid raft fractions. Achieved almost complete translocation of Fas/CD95, DR5, FADD, and Bid into lipid rafts.\n Induced formation of DISC containing Fas/CD95, FADD, and caspase-8 in whole cell lysates and in isolated lipid raft fractions. Had its induced DISC formation prevented by disruption of lipid rafts with methyl-β-cyclodextrin.

Apoptosis Analysis^[1]

Cell Line:	Fas/CD95-deficient human OPM-2 MM cells, and OPM-2 cells transduced with full-length Fas/CD95 or truncated FasΔ57C retrovirus
Concentration:	10 μM
Incubation Time:	24 h
Result:	Did not induce apoptosis in Fas/CD95-deficient OPM-2 cells. Restored sensitivity to edelfosine in OPM-2 cells transduced with full-length Fas/CD95. Failed to restore sensitivity in OPM-2 cells transduced with truncated FasΔ57C. Did not restore Fas/CD95 expression in Fas/CD95-deficient OPM-2 cells, nor increase Fas/CD95 expression in Fas/CD95-positive MM144 cells.

Apoptosis Analysis^[1]

Cell Line:	Human MM144 cells stably transfected with Bcl-Xₗ (MM144-Bcl-Xₗ) or empty vector (MM144-Neo)
Concentration:	10 μM
Incubation Time:	15 h (cytochrome c release); 24 h (apoptosis)
Result:	Induced apoptosis and cytochrome c release from mitochondria to the cytosol in MM144-Neo cells. Had both induced cytochrome c release and apoptosis prevented by overexpression of Bcl-Xₗ.

In Vivo

Edelfosine (2.5-5 mg/kg; p.o.; daily; 21 days) inhibits bentonite-induced paw edema in Swiss mice by 34% (2.5 mg/kg) and 49% (5 mg/kg), with no associated body weight loss^[2].
Edelfosine (5 mg/kg; p.o.; daily) reduces TNBS-induced ulcerative colitis severity in Wistar rats by 45.5% at 24 hours and 76.5% at 7 days post-TNBS administration, while abating neutrophil infiltration and supporting colon tissue repair^[2].
Edelfosine (40 mg/kg; p.o.; daily; up to 4 weeks) shows no cardiotoxicity, hepatotoxicity, renal toxicity, or gastrointestinal histologic damage in healthy Wistar rats, and does not inhibit colonic mucosal prostaglandin E₂ synthesis^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Swiss mice inflammation model^[2]
Dosage:	2.5 mg/kg; 5 mg/kg
Administration:	p.o.; daily; 21 days
Result:	Inhibited inflammation by 34%.\nInhibited inflammation by 49%.\nCaused no body weight loss during treatment.

Animal Model:	Wistar rats with Inflammatory bowel disease^[2]
Dosage:	5 mg/kg
Administration:	p.o.; daily
Result:	Protected against TNBS-induced body weight loss.\nReduced colon wet weight.\nInhibited colonic mucosal damage score by 45.5% at 24 hours post-TNBS administration.\nInhibited colonic mucosal damage score by 76.5% at 7 days post-TNBS administration.\nReduced ulcer formation, edema, and inflammatory cell infiltration in colon sections, with focal reparative processes observed.\nDramatically reduced colonic myeloperoxidase and neutrophil elastase activities.\nResulted in only submucosal focal mild inflammatory cell infiltration, compared to widespread intense infiltration in untreated controls.

Animal Model:	Healthy Wistar rats^[2]
Dosage:	40 mg/kg
Administration:	p.o.; daily; 1 week; 4 weeks
Result:	Caused no body weight loss or overt toxicity during 4 weeks of treatment.\nShowed no cardiotoxicity, hepatotoxicity, or renal toxicity via biochemical and functional analyses.\nCaused no histologic damage to kidney, liver, heart, or stomach tissue.\nDid not inhibit basal prostaglandin E2 synthesis in rat colonic mucosal samples (78 ± 10 pg PGE2/mg tissue in control vs. 83 ± 9 pg PGE2/mg tissue in treated rats).

Molecular Weight

523.73

Formula

C₂₇H₅₈NO₆P

CAS No.

70641-51-9

Appearance

Solid

Color

White to off-white

SMILES

CCCCCCCCCCCCCCCCCCOCC(OC)COP([O-])(OCC[N+](C)(C)C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL (47.73 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9094 mL	9.5469 mL	19.0938 mL
5 mM	0.3819 mL	1.9094 mL	3.8188 mL
10 mM	0.1909 mL	0.9547 mL	1.9094 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.25 mg/mL (2.39 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.25 mg/mL (2.39 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 1.25 mg/mL (2.39 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS
Solubility: 25 mg/mL (47.73 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.0%

Select Batch:

Data Sheet (280 KB) SDS (254 KB)

COA (239 KB)

Handling Instructions (2659 KB)

References

[1]. Gajate C, et al. Edelfosine and perifosine induce selective apoptosis in multiple myeloma by recruitment of death receptors and downstream signaling molecules into lipid rafts. Blood. 2007;109(2):711-719. [Content Brief]

[2]. Mollinedo F, et al. Novel anti-inflammatory action of edelfosine lacking toxicity with protective effect in experimental colitis. J Pharmacol Exp Ther. 2009;329(2):439-449. [Content Brief]

[3]. Azzouz S, et al. Leishmanicidal activity of edelfosine, miltefosine and ilmofosine. Basic Clin Pharmacol Toxicol. 2005;96(1):60-65. [Content Brief]

[4]. Hac-Wydro K, et al. Effect of edelfosine on tumor and normal cells model membranes--a comparative study. Colloids Surf B Biointerfaces. 2010;76(1):366-369. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.9094 mL	9.5469 mL	19.0938 mL	47.7345 mL
	5 mM	0.3819 mL	1.9094 mL	3.8188 mL	9.5469 mL
	10 mM	0.1909 mL	0.9547 mL	1.9094 mL	4.7735 mL
	15 mM	0.1273 mL	0.6365 mL	1.2729 mL	3.1823 mL
	20 mM	0.0955 mL	0.4773 mL	0.9547 mL	2.3867 mL
	25 mM	0.0764 mL	0.3819 mL	0.7638 mL	1.9094 mL
	30 mM	0.0636 mL	0.3182 mL	0.6365 mL	1.5912 mL
	40 mM	0.0477 mL	0.2387 mL	0.4773 mL	1.1934 mL

Edelfosine Related Classifications

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Edelfosine (Synonyms: ET-18-OCH3)

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Other Forms of Edelfosine:

1 Publications Citing Use of MCE Edelfosine

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Complete Stock Solution Preparation Table

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Edelfosine (Synonyms: ET-18-OCH3)

Customer Review

Other Forms of Edelfosine:

Edelfosine Related Antibodies

1 Publications Citing Use of MCE Edelfosine

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Edelfosine Related Antibodies

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Complete Stock Solution Preparation Table

Edelfosine Related Classifications

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