2. Metabolic Enzyme/Protease Apoptosis
  3. Phospholipase Apoptosis
  4. DS68591889

DS68591889 is a selective and orally active phosphatidylserine synthase 1 (PTDSS1) inhibitor. DS68591889 has no inhibitory activity against PTDSS2. DS68591889 induces the phospholipid imbalance in a wide range of cancer cells. DS68591889 negatively regulates B cell receptor (BCR)-induced Ca2+ signaling and subsequent apoptotic cell death. DS68591889 can be used for the cancer research, such as B cell lymphoma.

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

DS68591889 Chemical Structure

DS68591889 Chemical Structure

CAS No. : 2488609-21-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO In-stock
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
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Description

DS68591889 is a selective and orally active phosphatidylserine synthase 1 (PTDSS1) inhibitor. DS68591889 has no inhibitory activity against PTDSS2. DS68591889 induces the phospholipid imbalance in a wide range of cancer cells. DS68591889 negatively regulates B cell receptor (BCR)-induced Ca2+ signaling and subsequent apoptotic cell death. DS68591889 can be used for the cancer research, such as B cell lymphoma[1].

IC50 & Target

PTDSS1[1]
In Vitro

DS68591889 (0.1-1000 nM; 4-6 days) strongly suppresses the growth of malignant B cell lymphoma-derived lines[1].
DS68591889 (100 nM; 3 days) enhances BCR-induced Ca2+ signaling and cell apoptosis in Ramos cells1.
DS68591889 (100 nM; 3 days) increases IP1 production, changes the levels of PI4P and PI(4,5)P2, and affects the subcellular localization of related proteins in Ramos cells1.
DS68591889 (100 nM; 24 hours) increases the PIP level, and alters the phospholipid metabolism related to ORP5/8 and Nir2/3 and the BCR-induced Ca2+ response in Ramos cells1.
In HeLa cells, DS68591889 (10-1000 nM; 2 days) causes a substantial loss of phosphatidylserine (PS) and phosphatidylethanolamine (PE), along with a slight decrease in phosphatidylglycerol (PG) and sphingomyelin (SM) and an increase in phosphatidic acid (PA)[1].
In a panel of 47 human cancer cell lines, DS68591889 causes a reduction of PS levels in a wide range of cell lines. DS68591889 reduces the levels of major PS acyl-chain species such as C36:1-PS and C34:1-PS, whereas it slightly increased the level of C40:6-PS, which is mainly produced by PTDSS2. DS68591889 also causes a profound reduction of C36:1-PE and C34:1-PE, indicating substantial PE production from PS species by PS decarboxylase in mitochondria[1].

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

Apoptosis Analysis1

Cell Line: Ramos cells
Concentration: 100 nM
Incubation Time: 3 days
Result: Enhanced BCR-induced Ca2+ signaling and cell apoptosis.
In Vivo

DS68591889 (PTDSS1i) (10-100 mg/kg; oral administration; once daily; treatment cycle of 21 days) inhibits the engraftment of Jeko-1 cells in the bone marrow of mice and prolongs the survival time of mice in an intravenous xenograft mouse model with Jeko-1 lymphoma cells expressing luciferase[1].

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

Animal Model: Female NSG mice (6-week-old) with intravenous injection of Jeko-1-Luc cells[1].
Dosage: 10 mg/kg, 30 mg/kg, 100 mg/kg
Administration: Oral administration, once daily, for 21 days
Result: Suppressed Jeko-1 cell engraftment in the bone marrow of mice with systemic spread1.
Molecular Weight

600.49

Formula

C29H21F5N4O5
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1OC2=C(C3=NNC4=C3C(C5=CC=C(C=C5)OC6=CC=C(C(C)=C6)OC(F)(F)F)N(CC(F)(C)F)C4=O)C=CC=C2N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 200 mg/mL (333.06 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 1.6653 mL 8.3265 mL 16.6531 mL
5 mM 0.3331 mL 1.6653 mL 3.3306 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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: 5 mg/mL (8.33 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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% Corn Oil

    Solubility: 5 mg/mL (8.33 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 5 mg/mL. 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 (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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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, PEG300/PEG400, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Purity & Documentation
References

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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6653 mL 8.3265 mL 16.6531 mL 41.6327 mL
5 mM 0.3331 mL 1.6653 mL 3.3306 mL 8.3265 mL
10 mM 0.1665 mL 0.8327 mL 1.6653 mL 4.1633 mL
15 mM 0.1110 mL 0.5551 mL 1.1102 mL 2.7755 mL
20 mM 0.0833 mL 0.4163 mL 0.8327 mL 2.0816 mL
25 mM 0.0666 mL 0.3331 mL 0.6661 mL 1.6653 mL
30 mM 0.0555 mL 0.2776 mL 0.5551 mL 1.3878 mL
40 mM 0.0416 mL 0.2082 mL 0.4163 mL 1.0408 mL
50 mM 0.0333 mL 0.1665 mL 0.3331 mL 0.8327 mL
60 mM 0.0278 mL 0.1388 mL 0.2776 mL 0.6939 mL
80 mM 0.0208 mL 0.1041 mL 0.2082 mL 0.5204 mL
100 mM 0.0167 mL 0.0833 mL 0.1665 mL 0.4163 mL
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DS68591889 Related Classifications

Keywords:

DS685918892488609-21-6DS 68591889DS-68591889PhospholipaseApoptosisPTDSS1PTDSS2InhibitorAntitumorinhibitorinhibit

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