Reagentes e instrumentos para imunologia, biologia celular e biologia molecular.
 
> JTE-013 [383150-41-2]

JTE-013 [383150-41-2]

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Referência HY-100675-100mg

Tamanho : 100mg

Marca : MedChemExpress


Description

JTE-013 is a potent and specific S1P2 (Sphingosine-1-Phosphate 2; EDG-5) antagonist. JTE-013 inhibits the specific binding of radiolabeled S1P to human and rat S1P2 with IC50s of 17 nM and 22 nM, respectively[1].

IC50 & Target

IC50: 17 nM (S1P2 for human) and 22 nM (S1P2 for rat)[1]
Cellular Effect
Cell Line Type Value Description References
Caco-2 CC50
16.45 μM
Compound: JTE-013
Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
10.21203/rs.3.rs-23951/v1
Caco-2 IC50
5.97 μM
Compound: JTE-013
Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
10.21203/rs.3.rs-23951/v1
HCT-116 EC50
17.13 μM
Compound: JTE-013
Reversal of 5-FU resistance against human HCT-116 cells overexpressing DPD assessed as inhibition of cell proliferation measured after 72 hrs in presence of 5-FU by MTT assay
Reversal of 5-FU resistance against human HCT-116 cells overexpressing DPD assessed as inhibition of cell proliferation measured after 72 hrs in presence of 5-FU by MTT assay
[PMID: 34411894]
HCT-116 EC50
18.28 μM
Compound: JTE-013
Reversal of 5-FU resistance against 5-FU resistant DPD expressed human HCT-116 cells assessed as reduction in cell viability incubated for 48 hrs in presence of 5-FU by MTT assay
Reversal of 5-FU resistance against 5-FU resistant DPD expressed human HCT-116 cells assessed as reduction in cell viability incubated for 48 hrs in presence of 5-FU by MTT assay
[PMID: 34688013]
NCM460 EC50
61.34 μM
Compound: JTE-013
Cytotoxicity against human NCM460 cells assessed as cell viability measured after 72 hrs in presence of 5-FU by MTT assay
Cytotoxicity against human NCM460 cells assessed as cell viability measured after 72 hrs in presence of 5-FU by MTT assay
[PMID: 34411894]
SW620/5-FU EC50
58.58 μM
Compound: JTE-013
Reversal of 5-FU resistance against human SW620/5-FU cells assessed as inhibition of cell proliferation measured after 72 hrs in presence of 5-FU by MTT assay
Reversal of 5-FU resistance against human SW620/5-FU cells assessed as inhibition of cell proliferation measured after 72 hrs in presence of 5-FU by MTT assay
[PMID: 34411894]
SW620/5-FU EC50
58.58 μM
Compound: JTE-013
Reversal of 5-FU resistance against human SW620/5-FU cells assessed as reduction in cell viability incubated for 48 hrs in presence of 5-FU by MTT assay
Reversal of 5-FU resistance against human SW620/5-FU cells assessed as reduction in cell viability incubated for 48 hrs in presence of 5-FU by MTT assay
[PMID: 34688013]
In Vitro

JTE-013 (50-200 μM; 1-3 days) reduces cell viability[1].
JTE-013 (10-1000 nM; 30 mins) reverses S1P-induced Akt inhibition and inhibits S1P-induced ERK activation[1].
JTE-013 displays 4.2% inhibition of S1P3 and does not antagonize S1P1 at concentrations up to 10 μM[1].

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

JTE-013 Related Antibodies

Cell Viability Assay[1]

Cell Line: SK-N-AS cells
Concentration: 50, 100, 150, 200 μM
Incubation Time: 1-3 days
Result: Reduced cell viability.

Western Blot Analysis[1]

Cell Line: SK-N-AS cells
Concentration: 10, 100, 1000 nM
Incubation Time: 30 mins
Result: Reversed S1P-induced Akt inhibition and inhibited S1P-induced ERK activation.
In Vivo

JTE-013 (gavage; 30 mg/kg daily for 14 consecutive days) reduces tumor size and tumor weight[1].

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

Animal Model: Six-week-old female athymic NCr-nu/nu nude mice[1]
Dosage: 30 mg/kg
Administration: Gavage; daily for 14 consecutive days
Result: Reduced tumor size and tumor weight.
Masse moléculaire

408.29

Formule

C17H19Cl2N7O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(C1=C2C(N(C)N=C2C)=NC(NNC(NC3=CC(Cl)=NC(Cl)=C3)=O)=C1)C
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
Solvant et solubilité
In Vitro: 

DMSO : 100 mg/mL (244.92 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 2.4492 mL 12.2462 mL 24.4924 mL
5 mM 0.4898 mL 2.4492 mL 4.8985 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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: ≥ 2.5 mg/mL (6.12 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (6.12 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Pureté et documentation
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