PF-06424439

Catalog No.S9921 Batch:S992101

Technical Data

Formula

C₂₃H₃₀ClN₇O₄S

Molecular Weight

536.05

CAS No.

1469284-79-4

Solubility (25°C)*

In vitro

DMSO

88 mg/mL (164.16 mM)

Water

88 mg/mL (164.16 mM)

Ethanol

88 mg/mL (164.16 mM)

In vivo (Add solvents to the product individually and in order)

Clear solution	5% DMSO 1 95% Corn oil	0.55mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 11 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	4.4mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 88 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

PF-06424439 is a first orally bioavailable small-molecule inhibitor of DGAT2 with an IC50 of 14 nM.

Targets

DGAT2 ^[1]

14 nM

In vitro

PF-06424439 treatment reduces LD content and inhibites cell migration, without affecting cell proliferation. PF-06424439 pre-treatment followed by radiation can enhance radiosensitivity of MCF7 cells.<a class="sref" href="#s_ref">[2]</a>

In vivo

PF-06424439 reduces plasma triglyceride (TG) and cholesterol levels and decreases nonsignificant in circulating lipids in mice (Ldlr-/-). PF-06424439 shows moderate clearance in rats following intravenous administration and moderate steady-state volume of distribution (Vdss) results in a short half-life.<a class="sref" href="#s_ref">[1]</a>

Protocol (from reference)

Cell Assay:^{<sup><a class="sref" href="#s_ref">[2]</a></sup>}	Cell lines MCF-7 cells Concentrations 1, 10, 50, 100, 200 μM Incubation Time 24, 48, 72, and 96 h Method MCF7 cells are seeded at 4.7 × 10<sup>3</sup> cells/well in 96-well black polystyrene microplates and incubated overnight at 37 °C to allow for cell attachment. The next day, cells are treated with 1, 10, 50, 100, 200 μM of PF-06424439 for 24, 48, 72, and 96 h, and then used for Cell Viability Assay by Presto Blue Cell Viability Reagent. Cells are seeded in 100 mm dishes, incubated overnight at 37 °C and then treated with 10 μM of PF-06424439 for 72 h. Subsequently, cells are collected for clonogenic survival assay, cell death detection, cell cycle analysis, γ-H2AX staining,and lipid droplets staining.<sup><a class="sref" href="#s_ref">[2]</a></sup>
Animal Study:^{<sup><a class="sref" href="#s_ref">[1]</a></sup>}	Animal Models Male low-density lipoprotein receptor (Ldlr) knockout mice (Ldlr-/-) Dosages 60 mg/kg Administration p.o., i.v.

Cell Assay:^{<a class="sref" href="#s_ref">[2]</a>}

Cell lines
MCF-7 cells
Concentrations
1, 10, 50, 100, 200 μM
Incubation Time
24, 48, 72, and 96 h
Method
MCF7 cells are seeded at 4.7 × 103 cells/well in 96-well black polystyrene microplates and incubated overnight at 37 °C to allow for cell attachment. The next day, cells are treated with 1, 10, 50, 100, 200 μM of PF-06424439 for 24, 48, 72, and 96 h, and then used for Cell Viability Assay by Presto Blue Cell Viability Reagent. Cells are seeded in 100 mm dishes, incubated overnight at 37 °C and then treated with 10 μM of PF-06424439 for 72 h. Subsequently, cells are collected for clonogenic survival assay, cell death detection, cell cycle analysis, γ-H2AX staining,and lipid droplets staining.<a class="sref" href="#s_ref">[2]</a>

Animal Study:^{<a class="sref" href="#s_ref">[1]</a>}

Animal Models
Male low-density lipoprotein receptor (Ldlr) knockout mice (Ldlr-/-)
Dosages
60 mg/kg
Administration
p.o., i.v.

References

RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.