PF-06424439

Catalog No.S9921 Batch:S992101

Print

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 40%PEG300 5%Tween80 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. 
Clear solution
5% DMSO 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. 
* <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.<sup><a class="sref" href="#s_ref">[2]</a></sup>

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.<sup><a class="sref" href="#s_ref">[1]</a></sup>

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.

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

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.