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PF-06424439

Catalog No.S9921 Purity:99.92%

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

PF-06424439 Chemical Structure

CAS No. 1469284-79-4

Purity & Quality Control

Batch: S992101 DMSO]88 mg/mL]false]Water]88 mg/mL]false]Ethanol]88 mg/mL]false Purity: 99.92%

99.92

PF-06424439 Related Products

Related Targets	ACAT ACAT1 ACAT2 DGAT DGAT1 DGAT2	Click to Expand
Related Compound Libraries	Metabolism Compound Library Anti-cancer Metabolism Compound Library Glutamine Metabolism Compound Library Carbohydrate Metabolism Compound Library Lipid Metabolism Compound Library	Click to Expand

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
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>
Cell Research	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>

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

References
[1] Kentaro Futatsugi , et al. J Med Chem . 2015 Sep 24;58(18):7173-85. [2] Nisticò C, et al. Int J Mol Sci. 2021 Sep 18;22(18):10102.

References

Chemical Information & Solubility

Molecular Weight	536.05	Formula	C₂₃H₃₀ClN₇O₄S
CAS No.	1469284-79-4	SDF	--
Smiles	C[S](O)(=O)=O.ClC1=C[N](N=C1)C2(CC2)C3=NC4=CC=C(N=C4[NH]3)N5CCCC(C5)C(=O)N6CCCC6
Storage (From the date of receipt)	3 years -20°C powder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years -20°C powder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 88 mg/mL ( (164.16 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 88 mg/mL

Ethanol : 88 mg/mL

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

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Molarity Calculator

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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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