[CAS NO. 1811510-56-1] PF-06260933

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PRODUCTS SPECIFICATIONS [1811510-56-1]

Catalog

HY-19562

Brand

MCE

CAS

1811510-56-1

DESCRIPTION [1811510-56-1]

Overview

MDL	-
Molecular Weight	296.75
Molecular Formula	C16H13ClN4
SMILES	NC1=C(C2=CC=C(Cl)C=C2)C=C(C(C=N3)=CC=C3N)C=N1

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

Summary

PF-06260933 is an orally active and highly selective inhibitor of MAP4K4 with IC ₅₀ s of 3.7 and 160 nM for kinase and cell, respectively.

IC50 & Target

MAP4K4

3.7 nM (IC ₅₀ )

In Vitro

PF-06260933 treatment of human aortic endothelial cell (EC) robustly prevents TNF-α-mediated endothelial permeability in vitro , similar to MAP4K4 knockdown ^[2] .

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

In Vivo

In the mice model, PF-06260933 treatment does not alter plasma lipid content, although reductions in glucose levels are observed, which is consistent with whole-body-inducible Map4k4 knockout animals. PF-06260933 administration ameliorates further plaque development and/or promotes plaque regression in this animal model (46.0% versus 25.5%), and a reduction in plasma glucose as well as lipid content is also observed ^[2] .

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

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 30 mg/mL ( 101.10 mM ; Need ultrasonic and warming)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.3698 mL	16.8492 mL	33.6984 mL
5 mM	0.6740 mL	3.3698 mL	6.7397 mL
10 mM	0.3370 mL	1.6849 mL	3.3698 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (8.42 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (8.42 mM); Clear solution

* All of the co-solvents are available by MCE.