Protein Inhibitors - PD173074 (CAS: 219580-11-7)

PD173074 (CAS: 219580-11-7)

Catalog #：EBC51147

Biological Activity

Synonyms

PD 173074, UNII-A4TLL8634Y, PD-173074

Chemical Name

N-[2-[[4-(Diethylamino)butyl]amino]-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-yl]-N'-(1,1-dimethylethyl)urea

Application

PD173074 is a poten and selective fibroblast growth factor receptor (FGR) inhibitor

CAS Number

219580-11-7

Purity

≥99.0%

Molecular Weight

523.67

Molecular Formula

C₂₈H₄₁N₇O₃

SMILES

CCN(CC)CCCCNC1=NC2=NC(=C(C=C2C=N1)C3=CC(=CC(=C3)OC)OC)NC(=O)NC(C)(C)C

Target & IC50

FGFR1: IC50 = 21.5 nM
PDGFR: IC50 = 17.6 μM
c-Src: IC50 = 19.8 μM

Shipping

Gel Pack

Storage

Store at -20°C

Preparing Stock Solutions

Molecular Structure

ConcentrationSolventMass	1 mg	5 mg	10 mg
1 mM	1.9096 ml	9.5480 ml	19.0960 ml
5 mM	0.3819 ml	1.9096 ml	3.8192 ml
10 mM	0.1910 ml	0.9548 ml	1.9096 ml
50 mM	0.0382 ml	0.1910 ml	0.3819 ml

Solubility
DMSO: 100 mg/mL (190.96 mM) Ethanol: 100 mg/mL (190.96 mM)

Product Description

PD173074 is a cell-permeable pyridopyrimidine compound that has been shown to act as a potent, ATP-competitive, and reversible inhibitor of FGF and VEGF receptors {IC50 = 21.5 nM for Flg (FGFR1)}. It has been used to inhibit PDGFR and c-Src only at much higher concentration (IC50 = 17.6 μM, 19.8 μM, respectively) and exhibits little effect against EGFR, InsR, MEK, and cPKC even at concentrations as high as 50 μM. It has also been shown to inhibit the autophosphorylation of endogenous Flg (FGFR1, IC50 <5 nM) and overexpressed Flk-1 (VEGFR2, IC50 <200 nM) in NIH3T3 cells in vitro. Inhibition of FGFR signaling impairs angiogenesis as well as self-renewal of stem cells via ERK1/2 activation. Also indicated as an inhibitor of FGFR-3.