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P2499

PD 173074

Name: PD 173074
Brand: SIGMA

≥96% (HPLC), FGFR1 and receptor-3 inhibitor, powder

Synonym(s):

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

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About This Item

Empirical Formula (Hill Notation):

C₂₈H₄₁N₇O₃

CAS Number:

219580-11-7

Molecular Weight:

523.67

UNSPSC Code:

12352200

PubChem Substance ID:

24724575

NACRES:

NA.77

MDL number:

MFCD08705327

Assay:

≥96% (HPLC)

Form:

powder

Quality level:

100

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Properties

Product Name

PD 173074, ≥96% (HPLC), powder

Quality Level

100

assay

≥96% (HPLC)

form

powder

color

faintly yellow to dark yellow

solubility

DMSO: 10 mg/mL, clear

storage temp.

2-8°C

SMILES string

CCN(CC)CCCCNc1ncc2cc(c(NC(=O)NC(C)(C)C)nc2n1)-c3cc(OC)cc(OC)c3

InChI

1S/C28H41N7O3/c1-8-35(9-2)13-11-10-12-29-26-30-18-20-16-23(19-14-21(37-6)17-22(15-19)38-7)25(31-24(20)32-26)33-27(36)34-28(3,4)5/h14-18H,8-13H2,1-7H3,(H3,29,30,31,32,33,34,36)

InChI key

DXCUKNQANPLTEJ-UHFFFAOYSA-N

Gene Information

human ... FGFR1(2260), KDR(3791)
mouse ... Pdgfrb(18596)

Description

Application

PD 173074 has been used:

to treat epithelial-mesenchymal transition (EMT)-induced cell lines in order to study its therapeutic use for head and neck squamous cell carcinoma (HNSCC)
in combination with PD0325901 to test whether an alternative downstream pathway for (fibroblast growth factor) FGF signalling is adopted during human hypoblast induction
to study its potential role in acute lymphoblastic leukaemia (ALL)-derived cell lines (TOM-1 and NALM-20)

Biochem/physiol Actions

PD 173074 is a fibroblast growth factor receptor 3 (FGFR3) inhibitor: IC₅₀ = 5 nM inhibition of FGFR3 autophosphorylation. PD 173074 arrests the G₀/G₁ phase of FGFR3-expressing cells. It is 100-fold more selective for FGFR3 than for VEGF receptors, IGF-1 receptors, and MAPKs.

PD 173074 is a fibroblast growth factor receptor 3 inhibitor.

PD 173074 inhibitor is specific for receptor tyrosine kinases. It competes with adenosine triphosphate (ATP) for its inhibition. PD 173074 prevents the FGF/ vascular endothelial growth factor (VEGF) induced angiogenesis.

Features and Benefits

This compound is a featured product for Kinase Phosphatase Biology research. Click here to discover more featured Kinase Phosphatase Biology products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

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Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

dust mask type N95 (US), Eyeshields, Gloves

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Articles

Naive Pluripotent Stem Cell Culture in Serum-Free Media

Naive pluripotent stem cells cultured in vitro using specialized media and inhibitors mimic "ground-state" cells from blastocysts.

Discover Bioactive Small Molecules for Kinase Phosphatase Biology

Introduction to Bioorganic Chemistry and Chemical Biology, 424-424 (2018)

The FGFR1 inhibitor PD173074 induces mesenchymal--epithelial transition through the transcription factor AP-1

Nguyen PT, et al.

British Journal of Cancer, 109(8), 2248-2248 (2013)

Melanoma: Biologically Targeted Therapeutics, 298-298 (2002)

View All Related Papers

Global Trade Item Number

SKU	GTIN
P2499-5MG	04061832434124
P2499-25MG	04061832434117