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

Product Name

PD 173074, ≥96% (HPLC), powder

SMILES string

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

InChI key

DXCUKNQANPLTEJ-UHFFFAOYSA-N

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)

assay

≥96% (HPLC)

form

powder

color

faintly yellow to dark yellow

solubility

DMSO: 10 mg/mL, clear

storage temp.

2-8°C

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 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.

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.

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.

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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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)

Deregulation of FGFR1 and CDK6 oncogenic pathways in acute lymphoblastic leukaemia harbouring epigenetic modifications of the MIR9 family

Rodriguez-Otero P, et al.

British Journal of Haematology, 155(1), 73-83 (2011)

Synthetic heparan sulfate oligosaccharides inhibit endothelial cell functions essential for angiogenesis.

Claire L Cole et al.

PloS one, 5(7), e11644-e11644 (2010-07-27)

Heparan sulfate (HS) is an important regulator of the assembly and activity of various angiogenic signalling complexes. However, the significance of precisely defined HS structures in regulating cytokine-dependent angiogenic cellular functions and signalling through receptors regulating angiogenic responses remains unclear.

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