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Merck
CN

P2499

PD 173074

≥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

Key Documents

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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

Quality Level

100

Gene Information

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

Related Categories

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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Certificates of Analysis (COA)

Lot/Batch Number
0000295949
0000341595
0000295949
0000187284
0000187285

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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)
Anais Julien et al.
Stem cell reports, 15(4), 955-967 (2020-09-12)
Most organs and tissues in the body, including bone, can repair after an injury due to the activation of endogenous adult stem/progenitor cells to replace the damaged tissue. Inherent dysfunctions of the endogenous stem/progenitor cells in skeletal repair disorders are
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)
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