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P2499

PD 173074

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

Synonym(e):

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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Über diesen Artikel

Empirische Formel (Hill-System):
C28H41N7O3
CAS-Nummer:
Molekulargewicht:
523.67
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
Assay:
≥96% (HPLC)
Form:
powder
Quality level:
Preise und Verfügbarkeit sind derzeit nicht verfügbar.
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Produktname

PD 173074, ≥96% (HPLC), powder

Quality Level

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)

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.


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Lagerklasse

11 - Combustible Solids

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WGK 3

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Artikel

Discover Bioactive Small Molecules for Kinase Phosphatase Biology

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


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



Global Trade Item Number

SKUGTIN
P2499-5MG04061832434124
P2499-25MG04061832434117

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