P2499

PD 173074

Name: PD 173074
Brand: SIGMA

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

Sinónimos:

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

Fórmula empírica (notación de Hill):

C₂₈H₄₁N₇O₃

Número CAS:

219580-11-7

Peso molecular:

523.67

UNSPSC Code:

12352200

PubChem Substance ID:

24724575

NACRES:

NA.77

MDL number:

MFCD08705327

Nombre del producto

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.

Clase de almacenamiento

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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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)

FGFR3 in Periosteal Cells Drives Cartilage-to-Bone Transformation in Bone Repair.

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

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)

Screening allergic components of Yejuhua injection using LAD2 cell membrane chromatography model online with high performance liquid chromatography-ion trap-time of flight-mass spectrum system.

Yanni Lv et al.

Journal of chromatography. B, Analytical technologies in the biomedical and life sciences, 1055-1056, 119-124 (2017-05-04)

Yejuhua (YJH) injection is a traditional Chinese medicine (TCM) injection and has a widely application in clinical practice. However, adverse drug reactions (ADRs) caused by YJH injection, majorly manifested as allergic reactions, have been reported. Hence, Effective and practical method

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