P2499

PD 173074

≥96% (HPLC), 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
• Empirical Formula (Hill Notation): C₂₈H₄₁N₇O₃
• CAS Number: 219580-11-7
• Molecular Weight: 523.67
• MDL number: MFCD08705327
• UNSPSC Code: 12352200
• PubChem Substance ID: 24724575
• NACRES: NA.77

Properties

• 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 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.

Features and Benefits

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Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable
• Personal Protective Equipment: dust mask type N95 (US), Eyeshields, Gloves