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PD173074

Catalog No. T2642   CAS 219580-11-7
Synonyms: Inhibitor, Fibroblast growth factor receptor, PD173074, Apoptosis, Vascular endothelial growth factor receptor, inhibit, PD 173074, FGFR, PD-173074, VEGFR

PD173074 is an effective FGFR1 inhibitor (IC50: 25 nM) and also inhibits VEGFR2 (IC50: 100-200 nM) in cell-free assays. The selectivity is higher ~1000-fold for FGFR1 than PDGFR and c-Src.

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PD173074, CAS 219580-11-7
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Purity: 98%
Biological Description
Chemical Properties
Storage & Solubility Information
Description PD173074 is an effective FGFR1 inhibitor (IC50: 25 nM) and also inhibits VEGFR2 (IC50: 100-200 nM) in cell-free assays. The selectivity is higher ~1000-fold for FGFR1 than PDGFR and c-Src.
Targets&IC50 VEGFR2:100 nM-200 nM, FGFR1:25 nM
Kinase Assay In vitro kinase inhibition assays: Assays using the full-length FGFR-1 kinase are performed in a total volume of 100 μL containing 25 mM HEPES buffer (pH 7.4), 150 mM NaCl, 10 mM MnCl2, 0.2 mM sodium orthovanadate, 750 μg/mL concentration of a random copolymer of glutamic acid and tyrosine (4:1), various concentrations of PD173074 and 60 to 75 ng of enzyme. The reaction is initiated by the addition of [γ-32P]ATP (5 μM ATP containing 0.4 μCi of [γ-32P]ATP per incubation), and samples are incubated at 25°C for 10 minutes. The reaction is terminated by the addition of 30% trichloroacetic acid and the precipitation of material onto glass-fiber filter mats. Filters are washed three times with 15% trichloroacetic acid, and the incorporation of [32P] into the glutamate tyrosine polymer substrate is determined by counting the radioactivity retained on the filters in a Wallac 1250 betaplate reader. Nonspecific activity is defined as radioactivity retained on the filters following incubation of samples without enzyme. Specific activity is determined as total activity (enzyme plus buffer) minus nonspecific activity. The concentration of PD173074 that inhibits FGFR-1 enzymatic activity by 50% (IC50) is determined graphically.
Cell Research Cells are incubated with increasing concentrations of PD173074 in the presence of aFGF/heparin for 48 hours. The percentage of viable cells is determined by MTT.(Only for Reference)
Synonyms Inhibitor, Fibroblast growth factor receptor, PD173074, Apoptosis, Vascular endothelial growth factor receptor, inhibit, PD 173074, FGFR, PD-173074, VEGFR
Molecular Weight 523.682
Formula C28H41N7O3
CAS No. 219580-11-7

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

Ethanol: 52.4 mg/mL (100 mM)

DMSO: 52.4 mg/mL (100 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Mohammadi M, et al. EMBO J, 1998, 17(20), 5896-5904. 2. Skaper SD, et al. J Neurochem, 2000, 75(4), 1520-1527. 3. Bansal R, et al. J Neurosci Res, 2003, 74(4), 486-493. 4. Trudel S, et al. Blood, 2004, 103(9), 3521-3528. 5. Pardo OE, et al. Cancer Res, 2009, 69(22), 8645-8651. 6. Zheng Y, et al. Inhibition of FGFR Signaling With PD173074 Ameliorates Monocrotaline-induced Pulmonary Arterial Hypertension and Rescues BMPR-II Expression. J Cardiovasc Pharmacol. 2015 Nov;66(5):504-14. 7. Mahe M, et al. An FGFR3/MYC positive feedback loop provides new opportunities for targeted therapies in bladder cancers. EMBO Mol Med. 2018 Apr;10(4). pii: e8163.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Compound Library Preclinical Compound Library Anti-Lung Cancer Compound Library HIF-1 Signaling Pathway Compound Library Glycometabolism Compound Library Anti-Cancer Metabolism Compound Library Cytokine Inhibitor Library Anti-Obesity Compound Library Anti-Pancreatic Cancer Compound Library Inhibitor Library

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