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PD173074

Catalog No. T2642 CAS 219580-11-7

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

Pack Size	Availability	Price/USD
5 mg	In stock	$ 36.00
10 mg	In stock	$ 52.00
25 mg	In stock	$ 91.00
50 mg	In stock	$ 143.00
100 mg	In stock	$ 233.00
200 mg	In stock	$ 413.00
500 mg	In stock	$ 689.00
1 mL * 10 mM (in DMSO)	In stock	$ 54.00

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Purity: 98.21%

Purity: 98.15%

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	FGFR1:25 nM, VEGFR2:100 nM-200 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)

Molecular Weight	523.67
Formula	C28H41N7O3
CAS No.	219580-11-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 52.4 mg/mL (100 mM)

DMSO: 52.4 mg/mL (100 mM)

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.

Citations

1. Huang G K, Huang C C, Kang C H, et al.Genetic Interference of FGFR3 Impedes Invasion of Upper Tract Urothelial Carcinoma Cells by Alleviating RAS/MAPK Signal Activity.International Journal of Molecular Sciences.2023, 24(2): 1776.

Related compound libraries

This product is contained In the following compound libraries：

Highly Selective Inhibitor Library Membrane Protein-targeted Compound Library Tyrosine Kinase Inhibitor Library Inhibitor Library Kinase Inhibitor Library Anti-Cancer Active Compound Library JAK-STAT Compound Library Bioactive Compounds Library Max Anti-Lung Cancer Compound Library Apoptosis Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

PD173074 219580-11-7 Angiogenesis Apoptosis JAK/STAT signaling Tyrosine Kinase/Adaptors IGF-1R EGFR VEGFR FGFR Src Inhibitor Fibroblast growth factor receptor PD 173074 Vascular endothelial growth factor receptor inhibit PD-173074 inhibitor

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