PD173074 Potent inhibitor of FGF and VEGF (Flt/Flk) receptors

PD173074 (CAS 219580-11-7)

PD173074 | CAS 219580-11-7 is rated 5.0 out of 5 by 1.
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Synonym: FGF/VEGF Receptor Tyrosine Kinase Inhibitor; N-[2-[[4-(Diethylamino)butyl]amino]-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-yl]-N'-(1,1-dimethylethyl)urea
Application: Potent inhibitor of FGF and VEGF (Flt/Flk) receptors
CAS Number: 219580-11-7
Purity: ≥98%
Molecular Weight: 523.67
Molecular Formula: C28H41N7O3
* Refer to Certificate of Analysis for lot specific data (including water content).
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FGF/VEGF Receptor Tyrosine Kinase Inhibitor, PD173074 is a cell-permeable pyridopyrimidine compound that has been shown to act as a potent, ATP-competitive, and reversible inhibitor of FGF and VEGF receptors {IC50 = 21.5 nM for Flg (FGFR1)}. It has been used to inhibit PDGFR and c-Src only at much higher concentration (IC50 = 17.6 μM, 19.8 μM, respectively) and exhibits little effect against EGFR, InsR, MEK, and cPKC even at concentrations as high as 50 μM. It has also been shown to inhibit the autophosphorylation of endogenous Flg (FGFR1, IC50 <5 nM) and overexpressed Flk-1 (VEGFR2, IC50 <200 nM) in NIH3T3 cells in vitro. Inhibition of FGFR signaling impairs angiogenesis as well as self-renewal of stem cells via ERK1/2 activation. Also indicated as an inhibitor of FGFR-3.


References

1. Mohammadi, M., et al. 1998. EMBO J. 17: 5896-5904. PMID: 9774334
2. Skaper, S.D., et al. 2000. J. Neurochem. 75: 1520-1527. PMID: 10987832
3. Trudel, S., et al. 2004. Blood. 103: 3521-3528. PMID: 14715624
4. Koziczak, M., et al. 2004. Oncogene. 23: 3501-3508. PMID: 15116089
5. St Bernard, R., et al. 2005. Endocrinology. 146: 1145-1153. PMID: 15564323
6. Zaragosi, L.E., et al. 2006. Stem Cells. 24: 2412-2419. PMID: 16840552
7. Stavridis, M.P., et al. 2007. Development. 134: 2889-2894. PMID: 17660197
8. Kunath, T., et al. 2007. Development. 134: 2895-2902. PMID: 17660198

Physical State :
Solid
Solubility :
Soluble in DMSO (21 mg/ml), ethanol (100 mM), water (partly miscible), methanol, and chloroform.
Storage :
Store at 4° C
Density :
~1.2 g/cm3 (Predicted)
Refractive Index :
n20D 1.60 (Predicted)
IC50 :
FGFR1: IC50 = 21.5 nM; PDGFR: IC50 = 17.6 µM; c-Src: IC50 = 19.8 µM; autophosphorylation of endogenous FGFR1: IC50 = <5 nM (NIH3T3 cells); overexpressed VEGFR2: IC50 = <200 nM (NIH3T3 cells); Fibroblast growth factor receptor 1: EC5050 = 21 nM (human); Fibroblast growth factor receptor 3: EC5050 = 30 nM (human)
pK Values :
pKa: 10.12 (Predicted), pKb: 10.47 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
1401
MDL Number :
MFCD08705327
SMILES :
CCN(CC)CCCCNC1=NC2=NC(=C(C=C2C=N1)C3=CC(=CC(=C3)OC)OC)NC(=O)NC(C)(C)C

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PD173074  Product Citations

See how others have used PD173074. Click on the entry to view the PubMed entry .

Citations 1 to 6 of 6 total

PMID: # 27514438  Khan, S. et al. 2016. J. Vasc. Surg.

PMID: # 27605627  Olianas, MC. et al. 2016. J. Pharmacol. Exp. Ther. 359: 340-353.

PMID: # 26708711  Oliveira, SM. et al. 2016. Acta Biomater. 32: 129-37.

PMID: # 25542183  Wang, WF. et al. 2015. Endocrine. 49: 385-95.

PMID: # 23690936  Matsuoka, J. et al. 2013. PLoS ONE. 8: e62310.

PMID: # 19903855  Pardo, OE. et al. 2009. Cancer Res. 69: 8645-8651.

Citations 1 to 6 of 6 total
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Rated 5 out of 5 by from Pardo Pardo, OE. et al. (PubMed 19903855) used PD173074, a FGF/VEGF receptor inhibitor, to determine its effect on small cell lung cancer (SCLC) growth. Found that PD173074 blocked H-510 and H-69 SCLC proliferation and clonogenic growth in a dose-dependent fashion and prevented FGF-2 induced chemoresistance. -SCBT Publication Review
Date published: 2015-04-05
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