PD173074 CAS: 219580-11-7
MF: C28H41N7O3
MW: 523.67
Potent inhibitor of FGF and VEGF (Flt/Flk) receptors.

PD173074 (CAS 219580-11-7)

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Noms alternatifs: 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: PD173074 is Potent inhibitor of FGF and VEGF (Flt/Flk) receptors
Numéro CAS: 219580-11-7
Pureté: ≥98%
Masse Moléculaire: 523.67
Formule Moléculaire: C28H41N7O3
Pour la Recherche Uniquement. Non conforme pour le Diagnostic ou pour une Utilisation Thérapeutique.
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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.


Références

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

État Physique :
Solid
Solubilité :
Soluble in DMSO (21 mg/ml), ethanol (100 mM), water (partly miscible), methanol, and chloroform.
STOCKAGE :
Store at 4° C
Densité :
~1.2 g/cm3 (Predicted)
Indice de Réfraction :
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)
Valeurs pK :
pKa: 10.12 (Predicted), pKb: 10.47 (Predicted)
Pour la Recherche Uniquement. Non conforme pour le Diagnostic ou pour une Utilisation Thérapeutique.
WGK Allemagne :
3
PubChem CID :
Numéro MDL :
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 (CAS 219580-11-7)  Références bibliographiques

Consultez les publications faisant référence à l' utilisation de PD173074 (CAS 219580-11-7). Cliquez sur le lien pour afficher lentrée PubMed .

Citations 1 à 10 sur un total de 14

PMID: # 33794254  Olianas, MC.|Dedoni, S.|Onali, P.| et al. 2021. Life Sci. 276: 119407.

PMID: # 30840161  Olianas, MC.|Dedoni, S.|Onali, P.| et al. 2019. Apoptosis.

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

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

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

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

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

PMID: # 31399472  Sikora, MJ.|Strumba, V.|Lippman, ME.|Johnson, MD.|Rae, JM.| et al. 2012. Development. 134: 1027-39.

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

PMID: # 28965199  Inflammation. 73-80.

Citations 1 à 10 sur un total de 14
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