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PD 173074 [FGFR1; FGFR3; VEGFR2 Inhibitor]

[CAT#: MOD2005ZP116]

FGFR1/ FGFR3 inhibitor. Inhibits oligodendrocyte progenitor proliferation and differentiation.

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Description
FGFR1/FGFR3 inhibitors (IC50 values of 22 and 5 nM, respectively). Inhibit angiogenesis. It also inhibits the proliferation and differentiation of oligodendrocyte precursor cells.
Chemical Name
N-[2-[[4-(Diethylamino)butyl]amino] -6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-y l]-N'-(1,1-dimethylethyl)urea
Modulator Type
Inhibitor
Relevant Disease
Neurological Disorders
Assay Description
PD 173074 inhibits autophosphorylation of FGFR1 in a dose-dependent manner with IC50 ranging from 1-5 nM. PD 173074 is a competitive ATP inhibitor of FGFR1 with an inhibition constant (Ki) of 40 nM [1]. PD 173074 and SU 5402 reduced FGF-2 enhancement of granular neuron survival in a concentration-dependent manner, with IC50 values of 8 nM and 9 μM, respectively. PD 173074 does not inhibit the neurotrophic effect and nerve center action of FGF-2 signaling molecules in cerebellar granule neurons. When tested on FGF-2 treated granule neurons grown on polylysine/laminin, PD 173074 and SU 5402 inhibited neurite outgrowth concentration-dependently with IC50 of 22 nM and 25 μM, respectively [2]. PD173074 effectively antagonized the effect of FGF-2 on the proliferation and differentiation of OL progenitor cells in culture. Mitogen-activated protein kinase (MAPK) activation is a downstream event after FGFR or PDGFR activation. PD173074 is also blocked by PD173074 in OL progenitor cells stimulated by FGF-2 but not stimulated by PDGF [3].
Reference
[1]. Mohammadi M, et al. Crystal structure of an angiogenesis inhibitor bound to the FGF receptor tyrosine kinase domain. EMBO J. 1998 Oct 15;17(20):5896-904.

[2]. Skaper SD, et al. The FGFR1 inhibitor PD 173074 selectively and potently antagonizes FGF-2 neurotrophic and neurotropic effects. J Neurochem. 2000 Oct;75(4):1520-7.

[3]. Bansal R, et al. Specific inhibitor of FGF receptor signaling: FGF-2-mediated effects on proliferation, differentiation, and MAPK activation are inhibited by PD173074 in oligodendrocyte-lineage cells. J Neurosci Res. 2003 Nov 15;74(4):486-93.
Assay Description
PD 173074 (1 mg/kg, i.p.) has a dose-dependent inhibitory effect on FGF-induced neovascularization and angiogenesis in mice [1]. D173074 (25 mg/kg, p.o.) significantly inhibited the growth of tumors in mice [2].
References
[1]. Mohammadi M, et al. Crystal structure of an angiogenesis inhibitor bound to the FGF receptor tyrosine kinase domain. EMBO J. 1998 Oct 15;17(20):5896-904.

[2]. Trudel S, et al. Inhibition of fibroblast growth factor receptor 3 induces differentiation and apoptosis in t(4;14) myeloma. Blood. 2004 May 1;103(9):3521-8.
Molecular Weight
523.67
Form
Powder
Chemical Formula
C28H41N7O3
SMILES
O=C(NC(C)(C)C)NC2=NC1=NC(NCCCCN(CC)CC)=NC=C1C=C2C3=CC(OC)=CC(OC)=C3
Solubility
Soluble in DMSO (100mM) or ethanol (100mM)
IC50
FGFR1-25 nM (IC50); VEGFR2-100 nM (IC50)
CAS NO.
219580-11-7
PubChem Substance ID
1401
Purity
>98%
Storage
Store at +4°C
Shipping
Room Temperature
Handling Advice
For obtaining a higher solubility, please warm the tube at 37 °C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -52°C for several months.
Research Use Only
For research use only
Official Name
FGFR1; FGFR2; VEGFR3
For Research Use Only. Not For Clinical Use.
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