| Identification | Back Directory | [Name]
PD 173074 | [CAS]
219580-11-7 | [Synonyms]
CS-458
PD176074
PD-0173074
PD173074, >=98%
PD173074/PD-173074
PD 173074, Free Base
Cholest-5-en-3-ol,(9α)-
PD-173074 FGFR1 FGFR3 inhibitor ab141117
FGF/VEGF Receptor Tyrosine Kinase Inhibitor
FGF/VEGF Receptor Tyrosine Kinase Inhibitor, PD173074
PD 173074;PD-173074;FGF/VEGF RECEPTOR TYROSINE KINASE INHIBITOR
FGF/VEGF Receptor Tyrosine Kinase Inhibitor, PD173074 - CAS 219580-11-7 - Calbiochem
1-(tert-Butyl)-3-(2-((4-(diethylamino)butyl)amino)-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimid
1-(tert-Butyl)-3-(2-((4-(diethylamino)butyl)amino)-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-
1-(tert-butyl)-3-(2-((4-(diethylaMino)butyl)aMino)-6-(3,5-diMethoxyphenyl)pyrido[2,3-d]pyriMidin-7-yl)urea
1-(tert-Butyl)-3-[7-[[4-(diethylamino)butyl]amino]-3-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-2-yl]urea
N-[2-[[4-(diethylaMino)butyl]aMino]-6-(3,5-diMethoxyphenyl)pyrido[2,3-d ]pyriMidin-7-yl]-N'-(1,1-diMethylethyl)-
n-[2-[[4-(diethylamino)butyl]amino-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-yl]-n'-(1,1-dimethylethyl)urea
Urea, N-[2-[[4-(diethylaMino)butyl]aMino]-6-(3,5-diMethoxyphenyl)pyrido[2,3-d]pyriMidin-7-yl]-N'-(1,1-diMethylethyl)-
PD 173074
N-[2-[[4-(Diethylamino)butyl]amino]-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-yl]-N'-(1,1-dimethylethyl)urea
Inhibitor,Fibroblast growth factor receptor,PD173074,Apoptosis,Vascular endothelial growth factor receptor,inhibit,PD 173074,FGFR,PD-173074,VEGFR
N-[2-[[4-(Diethylamino)butyl]amino]-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-yl]-N'-(1,1-dimethylethyl)urea PD 173074 | [Molecular Formula]
C28H41N7O3 | [MDL Number]
MFCD08705327 | [MOL File]
219580-11-7.mol | [Molecular Weight]
523.678 |
| Chemical Properties | Back Directory | [Melting point ]
82-85°C | [density ]
1.163 | [storage temp. ]
2-8°C
| [solubility ]
DMSO: 21 mg/mL
| [form ]
solid
| [pka]
10.12±0.43(Predicted) | [color ]
yellow
| [Stability:]
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. |
| Hazard Information | Back Directory | [Description]
PD173074 (219580-11-7) is an inhibitor of FGFR tyrosine kinase, and to a lesser extent VEGFR1?(IC50?values are 5 nM, 22.5 nM and 100 nM for FGFR1, FGFR3 and VEGFR respectively). Inhibition of FGFR by PD173074 promotes stem cell self renewal.2,3 | [Chemical Properties]
Yellow Solid | [Uses]
A cell-permeable compound that acts as a potent, ATP-competitive, and reversible inhibitor of FGF and VEGF receptors. PD 173074 inhibits PDGFR and c-Src only at much higher concentration. Shown to inhibit the autophosphorylation of endogenous FGFR1 and overexpressed VEGFR2. | [Uses]
A selective FGFR1 and | [Uses]
PD 173074
ar signal-related kinase phosphorylation. | [Uses]
PD173074 is a potent FGFR1 inhibitor with IC50 of ~25 nM and also inhibits VEGFR2 with IC50 of 100-200 nM. | [Definition]
ChEBI: A member of the class of ureas that is 1-tert-butylurea in which one of the hydrogens attached to N3 is substituted by a pyrido[2,3-d]pyrimidin-7-yl group, which is itself substituted at pos
tions 2 and 6 by a 4-(diethylamino)butyl]amino group and a 3,5-dimethoxyphenyl group, respectively. It is a FGF/VEGF receptor tyrosine kinase inhibitor. | [Biological Activity]
Selective FGFR1 and FGFR3 inhibitor (IC 50 values are 5, 21.5, ~100, 17600 and 19800 nM for FGFR3, FGFR1, VEGFR2, PDGFR and c-Src respectively, and > 50000 nM for EGFR, InsR, MEK and PKC). Inhibits VEGF- and FGF-induced angiogenesis in the mouse cornea model of angiogenesis. Inhibits proliferation and differentiation of oligodendrocyte progenitors. | [Biochem/physiol Actions]
PD 173074 is a fibroblast growth factor receptor 3 (FGFR3) inhibitor: IC50 = 5 nM inhibition of FGFR3 autophosphorylation. PD 173074 arrests the G0/G1 phase of FGFR3-expressing cells. It is 100-fold more selective for FGFR3 than for VEGF receptors, IGF-1 receptors, and MAPKs. | [in vitro]
pd173074 was found to block h-510 and h-69 sclc proliferation and clonogenic growth in a dose-dependent fashion and prevent fgf-2-induced chemoresistance as well. these effects correlate with the inhibition of both fgfr1 and fgfr2 transphosphorylation. in addition, pd173074 showed a high degree of selectivity for fgfr tyrosine kinase [2]. | [Enzyme inhibitor]
This pyrido[2,3-d]pyrimidine (FWfree-base = 523.68 g/mol; CAS 219580-11-
7; Solubility: 100 mM in DMSO, 100 mM in ethanol), also known as N-[2-
[[4- (diethylamino) butyl]amino]-6- (3,5-dimethoxyphenyl) pyrido[2,3-
d]pyrimidin-7-yl]-N'- (1,1-dimethylethyl) urea, inhibits the fibroblast growth
factor receptor protein-tyrosine kinase and vascular endothelial growth
factor receptor protein-tyrosine kinase. PD173074 inhibits FGF-2-
mediated effects on proliferation, differentiation, as well as MAPK
activation in oligodendrocyte-lineage cells. It likewise inhibits
fibroblast growth factor receptor-3, inducing differentiation and apoptosis in
t (4;14) myeloma. PD173074 also selectively inhibits fibroblast growth
factor receptor-3 (FGFR3) tyrosine kinase. It inhibits proliferation of
bladder cancer cell carrying the FGFR3 gene mutation along with up-
regulation of p27/Kip1 and G1/G0 arrest. PD173074 blocks small cell
lung cancer growth in vitro and in vivo. | [in vivo]
in the h-510 xenograft mouse model, tumor growth was significanlty improved similar to that seen with single-agent cisplatin administration. accordingly, pd173074 treatment resulted in significanlty prolonged median survival when compared with that of control sham-treated animals. more dramatically, pd173074 also induced complete responses lasting >6 months in 50% of in mice h-69 xenografts [2]. | [storage]
+4°C | [References]
1 Bansal?et al. (2003),?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.,?74?486
2) Kim?et al. (2012),?Regulation of autocrine fibroblast growth factor-2 signaling by perfusion flow in 3D human mesenchymal stem cell constructs; Biotechnol. Prog.,?28?1384
3) Zaragosi?et al. (2006),?Autocrine fibroblast growth factor 2 signaling is critical for self renewal of human multipotent adipose-derived stem cells; Stem Cells,?24?2412 |
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