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PD 173074

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Products Intro: Product Name:PD 173074
CAS:219580-11-7
Purity:98%(Min,HPLC) Package:100g;1kg;5kg,10kg,25kg,50kg
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CAS:219580-11-7
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CAS:219580-11-7
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Products Intro: Product Name:N-[2-[[4-(diethylamino)butyl]amino-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-yl]-N'-(1,1-dimethylethyl)urea
CAS:219580-11-7
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Products Intro: Product Name:PD173074
CAS:219580-11-7
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  • CAS:219580-11-7
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  • 2019-07-06
  • CAS:219580-11-7
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PD 173074 Basic information
Product Name:PD 173074
Synonyms:CS-458;FGF/VEGF Receptor Tyrosine Kinase Inhibitor, PD173074 - CAS 219580-11-7 - Calbiochem;FGF/VEGF Receptor Tyrosine Kinase Inhibitor;PD 173074;PD-173074;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;N-[2-[[4-(diethylaMino)butyl]aMino]-6-(3,5-diMethoxyphenyl)pyrido[2,3-d ]pyriMidin-7-yl]-N'-(1,1-diMethylethyl)-;PD173074/PD-173074;1-(tert-butyl)-3-(2-((4-(diethylaMino)butyl)aMino)-6-(3,5-diMethoxyphenyl)pyrido[2,3-d]pyriMidin-7-yl)urea
CAS:219580-11-7
MF:C28H41N7O3
MW:523.67
EINECS:
Product Categories:Antineoplastic;API;Aromatics;Bases & Related Reagents;Heterocycles;Inhibitors;Intermediates & Fine Chemicals;Nucleotides;Pharmaceuticals
Mol File:219580-11-7.mol
PD 173074 Structure
PD 173074 Chemical Properties
Melting point 82-85°C
density 1.163
storage temp. 2-8°C
solubility DMSO: 21 mg/mL
form solid
pka10.12±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.
InChIKeyDXCUKNQANPLTEJ-UHFFFAOYSA-N
SMILESN(C1=NC2C(C=C1C1=CC(OC)=CC(OC)=C1)=CN=C(NCCCCN(CC)CC)N=2)C(NC(C)(C)C)=O
Safety Information
Hazard Codes Xi
Risk Statements 36/37/38
Safety Statements 26
WGK Germany 3
HS Code 2933599590
Storage Class11 - Combustible Solids
MSDS Information
PD 173074 Usage And Synthesis
DescriptionPD173074 (219580-11-7) is an inhibitor of FGFR tyrosine kinase, and to a lesser extent VEGFR1(IC50values 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 PropertiesYellow Solid
UsesPD173074 is a potent FGFR1 inhibitor with IC50 of ~25 nM and also inhibits VEGFR2 with IC50 of 100-200 nM.
UsesPD 173074 ar signal-related kinase phosphorylation.
UsesA selective FGFR1 and
DefinitionChEBI: 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 ActivitySelective 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 ActionsPD 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 vitropd173074 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].
in vivoin 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] RASHMI BANSAL  Susan W  Suma Magge. 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]. Journal of Neuroscience Research, 2003, 74 4: 486-493. DOI:10.1002/jnr.10773
[2] JUNHO KIM  Teng M. Regulation of autocrine fibroblast growth factor-2 signaling by perfusion flow in 3D human mesenchymal stem cell constructs[J]. Biotechnology Progress, 2012, 28 5: 1384-1388. DOI:10.1002/btpr.1604
[3] LAURE-EMMANUELLE ZARAGOSI  Christian D Ph D  Gérard Ailhaud. Autocrine Fibroblast Growth Factor 2 Signaling Is Critical for Self-Renewal of Human Multipotent Adipose-Derived Stem Cells[J]. STEM CELLS, 2009, 24 11: 2412-2419. DOI:10.1634/stemcells.2006-0006
PD 173074 Preparation Products And Raw materials
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