PD 173074

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.
Safety Information
Hazard Codes Xi
Risk Statements 36/37/38
Safety Statements 26
WGK Germany 3
HS Code 2933599590
MSDS Information
PD 173074 Usage And Synthesis
DescriptionPD173074 (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 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
References1 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
PD 173074 Preparation Products And Raw materials
Motesanib BEZ235 (NVP-BEZ235, Dactolisib) 6-HYDROXY-2,5,7,8-TETRAMETHYLCHROMAN-2-CARBOXYLIC ACID Olaparib PLX4032 Verdinexor (KPT-335) 2-[(6-Amino-9H-purin-9-yl)methyl]-5-methyl-3-(2-methylphenyl)-4(3H)-quinazolinone KPT-330 ERK Inhibitor N-[4-[5-(1,3-BENZODIOXOL-5-YL)-3-METHOXY-1H-1,2,4-TRIAZOL-1-YL]PHENYL]-2-(PHENYLTHIO)ACETAMIDE Compound 23 JNJ-10198409 Pictilisib NVP-BGJ398 MK-2206 2HCl (Z)-3-(3-(3,5-bis(trifluoroMethyl)phenyl)-1H-1,2,4-triazol-1-yl)-1-(3,3- AZD-4547 KPT-330, (E)-RN

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