Cat. No. Name Size Price Add Cart
KI0248PD1730745 mg$112
PD17307410 mg$192
PD17307450 mg$752

Chemical Characteristic

Product NamePD173074
CAS No.219580-11-7
Molecular Weight 523.67
FormulaC28H41N7O3
Chemical NameN-[2-[[4-(Diethylamino)butyl]amino]-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-yl]-N'-(1,1-dimethylethyl)urea
SmilesN(C(=O)NC(C)(C)C)c1c(cc2c(nc(nc2)NCCCCN(CC)CC)n1)c1cc(cc(c1)OC)OC
Chemical Structure

Biological activities

PD173074 is an ATP pocket inhibitor that inhibits the tyrosine kinase activities of the FGF and VEGF receptors. PD173074 shows both of high affinity and selectivity for the fibroblast growth factors receptor (FGFR) family, with IC50s of 5, 21.5 and ∼100 nM for FGFR3, FGF-2, FGFR1, respectively. [1] PD 173074 represents a valuable tool for exploring FGF action in the nervous systems. PD173074 concentration- dependently inhibits FGF-2 promotion of granule neuron survival under low-K+/serum-free conditions with IC50 of 12 nM.[1] PD173074 competes with ATP binding located in the intracellular domain of FGFR3, thus can function as a therapeutic for bladder urothelial carcinoma, in association with p27 up-regulation and G1/G0 arrest( 325 nM). Meanwhile, PD173074 inhibits mutated FGFR3- expressing UM-UC-14 and MGHU3 with IC50 of approximately 10 nM. [2] For small cell lung cancer (SCLC), PD173074 blocks H-510 and H-69 SCLC proliferation and clonogenic growth in a dose-dependent fashion and prevents FGF-2??nduced chemoresistance. In H-69 SCLC xenografts, PD173074 significantly impairs tumor growth compared with control, resulting in complete remission and long-term survival beyond 6 months in 50% of the treated animals, whereas all controls sacrifices within 2 months. [3]

Protocols

PD173074 is dissolved in DMSO at a concentration of 20 nM. [2]

References

[1] Stephen D, et al. The FGFR1 Inhibitor PD 173074 Selectively and Potently Antagonizes FGF-2 Neurotrophic and Neurotropic Effects. J. Neyrochem. 2000, 75:1520-1527.
[2] Makito M, et al. 1- tert -Butyl-3-[6-(3,5-dimethoxy-phenyl)-2-(4-diethylamino- butyl amino)-Pyrido [2,3-d] pyrimidin-7-yl]-urea (PD173074), a Selective Tyrosine Kinase Inhibitor of Fibroblast Growth Factor Receptor-3 (FGFR3), Inhibits Cell Proliferation of Bladder Cancer Carrying the FGFR3 Gene Mutation along with Up-Regulation of p27/Kip1 and G1/G0 Arrest. J Pharmacol Exp Ther. 2010, 332: 795??02.
[3] Olivier E, et al. The Fibroblast Growth Factor Receptor Inhibitor PD173074 Blocks Small Cell Lung Cancer Growth In vitro and In vivo. Cancer Res. 2009, 69: 8645-8651.

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