PD173074

PD173074 is a potent FGFR1 inhibitor with an IC50 of 25 nM and also inhibits VEGFR2 with an IC50 of 100-200 nM, showing 1000-fold selectivity for FGFR1 over PDGFR and c-Src.

Product Specifications

CAS Number

[219580-11-7]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; FGFR; VEGFR

Type

Reference compound

Related Pathways

Apoptosis; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/PD173074.html

Purity

99.86

Solubility

DMSO : ≥ 100 mg/mL

Smiles

O=C(NC1=NC2=NC(NCCCCN(CC)CC)=NC=C2C=C1C3=CC(OC)=CC(OC)=C3)NC(C)(C)C

Molecular Formula

C28H41N7O3

Molecular Weight

523.67

Precautions

H302, H315, H319, H335

References & Citations

[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.|[4]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.|[5]Mahe M, et al. An FGFR3/MYC positive feedback loop provides new opportunities for targeted therapies in bladder cancers. EMBO Mol Med. 2018 Apr;10 (4) . pii: e8163.|[6]Zheng Y, et al. Inhibition of FGFR Signaling With PD173074 Ameliorates Monocrotaline-induced Pulmonary Arterial Hypertension and Rescues BMPR-II Expression. J Cardiovasc Pharmacol. 2015 Nov;66 (5) :504-14.