PD-161570

PD-161570 is a potent and ATP-competitive human FGF-1 receptor inhibitor with an IC50 of 39.9 nM and a Ki of 42 nM. PD-161570 also inhibits the PDGFR, EGFR and c-Src tyrosine kinases with IC50 values of 310 nM, 240 nM, and 44 nM, respectively. PD-161570 inhibits PDGF-stimulated autophosphorylation and FGF-1 receptor phosphorylation with IC50s of 450 nM and 622 nM, respectively[1][2]. PD-161570 is also a bone morphogenetic proteins (BMPs) and TGF-β signaling inhibitor[3].

Product Specifications

CAS Number

[192705-80-9]

UNSPSC

12352005

Hazard Statement

H301, H315, H319, H335

Target

EGFR; FGFR; PDGFR; Src; TGF-β Receptor

Type

Reference compound

Related Pathways

JAK/STAT Signaling; Protein Tyrosine Kinase/RTK; TGF-beta/Smad

Applications

Cancer-Kinase/protease

Field of Research

Cancer; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/pd-161570.html

Purity

99.82

Solubility

DMSO : 33.33 mg/mL (ultrasonic)

Smiles

O=C(NC(C)(C)C)NC1=NC2=NC(NCCCCN(CC)CC)=NC=C2C=C1C3=C(Cl)C=CC=C3Cl

Molecular Formula

C26H35Cl2N7O

Molecular Weight

532.51

Precautions

H301, H315, H319, H335

References & Citations

[1]Hamby JM, et al. Structure-activity relationships for a novel series of pyrido[2,3-d]pyrimidine tyrosine kinase inhibitors. J Med Chem. 1997 Jul 18;40 (15) :2296-303.|[2]Batley BL, et al. Inhibition of FGF-1 receptor tyrosine kinase activity by PD 161570, a new protein-tyrosine kinase inhibitor. Life Sci. 1998;62 (2) :143-50.|[3]Wolfe A, et al. Pharmacologic characterization of a kinetic in vitro human co-culture angiogenesis model using clinically relevant compounds. J Biomol Screen. 2013 Dec;18 (10) :1234-45.|[4]Kyosuke Hino, et al. An mTOR Signaling Modulator Suppressed Heterotopic Ossification of Fibrodysplasia Ossificans Progressiva. Stem Cell Reports. 2018 Nov 13;11 (5) :1106-1119.