PD-161570

• Description :

  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].

• 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.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• Isoform :

  EGFR/ErbB1/HER1; PDGFR; PDGFRβ

• CAS Number :

  [192705-80-9]