Platelet-Derived Growth Factor Receptor Tyrosine Kinase Inhibitor

JNJ-10198409 (1) is an ATP competitive platelet-derived growth factor receptor tyrosine kinase inhibitor and inhibits kinases shown in the table below.^1,2) Cao et al. reported the identification of a combination of small molecules that enables reprogramming of human fibroblasts into chemically induced functional cardiomyocytes (ciCMs) that uniformly display contractile properties. 1 is one of their small molecules.³⁾

References

• 1) (6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: Platelet-Derived Growth Factor Receptor Tyrosine Kinase Inhibitors with Broad Antiproliferative Activity against Tumor Cells
  • C. Y. Ho, D. W. Ludovici, et al., J. Med. Chem. 2005, 48, 8163.
• 2) Validation of in vivo pharmacodynamic activity of a novel PDGF receptor tyrosine kinase inhibitor using immunohistochemistry and quantitative image analysis
  • M. R. D'Andrea, J. M. Mei, R. W. Tuman, R. A. Galemmo, D. L. Johnson, Mol. Cancer. Ther. 2005, 4, 1198.
• 3) Conversion of human fibroblasts into functional cardiomyocytes by small molecules
  • N. Cao, Y. Huang, et al., Science 2016, 352, 1216.

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