Formulation: A solid
Formal Name: N-[3-[(1S)-1-[[6-(3,4-dimethoxyphenyl)-2-pyrazinyl]amino]ethyl]phenyl]-5-methyl-3-pyridinecarboxamide
Purity: ≥98%
Formula Markup: C27H27N5O3
Formula Weight: 469,5
Shelf life (days): 1460
CAS Number: 1619931-27-9
Notes: Seralutinib is an inhibitor of PDGFR, c-Kit, and colony stimulating factor 1 receptor (CSF1R).{65685} It inhibits PDGF-BB-induced phosphorylation of ERK in PDGFRα-dependent H1703 human lung epithelial cells, human pulmonary arterial smooth muscle cells (HPASMCs), which express PDGFRα and PDGFRβ, and human lung fibroblasts (HLFs), which express higher levels of PDGFRβ than PDGFRα (IC50s = 74, 49, and 62 nM, respectively). Seralutinib also inhibits stem cell factor-induced c-Kit autophosphorylation in human pulmonary endothelial cells (HPAECs) and M-CSF-induced CSF1R phosphorylation in human primary differentiated macrophages (IC50s = 7.8 and 14.4 nM, respectively). It inhibits the proliferation of H1703 cells and PDGF-BB-induced HPASMCs and HLFs (IC50s = 32, 33, and 29 nM, respectively). Seralutinib (2.5 mg/kg) prevents increases in pulmonary artery systolic pressure in a rat model of pulmonary arterial hypertension induced by monocrotaline (Item No. 16666) pneumonectomy when administered via passive inhalation.
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