Pimicotinib is a CSF1R inhibitor with antitumor activity.
IC50&Target
CSF1R
体外研究
The IC50 values of Pimicotinib for KIT and PDGFRA kinases were 76.98 and 1399.21 nM, respectively.
Pimicotinib can strongly inhibit the phosphorylation of CSF1R and the proliferation of bone marrow-derived macrophages at low nanomolar concentrations.
体内研究
Pimicotinib exhibits anti-tumor activity in NCI-H2122 PBMC humanized mice and LLC syngeneic mice, with better efficacy when used in combination with Sotorasib. It can lead to a decrease in the number of immune suppressive tumor associated macrophages, enhanced regulation of the tumor microenvironment related to anti-tumor immunity, and increased infiltration of CD8 T cells.
分子式
C22H24N6O3
分子量
420.46
CAS号
2253123-16-7
运输条件
Room temperature in continental US; may vary elsewhere.