Tinengotinib (TT00420) is an orally active, spectrally selective small molecule kinase inhibitor targeting Aurora A/B ( IC 50 =1.2-3.3 nM), FGFR1/2/3 ( IC 50 =1.5-3.5 nM), VEGFRs , JAK1/2 and CSF1R . Tinengotinib blocks Aurora kinase-mediated cell cycle progression (inducing G2/M arrest), inhibits FGFR/JNK-JUN signaling pathway and activates MEK/ERK -dependent apoptotic pathway. Tinengotinib has the activity of anti-tumor proliferation, inducing apoptosis , inhibiting angiogenesis and regulating tumor microenvironment. Tinengotinib can be used in the study of triple-negative breast cancer (TNBC), gallbladder cancer and tumor immune microenvironment.
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