mer 29

Triparanol (NSC-65345) interferes with posttranslational modification of Hedgehog signaling molecules as well as the sterol sensing domain of its receptor PTCH1, leading to down-regulation of Hedgehog signaling. Triparanol suppresses human tumor growth and is an antilipemic agent with high ophthalmic toxicity.

Sitravatinib malate is an orally bioavailable receptor inhibitor of tyrosine kinase (RTK) (IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively.) , shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment.

LDC1267 is a excellently specific TAM(Tyro3, Axl and Mer) kinase inhibitor, for Mer( IC50<5 nM), Tyro3(IC50=8 nM), and Axl(IC50=29 nM).

CEP-40783 (RXDX-106) is an effective, specific and orally active AXL/c-Met inhibitor (IC50: 7/12 nM). It also inhibits MER and TYRO3 (IC50: 29/19 nM).