Description: TPX-0046 is a RET inhibitor designed to overcome resistance to Selpercatinib and Pralsetinib. Target: c-RET, Src. Smiles: FC=1C=C2CN3C=4C(=CN5C(N4)=C(C=N5)C(=O)NC[C@@H](C)OC2=NC1)O[C@]6([C@@]3(CCC6)[H])[H]. References: Repetto M, et al. The return of RET GateKeeper mutations? an in-silico exploratory...

A RET inhibitor (IC50 = 0.26 nM for the wild-type enzyme), selective for RET over a panel of 217 additional kinases but does inhibit 39 tyrosine kinases by > 50% at 26 nM, inhibits the phosphorylation of wild-type RET (IC50 = 21.9 nM) and 15 RET mutants (IC50s = 2.69-108 nM) in Ba/F3 cells. Formulation: A solid....