TPX-0046

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. InChI: InChI=1S/C21H21FN6O3/c1-11-6-23-20(29)14-8-25-28-10-17-19(26-18(14)28)27(15-3-2-4-16(15)31-17)9-12-5-13(22)7-24-21(12)30-11/h5,7-8,10-11,15-16H,2-4,6,9H2,1H3,(H,23,29)/t11-,15+,16-/m1/s1. InChIKey: BYYQDEOVMILBQT-XFBWCDHKSA-N. SMILES: O=C(C1=C2N=C3C(O[C@@](CCC4)([H])[C@@]4([H])N3CC(C=C(F)C=N5)=C5O6)=CN2N=C1)NC[C@H]6C