SNX-2112 (PF-04928473) is a potent, selective Hsp90 inhibitor with binding IC50 of 30 nM for both HSP90α and HSP90β.
SNX-2112 shows weak affinity for Hsp90 family members Grp94 and Trap-1 (IC50=0.8-4.2 uM).
SNX-2112 has properties and potency, including degradation of HER2, mutant EGFR, and other client proteins, inhibition of ERK and Akt activation, and induction of a Rb-dependent G1 arrest with subsequent apoptosis.
SNX-2112 is the orally bioavailbe prodrug SNX-5422, inhibits MM cell growth and prolongs survival in a xenograft murine model.
