SNX-2112

SNX-2112 is a potent, selective small molecule inhibitor of heat shock protein 90 (Hsp90), a molecular chaperone involved in the maturation and stability of numerous proteins critical for tumor cell survival and proliferation. It competitively binds to the N-terminal ATP-binding site of Hsp90, leading to degradation of client proteins such as HER2 and mutant EGFR, inhibition of downstream signaling pathways including Akt and ERK, induction of cell cycle arrest (G1 or G2/M phase), and apoptosis in various cancer cell lines. SNX-2112 has demonstrated strong anti-tumor activity in vitro and in vivo against multiple solid tumors (including breast cancer) and hematologic malignancies such as multiple myeloma. The orally bioavailable prodrug form is known as SNX-5422. Development was discontinued due to ocular toxicity observed during phase I clinical trials[1][3][5][8].