SHP099

Description: SHP099 (SHP099 free base) free base is an effective, selective, orally bioavailable, and efficacious SHP2 inhibitor (IC50 =0.07 µM and p-ERK modulation in cells IC50 = 0.250 µM). SHP099 shows dose-dependent pathway inhibition and antitumor activity in xenograft models. Target: Phosphatase, PERK. Smiles: CC1(N)CCN(CC1)c1cnc(c(N)n1)-c1cccc(Cl)c1Cl. References: LaRochelle JR, Fodor M, Vemulapalli V, Mohseni M, Wang P, Stams T, LaMarche MJ, Chopra R, Acker MG, Blacklow SC. Structural reorganization of SHP2 by oncogenic mutations and implications for oncoprotein resistance to allosteric inhibition. Nat Commun. 2018 Oct 30,9(1):4508. doi: 10.1038/s41467-018-06823-9.