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SHP099 is a highly potent (IC50 = 71 nM), selective and orally bioavailable small-molecule SHP2 inhibitor that stabilizes SHP2 in an auto-inhibited conformation. It concurrently binds to the interface of the N-terminal SH2, C-terminal SH2, and protein tyrosine phosphatase domains, thus inhibiting SHP2 activity through an allosteric mechanism. SHP099 suppresses RAS–ERK signaling to inhibit the proliferation of receptor-tyrosine-kinase-driven human cancer cells in vitro and is efficacious in mouse tumour xenograft models (ref. 1). Inhibition of SHP2 by SHP099 also triggers anti-tumor immunity and synergizes with PD-1 blockade (ref. 2).
Catalog NO: CT-SHP099
Synonym: SHP-099
CAS NO: 1801747-11-4 (HCl salt) 1801747-42-1 (free base)
Mol. Formula: C16H19Cl2N5 ∙ 2HCl
MW: 425.1
** 99.9% Pure, in vivo Quality Material. A yellow powder, with multi cycle recrystallizations. Dihydrochloride, validated by a spot-on Quantitative Elemental Analysis. Made for in vivo studies. Bulk Stock!! Same Day Shipping.