RMC-4550 是选择性的蛋白酪氨酸磷酸酶 2 的变构抑制剂，其IC50=0.583 nM。

RMC-4550 is an effective and allosteric inhibitor of SHP2 (IC50: 0.583 nM).

RMC-4550 stabilizes the auto-inhibited conformation of wild-type SHP2 enzyme, with a mode of inhibition similar to SHP099. RMC-4550 inhibits the activity of full-length wild-type SHP2 enzyme activated by a di-phosphotyrosine peptide but lacks activity against the free catalytic domain of SHP2 [1].

RMC-4550 has moderate to high bioavailability and has a half-life amenable for once daily oral administration. In the EGFR-driven KYSE-520 human esophageal cancer xenograft model, RMC-4550 has a dose dependent efficacy consistent with target modulation, assessed by phospho-ERK inhibition in tumors. RMC-4550 is well tolerated at doses that achieved maximal and sustained efficacy in this model[2].

2172651-73-7

C21H26Cl2N4O2

437.36

DMSO:260 mg/mL (571.61 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years