RMC-4550

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

RMC-4550 是一种有效的 SHP2 变构抑制剂 (IC50: 0.583 nM)。

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

RMC-4550 is an allosteric inhibitor of SHP2 and stabilizes the auto-inhibited conformation of wild-type SHP2 enzyme, with a mode of inhibition similar to SHP099. Consistent with an allosteric mode of inhibition, 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.

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Metabolic Enzyme/Protease

Phosphatase

S. aureus

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2172651-73-7

437.37

C21H26Cl2N4O2

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (228.64 mM)

C[C@@H]1OCC2(CCN(CC2)c2nc(C)c(nc2CO)-c2cccc(Cl)c2Cl)[C@@H]1N

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(-20℃)

With Ice Pack

≥ 2 years