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RMC-4550

Names

[ CAS No. ]:
2172651-73-7

[ Name ]:
RMC-4550

Biological Activity

[Description]:

RMC-4550 is a potent, selective and allosteric inhibitor of SHP2, with an IC50 of 0.583 nM.

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphatase
Research Areas >> Cancer

[Target]

IC50:0.583 nM (SHP2)[1].


[In Vitro]

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[1].

[References]

[1]. Nichols RJ, et al. RAS nucleotide cycling underlies the SHP2 phosphatase dependence of mutant BRAF-, NF1- and RAS-driven cancers. Nat Cell Biol. 2018 Sep;20(9):1064-1073.


[Related Small Molecules]

SHP099 hydrochloride | LB-100 | Salubrinal | Calyculin A | SF1670 | Stibogluconate sodium | TPI-1 | MSI-1436 lactate | Microcystin-LR | Sodium orthovanadate | GSK 2830371 | PTP1B-IN-2 | Rosiptor | NSC 663284(DA3003-1) | TCS 401

Chemical & Physical Properties

[ Molecular Formula ]:
C21H26Cl2N4O2

[ Molecular Weight ]:
437.36

[ Storage condition ]:
2-8℃


Related Compounds