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RMC-4550

Chemical Structure : RMC-4550

CAS No.: 2172651-73-7

RMC-4550 (RMC4550)

Catalog No.: PC-35116Not For Human Use, Lab Use Only.

RMC-4550 (RMC4550) is a potent, selective, allosteric inhibitor of SHP2 with IC50 of 0.58 nM (full-length SHP2 enzyme), suppresses pERK signaling in Calu-1 cells with IC50 of 7 nM.

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Purity & Documentation Purity: 98.12% (HPLC) Select Batch:

Biological Activity

RMC-4550 (RMC4550) is a potent, selective, allosteric inhibitor of SHP2 with IC50 of 0.58 nM (full-length SHP2 enzyme), suppresses pERK signaling in Calu-1 cells with IC50 of 7 nM.
RMC-4550 shows no activity against the SHP2 catalytic domain up to 10 uM, RMC-4550 is highly selective for full-length SHP2 across panels comprising 15 other phosphatases, 468 kinases, and 44 cellular targets.
Cancer cell lines bearing missense mutations in KRAS at G12, but neither G13 nor Q61, exhibit sensitivity to RMC-4550 (IC50<2 uM), suppresses growth and RAS/MAPK signaling in cancer cell lines with Class 3 BRAF mutations.
RMC-4550 inhibits tumor growth and RAS/MAPK signaling in xenograft models of KRASG12C-driven cancer.

Physicochemical Properties

M.Wt 437.365
Formula C21H26Cl2N4O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-Pyrazinemethanol, 3-[(3S,4S)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]dec-8-yl]-6-(2,3-dichlorophenyl)-5-methyl-

References

1. Robert J. Nichols, et al. Efficacy of SHP2 phosphatase inhibition in cancers with nucleotide-cycling oncogenic RAS, RAS-GTP dependent oncogenic BRAF and NF1 loss. http://dx.doi.org/10.1101/188730.

2. Nichols RJ, et al. Nat Cell Biol. 2018 Sep;20(9):1064-1073.

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