RMC-5552 | mTORC1 inhibitor | Probechem Biochemicals

Chemical Structure : RMC-5552

RMC-5552 (RMC5552)

Catalog No.: PC-49617Not For Human Use, Lab Use Only.

RMC-5552 (RMC5552) is a potent, selective bi-steric inhibitor of mTORC1 with cellular IC50 of 0.48 nM for p4EBP1 inhibition, 40-fold selectivity over mTORC2.

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Biological Activity

RMC-5552 (RMC5552) is a potent, selective bi-steric inhibitor of mTORC1 with cellular IC50 of 0.48 nM for p4EBP1 inhibition, 40-fold selectivity over mTORC2.
RMC-5552 displays >53-fold selectivity over other lipid kinases.
Treament of RMC-5552 resulted in a dose-dependent, prolonged, and profound inhibition of tumor p4EBP1 levels up to 48 h in Michigan Cancer Foundation-7 (MCF-7) breast cancer cell line, which bears an activating mutation in the p110α catalytic subunit of Phosphoinositide 3-kinase (PIK3CAE545K).
RMC-5552 (10 mg/kg, ip, qw) reduced tumor volume in MCF-7 CDX models.

Physicochemical Properties

M.Wt	1778.16
Formula	C93H136N10O24
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	(1R,2R,4S)-2-Methoxy-4-((R)-2-((3S,5R,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34aS)-5,9,27-trihydroxy-10,21-ddimethoxy-6,8,12,14,20,26-hexamethyl-1,11,28,29-tetraoxo-1,4,5,6,9,10,11,12,13,14,21,22,23,24,25,26,27,28,29,31,32,33,34,34a-tetracosahydro-3H-23,27-epoxypyrido[2,1-c][1]oxa[4]azacyclohentriacontin-3-yl)propyl)cyclohexyl (27-(6-((4-Amino-3-(2-aminobenzo[d]oxazol-5-yl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)methyl)-3,4-dihydroisoquinolin-2(1H)-yl)-27-oxo-3,6,9,12,15,18,21,24-octaoxahept

References

1. G Leslie Burnett, et al. J Med Chem. 2023 Jan 12;66(1):149-169.

RMC-5552 (RMC5552)

Biological Activity

Physicochemical Properties

References

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