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. 2022 Dec 19;66(1):149–169. doi: 10.1021/acs.jmedchem.2c01658

Table 8. Preclinical Profile of RMC-5552 38 and RMC-6272 40.

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key data summary RMC-5552 38 RMC-6272 40
molecular weight (g/mol) 1778.2 1850.3
MDA-MB-468 cell p4EBP1 IC50 (nM) 0.48 0.44
mTORC1/2 selectivity in MDA-MB-486 cell assay 40× 27×
selectivity for mTORC1 over other lipid kinases >53× >1000×
cellular kinase panel (∼300) (1 μM) <30% inhibition <30% inhibition
MCF-7 tumor PD: dose proportional duration of >80% p4EBP1 inhibition 24–48 h 24–48 h
in vitro hERG inhibition (10 μM) 16% 6%
Eurofins Safety Screen 44 (10 μM) <5% inhibition (low promiscuity)