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RMC-5552

Cat. No. M21167
RMC-5552  Structure
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Biological Activity

The selective mTORC1 complex inhibitor RMC-4529 is a bidentate inhibitor that has a rapamycin-derived, FKBP12-induced heterologous mTOR inhibitor covalently linked to an active-site (orthologous) inhibitor.

Chemical Information
Molecular Weight 1778.13
Formula C93H136N10O24
CAS Number 2382768-62-7
Solubility (25°C) DMSO ≥ 100 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] G Leslie Burnett, et al. J Med Chem. Discovery of RMC-5552, a Selective Bi-Steric Inhibitor of mTORC1, for the Treatment of mTORC1-Activated Tumors

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