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RMC-6272

Cat. No. M29584
RMC-6272 Structure
Synonym:

RM-006

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Biological Activity

RMC-6272 (RM-006) is a bi-steric mTORC1-selective inhibitor. RMC-6272 exhibits potent and selective (> 10-fold) inhibition of mTORC1 over mTORC2. RMC-6272 shows improved inhibition of mTORC1 in comparison to Rapamycin, and induces more cell death in TSC2 null tumors.

Chemical Information
Molecular Weight 1850.22
Formula C95H141FN6O27S
CAS Number 2382769-46-0
Form Solid
Solubility (25°C) DMSO 25 mg/mL (ultrasonic and warming and heat to 60°C)
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] Delong Meng, et al. Oncogene. A bi-steric mTORC1-selective inhibitor overcomes drug resistance in breast cancer

[2] Inci Aksoylu, et al. Res Sq. Translatome analysis of Tuberous Sclerosis Complex-1 patient-derived neural progenitor cells reveal rapamycin-dependent and independent alterations

[3] 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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Keywords: RMC-6272, RM-006 supplier, mTOR, inhibitors, activators


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