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MS170

Cat. No. M21435
MS170  Structure
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Biological Activity

MS170 is a potent selective PROTAC AKT depressant. MS170 consumes total AKT (T-AKT) and has a DC50 value of 32 nM. MS170 binds to AKT1, AKT2 and AKT3 with Kd of 1.3 nM, 77 nM and 6.5 nM, respectively.

Chemical Information
Molecular Weight 870.45
Formula C45H56ClN9O7
CAS Number 2376136-61-5
Solubility (25°C) N/A
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] Xufen Yu, et al. J Med Chem. Design, Synthesis, and Evaluation of Potent, Selective, and Bioavailable AKT Kinase Degraders

[2] Laurie S Stevison, et al. Mol Ecol. Divergence population genetic analysis of hybridization between rhesus and cynomolgus macaques

[3] A Fortunato, et al. Mol Ecol. Co-occurrence in nature of different clones of the social amoeba, Dictyostelium discoideum

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