| Identification | Back Directory | [Name]
INDEX NAME NOT YET ASSIGNED | [CAS]
2376137-31-2 | [Synonyms]
MS98
N'-(2-{[(2S)-2-(4-chlorophenyl)-3-{4-[(5R,7R)-7-hydroxy-5-methyl-5H,6H,7H-cyclopenta[d]pyrimidin-4-yl]piperazin-1-yl}-3-oxopropyl]amino}ethyl)-N-[(2S)-1-[(2S,4R)-4-hydroxy-2-{[(1S)-1-[4-(4-methyl-1,3-thiazol-5-yl)phenyl]ethyl]carbamoyl}pyrrolidin-1-yl]-3,3-dimethyl-1-oxobutan-2-yl]dodecanediamide | [Molecular Formula]
C58H81ClN10O7S | [MOL File]
2376137-31-2.mol | [Molecular Weight]
1097.86 |
| Hazard Information | Back Directory | [Uses]
MS98 is a potent and selective PROTAC AKT degrader. MS98 depletes cellular total AKT (T-AKT) with the DC50 value of 78 nM. MS98 binds to AKT1, AKT2, and AKT3 with Kds of 4 nM, 140 nM, and 8.1 nM, respectively[1]. | [in vivo]
MS98 (a single intraperitoneal injection at a dose of 50 mg/kg) is bioavailable in mice via IP injection. The maximum plasma concentration (Cmax) reaches approximately 3.5 μM at 2 h, and the plasma concentrations remains above 3 μM over 8 h[1]. | Animal Model: | Male Swiss albino mice[1] | | Dosage: | Single 50 mg/kg(Pharmacokinetic Analysis) | | Administration: | IP injection over 8 h | | Result: | Bioavailable in mouse PK studies. The Cmax is 3.5 μM at 2 h. |
| [IC 50]
Akt1: 4 nM (); Akt2: 140 nM (); Akt3: 8.1 nM (); VHL | [References]
[1] Yu X, et al. Design, Synthesis, and Evaluation of Potent, Selective, and Bioavailable AKT Kinase Degraders. J Med Chem. 2021;64(24):18054-18081. DOI:10.1021/acs.jmedchem.1c01476 |
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