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ChemicalBook--->CAS DataBase List--->2376137-41-4

2376137-41-4

2376137-41-4 Structure

2376137-41-4 Structure
IdentificationBack Directory
[Name]

INDEX NAME NOT YET ASSIGNED
[CAS]

2376137-41-4
[Synonyms]

MS143
MS 143 New
[Molecular Formula]

C59H81ClN12O6S
[MOL File]

2376137-41-4.mol
[Molecular Weight]

1121.87
Chemical PropertiesBack Directory
[density ]

1.259±0.06 g/cm3(Predicted)
[pka]

13.93±0.50(Predicted)
Hazard InformationBack Directory
[Uses]

MS143 is a potent PROTAC AKT degrader (DC50=46 nM and GI50=0.8 μM in PC3 cells). MS143 induces rapid and robust AKT degradation in a concentration- and time-dependent manner via hijacking the ubiquitin-proteasome system. MS143 can suppress cancer cell growth (Pink: AKT ligand (HY-15431); Blue: E3 ligase ligand (HY-125845); Black: linker)[1].
[in vivo]

MS143 (75 mg/kg; i.p., 22 days) drastically inhibits the tumor growth by 92%, also substantially degrades T-AKT and P-AKT, and effectively inhibits the downstream signaling (PRAS40 phosphorylation) in xenograft mice[1].
Pharmacokinetic Parameters of MS143 in male Swiss Albino mice[1].

IP (75 mg/kg)
Cmax (μM)7
Tmax (h)2
AUC0-12 (h·ng/mL)63600
Animal Model:Male immunocompromised NU/J mice (6 weeks old)[1]
Dosage:75 mg/kg
Administration:i.p., 22 days
Result:Drastically inhibited the tumor growth by 92%, also substantially degraded T-AKT and P-AKT, and effectively inhibited the downstream signaling (PRAS40 phosphorylation).
[References]

[1] Yu X, et al. Discovery of Potent, Selective, and In Vivo Efficacious AKT Kinase Protein Degraders via Structure-Activity Relationship Studies. J Med Chem. 2022;65(4):3644-3666. DOI:10.1021/acs.jmedchem.1c02165
2376137-41-4 suppliers list
Company Name: R&D Systems, Inc  
Tel: 18003437475
Website: www.rndsystems.com
Company Name: Henan Inokai New Materials Co., Ltd  
Tel: 13253687330
Website:
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