MS143
Based on 1 Customer Validation
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: VHL ligand (HY-125845); Black: linker).
Para uso exclusivo en investigación. No vendemos a pacientes.
- No. CAS: 2376137-41-4
- Fòrmula: C59H81ClN12O6S
- Peso molecular:1121.87
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Actividad biológica
AKT
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDA-MB-468 | GI50 |
1 μM
Compound: 20; , MS143
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Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth by measured after 5 days by IncuCyte zoom live cell analysis
Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth by measured after 5 days by IncuCyte zoom live cell analysis
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[PMID: 35119851] |
| PC-3 | GI50 |
0.8 μM
Compound: 20; , MS143
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Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth measured after 5 days by IncuCyte zoom live cell analysis
Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth measured after 5 days by IncuCyte zoom live cell analysis
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[PMID: 35119851] |
MS143 (1 nM-10 μM; 24 hours) induces T-AKT degradation with a concentration-dependent manner in PC3 cells[1].
MS143 (0.1-10 μM;14 days, replenish every 2 days) effectively inhibits colony formation in BT474 cells[1].
MS143 (1 μM; 24 hours) promotes AKT degradation in an E3 ligase- and UPS-dependent manner[1].
MS143 (1 nM-10 μM) can inhibit the cell growth of PC3 cells (GI50=0.8 nM) and MDA-MB-468 cells (GI50=1.0 nM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PC3 cells and MDA-MB-468 cells[1]
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Concentration:1 nM, 10 nM, 100 nM, 1 μM, 10 μM
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Incubation Time:5 days
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Result:Inhibited the cell growth of PC3 cells (GI50=0.8 nM) and MDA-MB-468 cells (GI50=1.0 nM).
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Cell Line:PC3 cells[1]
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Concentration:1 μM
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Incubation Time:24 hours
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Result:Promoted AKT degradation in an E3 ligase- and UPS-dependent manner.
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 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male immunocompromised NU/J mice (6 weeks old)[1]
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Dosage:75 mg/kg
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Administration:i.p., 22 days
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Result:Drastically inhibited the tumor growth by 92%, also substantially degraded T-AKT and P-AKT, and effectively inhibited the downstream signaling (PRAS40 phosphorylation).
Chemical Information
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No. CAS 2376137-41-4
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Appearance Solid
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Peso molecular 1121.87
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Fòrmula C59H81ClN12O6S
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Color White to off-white
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SMILES
O=C(N1[C@@H](C[C@H](C1)O)C(NCC2=CC=C(C3=C(N=CS3)C)C=C2)=O)[C@H](C(C)(C)C)NC(CCCCCCCCCCC(N(CC4)CCN4CC[C@@H](C5=CC=C(C=C5)Cl)NC(C6(CCN(CC6)C7=C8C(NC=C8)=NC=N7)N)=O)=O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Pureza y Documentación
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Ficha de datos (270 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MS143 Related Classifications
HY-143883 Related Classifications
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