MS15
MS15 is a potent and selective AKT PROTAC degrader. MS15 inhibits the AKT1, -2, and -3 activities, with IC50 values of 798 nM, 90 nM, and 544 nM, respectively.
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- CAS No.: 3035638-40-2
- Formule: C64H79N11O5S
- Masse moléculaire:1114.45
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
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Akt2 90 ± 2.8 nM (IC50) |
Akt3 544 ± 2.9 nM (IC50) |
Akt1 798 ± 190 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| SW-620 | GI50 |
3.1 μM
Compound: 62; MS15
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Antiproliferative activity against human SW620 cells harboring KRAS mutant assessed as inhibition of cell growth incubated for 5 days by IncuCyte live-cell imaging analysis
Antiproliferative activity against human SW620 cells harboring KRAS mutant assessed as inhibition of cell growth incubated for 5 days by IncuCyte live-cell imaging analysis
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[PMID: 36197750] |
MS15 (0-10 μM, 24 h) potently induces AKT degradation in SW620 cells and MS21-resistant KRAS/BRAF mutant cells[1].
MS15 (0-10 μM, 5 days) inhibits the proliferation of KRAS mutant SW620 cells[1].
MS15 (1 μM, 1-24 h) mediates AKT degradation in a time- and UPS-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SW620 cells, Colo205, HT-29, SKMEL 239, and PANC-1 cells
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Concentration:1 nM, 3 nM, 10 nM, 30 nM, 100 nM, 300 nM, 1 μM, 3 μM, 10 μM
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Incubation Time:24 h
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Result:Effectively induced T-AKT degradation in a concentration-dependent manner, with a DC50 value of 23 ± 16 nM in SW620 cells. Nearly complete AKT degradation was achieved at a concentration of 100 nM in SW620 cells and PANC-1 cells. Induced AKT degradation at 1 μM in BRAF mutant cell lines, such as Colo205, HT-29, and SKMEL 239 cells.
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Cell Line:SW620 cells
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Concentration:0 nM, 30 nM, 100 nM, 1 μM, 3 μM, 10 μM
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Incubation Time:5 days
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Result:Displayed slightly better antiproliferative activity than Miransertib (HY-19719), with a GI50 of 3.1 ± 0.3 μM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Swiss albino mice[1]
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Dosage:75 mg/kg
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Administration:IP, once (Pharmacokinetic Analysis)
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Result:The maximum plasma concentration (Cmax = 1 μM) was achieved at 0.5 h post-treatment, and plasma concentrations were maintained above 100 nM for at least 12 h.Could achieve enough plasma exposure for effective AKT degradation.
Chemical Information
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CAS No. 3035638-40-2
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Masse moléculaire 1114.45
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Formule C64H79N11O5S
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SMILES
NC1(CCC1)C(C=C2)=CC=C2N3C4=NC(C5=CC(CCC(NCCCCCCCCCCC(N[C@H](C(N6C[C@@H](C[C@H]6C(N[C@@H](C)C7=CC=C(C=C7)C8=C(N=CS8)C)=O)O)=O)C(C)(C)C)=O)=O)=CC=C5)=CC=C4N=C3C9=CC=CN=C9N
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MS15 Related Classifications
HY-151613 Related Classifications
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