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.
(Pink: Akt ligand (HY-19719); Blue: VHL ligand (HY-112078); Black: linker (HY-128421)).
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 3035638-40-2
- 分子式: C64H79N11O5S
- 分子量:1114.45
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
製品説明
IC50 & Target
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Akt2 90 ± 2.8 nM (IC50) |
Akt3 544 ± 2.9 nM (IC50) |
Akt1 798 ± 190 nM (IC50) |
Cellular Effect
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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] |
体外実験
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. Further protocols information, click here.
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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.
体内実験
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.
化学情報
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CAS 番号 3035638-40-2
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分子量 1114.45
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
MS15 関連分類
HY-151613 関連分類
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