MS15 是一种有效且选择性的AKT PROTAC降解剂。 MS15 可抑制 AKT1、-2 和 -3 活性，IC50值分别为 798 nM、90 nM 和 544 nM。
| 生物活性 | MS15 is a potent and selectiveAKTPROTACdegrader. MS15 inhibits theAKT1, -2, and -3 activities, withIC50values of 798 nM, 90 nM, and 544 nM, respectively[1]. |
| IC50& Target | Akt2 90 ± 2.8 nM (IC50) | Akt3 544 ± 2.9 nM (IC50) | Akt1 798 ± 190 nM (IC50) |
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体外研究
(In Vitro) | 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].
Western Blot Analysis[1] | Cell Line: | SW620 cells, Colo205, HT-29, SKMEL 239, and PANC-1 cells | | Concentration: | 1 nM, 3 nM, 10 nM, 30 nM, 100 nM, 300 nM, 1 μM, 3 μM, 10 μM | | Incubation Time: | 24 h | | Result: | Effectively induced T-AKT degradation in a concentration-dependent manner, with a DC50value 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. |
Cell Proliferation Assay[1] | Cell Line: | SW620 cells | | Concentration: | 0 nM, 30 nM, 100 nM, 1 μM, 3 μM, 10 μM | | Incubation Time: | 5 days | | Result: | Displayed slightly better antiproliferative activity thanMiransertib(HY-19719), with a GI50of 3.1 ± 0.3 μM. |
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体内研究
(In Vivo) | MS15 (75 mg/kg, IP, once) is bioavailable in mice through intraperitoneal administration[1].
| Animal Model: | Male Swiss albino mice[1] | | Dosage: | 75 mg/kg | | Administration: | IP, once (Pharmacokinetic Analysis) | | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
