2376136-61-5
2376136-61-5 structure
- Name: MS170
- Chemical Name: MS170
- CAS Number: 2376136-61-5
- Molecular Formula: C45H56ClN9O7
- Molecular Weight: 870.44
- Catalog: Signaling Pathways PI3K/Akt/mTOR Akt
- Create Date: 2022-03-24 13:50:52
- Modify Date: 2024-01-09 17:54:11
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MS170 is a potent and selective PROTAC AKT degrader. MS170 depletes cellular total AKT (T-AKT) with the DC50 value of 32 nM. MS170 binds to AKT1, AKT2, and AKT3 with Kds of 1.3 nM, 77 nM, and 6.5 nM, respectively[1].
| Name | MS170 |
|---|
| Description | MS170 is a potent and selective PROTAC AKT degrader. MS170 depletes cellular total AKT (T-AKT) with the DC50 value of 32 nM. MS170 binds to AKT1, AKT2, and AKT3 with Kds of 1.3 nM, 77 nM, and 6.5 nM, respectively[1]. |
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| Related Catalog | |
| Target |
Akt1:1.3 nM (Kd) Akt2:77 nM (Kd) Akt3:6.5 nM (Kd) CRBN-DDB1 |
| In Vitro | Cereblon (CRBN)-recruiting degrader MS170 is an effective AKT degrader without a ″hook effect″. MS170 selectively induces robust AKT protein degradation, inhibits downstream signaling, and suppresses cancer cell proliferation. MS170 concentration- and time-dependently induces AKT degradation through the ubiquitin-proteasome system (UPS)[1]. MS170 (10 nM-10 μM) effectively inhibits the proliferation in multiple cancer cell lines[1]. MS170 (1 nM-10 μM) concentration-dependently depletes cellular total AKT (T-AKT) with the DC50 value of 32±18 nM[1]. Cell Proliferation Assay[1] Cell Line: BT474, PC3, and MDA-MB-468 cells Concentration: 10 nM, 100 nM, 1 μM, 10 μM Incubation Time: 5 days Result: Inhibited the cell growth with GI50s of 0.7±0.2 μM, 7.4±2.2 μM, and 5.7±2.4 μM for BT474 cells, PC3 cells, and MDA-MB-468 cells, respectively. Western Blot Analysis[1] Cell Line: BT474 cells Concentration: 1 nM, 3 nM, 10 nM, 30 nM, 100 nM, 300 nM, 1 μM , 3 μM, and 10 μM Incubation Time: 24 hours Result: Potently induced AKT degradation. |
| In Vivo | MS170 (a single intraperitoneal injection at a dose of 50 mg/kg) is bioavailable in mice via IP injection[1]. Animal Model: Male Swiss albino mice[1] Dosage: Single 50 mg/kg(Pharmacokinetic Analysis) Administration: IP injection over 8 h Result: Bioavailable in mouse PK studies. The Cmax is1.4 μM at 2 h. |
| References |
| Molecular Formula | C45H56ClN9O7 |
|---|---|
| Molecular Weight | 870.44 |