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MS170

Catalog No. T39928 CAS 2376136-61-5

MS170 is a highly effective and specific PROTAC AKT degrader compound that exhibits potent activity. It efficiently reduces the levels of total AKT (T-AKT) within cells, with a DC 50 value of 32 nM. Furthermore, MS170 demonstrates strong binding affinity towards AKT isoforms, specifically AKT1, AKT2, and AKT3, with respective dissociation constants (Kd) of 1.3 nM, 77 nM, and 6.5 nM.

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MS170, CAS 2376136-61-5

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5 mg	Inquiry	$ 996.00

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Description	MS170 is a highly effective and specific PROTAC AKT degrader compound that exhibits potent activity. It efficiently reduces the levels of total AKT (T-AKT) within cells, with a DC 50 value of 32 nM. Furthermore, MS170 demonstrates strong binding affinity towards AKT isoforms, specifically AKT1, AKT2, and AKT3, with respective dissociation constants (Kd) of 1.3 nM, 77 nM, and 6.5 nM.
Targets&IC50	Akt3:6.5 nM (Kd), Akt2:77 nM (Kd), Akt1:1.3 nM (Kd)
In vitro	Cereblon (CRBN)-recruiting degrader MS170 is a potent AKT degrader, demonstrating efficacy without exhibiting a hook effect. It selectively degrades AKT proteins, hindering downstream signaling and effectively inhibiting cancer cell growth. MS170 operates in a concentration- and time-dependent manner to degrade AKT via the ubiquitin-proteasome system (UPS)[1], and has been shown to significantly inhibit proliferation across various cancer cell lines at concentrations ranging from 10 nM to 10 μM[1]. Specifically, MS170 depletes total AKT (T-AKT) in a concentration-dependent fashion with a DC50 value of 32±18 nM[1]. In cell proliferation assays using BT474, PC3, and MDA-MB-468 cells, MS170 demonstrated growth inhibition with GI50s of 0.7±0.2 μM, 7.4±2.2 μM, and 5.7±2.4 μM, respectively, over a 5-day incubation period. Western blot analyses further corroborate these findings, showing potent AKT degradation in BT474 cells treated with MS170 across a broad range of concentrations for 24 hours.
In vivo	MS170, administered through a single intraperitoneal (IP) injection at a dosage of 50 mg/kg, demonstrates bioavailability in male Swiss albino mice. Pharmacokinetic analysis reveals that the peak concentration (C max) reaches 1.4 μM at 2 hours post-administration, underscoring its effective distribution within the mouse model over an 8-hour period.

Molecular Weight	870.45
Formula	C45H56ClN9O7
CAS No.	2376136-61-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Yu X, et al. Design, Synthesis, and Evaluation of Potent, Selective, and Bioavailable AKT Kinase Degraders. J Med Chem. 2021;64(24):18054-18081.

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Keywords

MS170 2376136-61-5 MS 170 MS-170 inhibitor inhibit

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