1. PROTAC
    MAPK/ERK Pathway
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  3. MS432

MS432 

Cat. No.: HY-130602
Handling Instructions

MS432 is a first-in-class and highly selective PD0325901-based VHL-recruiting PROTAC degrader for MEK1 and MEK2. MS432 displays good plasma exposure in mice, exhibiting DC50 values of 31 nM and 17 nM for MEK1, MEK2 in HT29 cells respectively.

For research use only. We do not sell to patients.

MS432 Chemical Structure

MS432 Chemical Structure

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Description

MS432 is a first-in-class and highly selective PD0325901-based VHL-recruiting PROTAC degrader for MEK1 and MEK2. MS432 displays good plasma exposure in mice, exhibiting DC50 values of 31 nM and 17 nM for MEK1, MEK2 in HT29 cells respectively[1].

IC50 & Target[1]

MEK1

31 nM (DC50, in HT29 cells)

MEK2

17 nM (DC50, in HT29 cells)

MEK1

31 nM (DC50, in SK-MEL-28 cells)

MEK2

9.3 nM (DC50, in SK-MEL-28 cells)

In Vitro

MS432 (compound 23) is potent in reducing MEK1/2 protein levels in COLO 205 cells (DC50 (MEK1) = 18 ± 7 nM, DC50 (MEK2) = 11 ± 2 nM) and UACC257 cells (DC50 (MEK1) = 56 ± 25 nM, DC50 (MEK2) = 27 ± 19 nM).

Cell Viability Assay[1]

Cell Line: (HT-29, SK-MEL-28, COLO 205 and UACC 257 cell lines.
Concentration: 0-1 μM.
Incubation Time: 72 hours.
Result: Effectively inhibited proliferation of these CRC and melanoma cells in a concentration-dependent manner, with GI50 values ranging from 30 to 200 nM.
In Vivo

MS432 (compound 23) displays good plasma exposure, which is approximately 3 to 20-fold higher than the GI50 values of compound 23 in the tested cancer cell lines[1].

Animal Model: Male Swiss Albino mice[1].
Dosage: 50 mg/kg (Pharmacokinetic Analysis).
Administration: IP
Result: Displays good plasma exposure with the maximum plasma concentration of 1,400 nM detected at 0.5 hour post dosing and plasma concentration of 710 nM at 8 hours post dosing.
Molecular Weight

1076.06

Formula

C₅₀H₆₅F₃IN₇O₆S

SMILES

O=C([[email protected]]1N(C([[email protected]](C(C)(C)C)NC(CCCCCCCCCCNCCCONC(C2=CC=C(F)C(F)=C2NC3=CC=C(I)C=C3F)=O)=O)=O)C[[email protected]](O)C1)N[[email protected]](C4=CC=C(C5=C(C)N=CS5)C=C4)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

MS432MS 432MS-432PROTACMEKProteolysis-targeting chimeraMitogen-activated protein kinase kinaseMAPKKMAP2KHT29SK-MEL-28COLO 205UACC 257ColoncancerVHLInhibitorinhibitorinhibit

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MS432
Cat. No.:
HY-130602
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