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2756323-15-4

2756323-15-4 Structure

2756323-15-4 Structure
IdentificationBack Directory
[Name]

MS934
[CAS]

2756323-15-4
[Synonyms]

MS934
[Molecular Formula]

C52H69F3IN7O6S
[MOL File]

2756323-15-4.mol
[Molecular Weight]

1104.12
Chemical PropertiesBack Directory
[density ]

1.334±0.06 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted)
[form ]

Solid
[pka]

13.974±0.40(predicted)
[color ]

White to off-white
Hazard InformationBack Directory
[Uses]

MS934 is a novel improved VHL-recruiting MEK 1/2 PROTAC degrader. MS934 also degrades CRAF. MS934 can be used for the research of variety of human cancers, such as melanoma, nonsmall cell lung cancer (NSCLC), colorectal cancer, primary brain tumors, and hepatocellular carcinoma (Pink: Target protein ligand (HY-168288); Black: linker (HY-168289); Blue: E3 ligase ligand (HY-112078))[1][2][3].
[in vivo]

MS934 (50 mg/kg, i.p., 2 weeks) and Lapatinib (HY-50898) reduces tumor growth with minimal impact on body weight in mice harboring LS513 xenografts[3].

[IC 50]

CRAF
[References]

[1] Hu J, et al. Potent and Selective Mitogen-Activated Protein Kinase Kinase 1/2 (MEK1/2) Heterobifunctional Small-molecule Degraders. J Med Chem. 2020 Dec 24;63(24):15883-15905. DOI:10.1021/acs.jmedchem.0c01609
[2] Herrera-Montávez C, et al. MEK1/2-Targeting PROTACs Promote the Collateral Degradation of CRAF in KRAS Mutant Cells. bioRxiv, 2023: 2023.06. 15.545136.
[3] Kurimchak AM, et al. The drug efflux pump MDR1 promotes intrinsic and acquired resistance to PROTACs in cancer cells. Sci Signal. 2022 Aug 30;15(749):eabn2707. DOI:10.1126/scisignal.abn2707
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