PROTAC c-Met degrader-1

PROTAC c-Met degrader-1 (Compound Met-DD4) is an orally active PROTAC degrader for c-Met with a DC50 of 6.21 nM. PROTAC c-Met degrader-1 inhibits the proliferation of c-Met-addicted cell MKN-45 with an IC50 of 4.37 nM, and arrests the cell cycle at G0/G1 phase. PROTAC c-Met degrader-1 exhibits antitumor efficacy in MKN-45 xenograft mouse models[1]. (Pink: Ligand for target protein (HY-13404) ; Blue: Ligand for E3 ligase (HY-W087383) ; Black: Linker (HY-W074901) )

Product Specifications

CAS Number

[3056647-52-7]

UNSPSC

12352005

Target

C-Met/HGFR; PROTACs

Type

Reference compound

Related Pathways

PROTAC; Protein Tyrosine Kinase/RTK

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/protac-c-met-degrader-1.html

Purity

98.48

Solubility

DMSO : 100 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

FC1=C(C=CC(C(C=N2)=NN3C2=NC=C3CC4=CC5=C(C=C4)N=CC=C5)=C1)C(N6CCC(CN7CCN(C8=CC9=C(C=C8)C(N(C9=O)C(C(N%10)=O)CCC%10=O)=O)CC7)CC6)=O

Molecular Formula

C45H41FN10O5

Molecular Weight

820.87

References & Citations

[1]Ying S, et al., Selective and Orally Bioavailable c-Met PROTACs for the Treatment of c-Met-Addicted Cancer. J Med Chem. 2024 Oct 10;67 (19) :17053-17069.