SIAIS164018

Names

[ Name ]:
SIAIS164018

Biological Activity

[Description]:

SIAIS164018 is a PROTAC-based ALK and EGFR degrader, which is designed from Brigatinib, with IC50 value of 2.5 nM and 6.6 nM for ALK and ALK G1202R, respectively. SIAIS164018 strongly inhibits cancer cells migration and invasion, causes G1 cell cycle arrest and induces apoptosis. SIAIS164018 exhibits better property than Brigatinib[1].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> JAK/STAT Signaling >> EGFR

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> ALK

Signaling Pathways >> PROTAC >> PROTAC

[Target]

IC50: 2.5 nM (ALK), 6.6 nM (ALK G1202R)[1]

[In Vitro]

SIAIS164018 significantly inhibits SR cell proliferation with an IC50 value of 2 nM[1]. SIAIS164018 shows better cell proliferation inhibition than Brigatinib does in ALK (G1202R) over-expressing 293T and EGFR expressing H1975 cell lines with IC50s 21 and 42 nM, respectively[1]. SIAIS164018 (100 nM; 24 or 48 h) induces a significant G1 cell cycle arrest in ALK-negative Calu-1 and MDA-MB-231 cells[1].

[References]

[1]. Ren C, et al. Discovery of a Brigatinib Degrader SIAIS164018 with Destroying Metastasis-Related Oncoproteins and a Reshuffling Kinome Profile. J Med Chem. 2021 Jul 8;64(13):9152-9165.

Chemical & Physical Properties

[ Molecular Formula ]:
C₄₃H₄₈ClN₁₀O₇P

[ Molecular Weight ]:
883.33

Related Compounds

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