2353492-68-7

2353492-68-7 structure

Name: SIAIS164018
Chemical Name: SIAIS164018
CAS Number: 2353492-68-7
Molecular Formula: C₄₃H₄₈ClN₁₀O₇P
Molecular Weight: 883.33
Catalog: Signaling Pathways Apoptosis Apoptosis
Create Date: 2022-08-06 12:05:51
Modify Date: 2024-01-10 04:04:27
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].

Name	SIAIS164018

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.

Molecular Formula	C₄₃H₄₈ClN₁₀O₇P
Molecular Weight	883.33