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SIAIS164018 hydrochloride

Chemical Structure : SIAIS164018 hydrochloride

CAS No.:

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SIAIS164018 hydrochloride

Catalog No.: PC-27488Not For Human Use, Lab Use Only.

SIAIS164018 hydrochloride is a potent, Brigatinib-based PROTAC degrader of multi-kinases ALK, EGFR, FAK, PYK2, PTK6 with IC50 of 2.5 nM and 6.6 nM against ALK and ALK (G1202R), respectively, promotes the ubiquitination and degradation of ALK, EGFR, FAK, PYK2 and PTK6, induces cell cycle arrest at the G1 phase and triggers cell apoptosis.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

SIAIS164018 hydrochloride is a potent, Brigatinib-based PROTAC degrader of multi-kinases ALK, EGFR, FAK, PYK2, PTK6 with IC50 of 2.5 nM and 6.6 nM against ALK and ALK (G1202R), respectively, promotes the ubiquitination and degradation of ALK, EGFR, FAK, PYK2 and PTK6, induces cell cycle arrest at the G1 phase and triggers cell apoptosis.

Physicochemical Properties

M.Wt 919.80
Formula C43H49Cl2N10O7P
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

4-((2-(4-(1-(4-((5-chloro-4-((2-(dimethylphosphoryl)phenyl)amino)pyrimidin-2-yl)amino)-3-methoxyphenyl)piperidin-4-yl)piperazin-1-yl)-2-oxoethyl)amino)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione hydrochloride

References

1. Ren C, et al. J Med Chem. 2021 Jul 8;64(13):9152-9165.

2. Chu D, et al. Bioorg Med Chem. 2026 Mar;134:118521.

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