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Thalidomide-NH-C6-NH-Boc

Catalog No. T39512 CAS 2093536-13-9

Synonyms: Thalidomide-NH-C6-NH-Boc

Thalidomide-NH-C6-NH-Boc is a synthesized E3 ligase ligand-linker conjugate containing the cereblon ligand derived from Thalidomide and a linker utilized in the synthesis of MI-389 (compound 22). MI-389 is a highly effective phthalimide PROTAC degrader developed from the multi-targeted receptor tyrosine kinase inhibitor sunitinib.

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Thalidomide-NH-C6-NH-Boc Chemical Structure

Thalidomide-NH-C6-NH-Boc, CAS 2093536-13-9

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Description

In vitro

MI-389, at concentrations ranging from 0-1 μM over 72 hours, significantly reduces cell growth with an EC50 of 21.3 nM, showcasing a potency similar to that of sunitinib, which has an EC50 of 17.3 nM[1]. Additionally, MI-389 induces rapid dose-dependent GSPT1 destabilization across a 0-500 nM range, achieving complete depletion at 100 nM[1]. In Kasumi-1 cells, a c-KIT dependent acute myeloid leukemia (AML) cell line, and GIST-T1 cells, MI-389 demonstrates a superior antiproliferative effect compared to sunitinib when tested at 0-1 μM for 72 hours[1]. Western blot analysis reveals that MI-389 decreases GSPT-1 protein expression in a dose-dependent manner within 4 hours across incremental concentrations from 1 nM to 500 nM[1].

Synonyms	Thalidomide-NH-C6-NH-Boc
Molecular Weight	472.542
Formula	C24H32N4O6
CAS No.	2093536-13-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Mette Ishoey, et al. Translation Termination Factor GSPT1 Is a Phenotypically Relevant Off-Target of Heterobifunctional Phthalimide Degraders.ACS Chem Biol. 2018 Mar 16;13(3):553-560.

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Keywords

Thalidomide-NH-C6-NH-Boc 2093536-13-9 Thalidomide NH C6 NH Boc Thalidomide-NH-C-6-NH-Boc ThalidomideNHC6NHBoc inhibitor inhibit

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