Thalidomide-NH-C6-NH-Boc

Modify Date: 2024-01-08 16:40:49

Thalidomide-NH-C6-NH-Boc Structure
Thalidomide-NH-C6-NH-Boc structure
Common Name Thalidomide-NH-C6-NH-Boc
CAS Number 2093536-13-9 Molecular Weight 472.53
Density N/A Boiling Point N/A
Molecular Formula C24H32N4O6 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Thalidomide-NH-C6-NH-Boc


Thalidomide-NH-C6-NH-Boc is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used for MI-389 (compound 22) synthesis. MI-389 is a potent phthalimide PROTAC degrader based on the multi-targeted receptor tyrosine kinase inhibitor sunitinib (HY-10255A)[1].

 Names

Name Thalidomide-NH-C6-NH-Boc

 Thalidomide-NH-C6-NH-Boc Biological Activity

Description Thalidomide-NH-C6-NH-Boc is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used for MI-389 (compound 22) synthesis. MI-389 is a potent phthalimide PROTAC degrader based on the multi-targeted receptor tyrosine kinase inhibitor sunitinib (HY-10255A)[1].
Related Catalog
Target

Cereblon

In Vitro MI-389 (0-1 μM; 72 hours) decreases cell growth with an EC50 value of 21.3 nM, which is comparable to the cellular potency of sunitinib (EC50=17.3 nM)[1]. MI-389 (0-500 nM; 72 hours) leads to GSPT1 destabilization fastly as a dosepdependent manner. It shows a complete GSPT1 depletion at 100 nM[1]. Cell Viability Assay[1] Cell Line: Kasumi-1 cells (a c-KIT dependent acute myeloid leukemia (AML) cell line); GIST-T1 Concentration: 0-1 μM Incubation Time: 72 hours Result: Outperform decreased-antiproliferative effect than sunitinib Western Blot Analysis[1] Cell Line: Kasumi-1 cells (a c-KIT dependent acute myeloid leukemia (AML) cell line); GIST-T1 Concentration: 1 nM, 5 nM, 10 nM, 50 nM, 100 nM, 500 nM Incubation Time: 4 hours Result: Decreased GSPT-1 protein expression.
References

[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.

 Chemical & Physical Properties

Molecular Formula C24H32N4O6
Molecular Weight 472.53