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).
性状
Solid
IC50 & Target[1][2]
Cereblon
体外研究(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).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. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability Assay
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[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.
溶解度数据
In Vitro: DMSO : 100 mg/mL (211.63 mM; Need ultrasonic)配制储备液
[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.