2093536-13-9
2093536-13-9 structure
- Name: Thalidomide-NH-C6-NH-Boc
- Chemical Name: Thalidomide-NH-C6-NH-Boc
- CAS Number: 2093536-13-9
- Molecular Formula: C24H32N4O6
- Molecular Weight: 472.53
- Catalog: Signaling Pathways PROTAC E3 Ligase Ligand-Linker Conjugate
- Create Date: 2020-06-01 18:30:50
- Modify Date: 2024-01-08 16:40:49
-
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].
| Name | Thalidomide-NH-C6-NH-Boc |
|---|
| 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 |
| Molecular Formula | C24H32N4O6 |
|---|---|
| Molecular Weight | 472.53 |