2655656-99-6
Chemical Structure
Zomiradomide
Synonym(s): KT-413
- CAS No.: 2655656-99-6
- Formula:C45H48F3N7O6S
- Molecular Weight:871.97
IUPAC Name: N-(2-((1r,4r)-4-((6-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)ethyl)-2-azaspiro[3.3]heptan-2-yl)methyl)cyclohexyl)-5-(2-hydroxypropan-2-yl)benzo[d]thiazol-6-yl)-6-(trifluoromethyl)picolinamide
InChIKey: WDRJGMSUTPVXDH-KBOGUJPVSA-N
SMILES: O=C(N1C2C(NC(CC2)=O)=O)C3=CC=CC(NCCC(C4)CC4(C5)CN5C[C@H]6CC[C@H](C(SC7=C8)=NC7=CC(C(C)(O)C)=C8NC(C9=CC=CC(C(F)(F)F)=N9)=O)CC6)=C3C1=O
Biological Activity: Zomiradomide (KT-413) is an orally active IRAK4 PROTAC degrader with a DC50 of 6 nM. Zomiradomide inhibits the NF-κB signaling pathway, while its molecular glue function mediates the degradation of Ikaros and Aiolos (with a DC50 of 1 nM for both), activates the IFN-I signaling pathway, and selectively degrades IMiD substrates. Zomiradomide inhibits cancer cell proliferation and tumor growth. Zomiradomide can be used in research related to B-cell non-Hodgkin's lymphoma and diffuse large B-cell lymphoma[1][2][3].
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Zomiradomide | 98.04% | Zomiradomide (KT-413) is an orally active IRAK4 PROTAC degrader with a DC50 of 6 nM. Zomiradomide inhibits the NF-κB signaling pathway, while its molecular glue function mediates the degradation of Ikaros and Aiolos (with a DC50 of 1 nM for both), activates the IFN-I signaling pathway, and selectively degrades IMiD substrates. Zomiradomide inhibits cancer cell proliferation and tumor growth. Zomiradomide can be used in research related to B-cell non-Hodgkin's lymphoma and diffuse large B-cell lymphoma. | ||||||||||||||||||||
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- [1]. Stevens D A, et al. Phase 1 study of KT-413, a targeted protein degrader, in adult patients with relapsed or refractory B-cell non-Hodgkin lymphoma[J]. 2022.
- [2]. Weiss MM, et al. Discovery of KT-413, a Targeted Protein Degrader of IRAK4 and IMiD Substrates Targeting MYD88 Mutant Diffuse Large B-Cell Lymphoma. Journal of medicinal chemistry. 2024 Jul 11;67(13):10548-10566. [Content Brief]
- [3]. Lue J K, et al. PHASE 1 TRIAL OF KT‐413, A DEGRADER OF IRAK4 AND IMID SUBSTRATES, IN ADULT PATIENTS WITH RELAPSED OR REFRACTORY B‐CELL NON‐HODGKIN'S LYMPHOMAS[J]. Hematological Oncology, 2023, 41.
Keywords
