3117940-39-0
Chemical Structure
TRI-611
- CAS. Nr.: 3117940-39-0
- Formula:C21H16N4O5
- Molecular Weight:404.38
InChIKey: XGNIJIQFXVUHJG-UHFFFAOYSA-N
SMILES: O=C(O1)N(C2CCC(NC2=O)=O)C3=C1C=CC(CC4=NC(C5=CC=CC=C5)=NO4)=C3
Biological Activity: TRI-611 is a brain-penetrant, orally active molecular glue degrader targeting ALK. TRI-611 engages ALK via a distal degron, forms a ternary complex with CRBN, triggers ALK polyubiquitination and degradation, including TKI-resistant ALK fusion proteins. TRI-611 inhibits ALK downstream signaling pathways, induces anti-proliferative effects in ALK-positive cancer cells. TRI-611 induces regression of ALK-positive non-small cell lung cancer tumors in preclinical xenograft models. TRI-611 can be used for the research of ALK-positive non-small cell lung cancer, including TKI-refractory tumors and central nervous system metastases[1][2][3].
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TRI-611 | 99.07% | TRI-611 is a brain-penetrant, orally active molecular glue degrader targeting ALK. TRI-611 engages ALK via a distal degron, forms a ternary complex with CRBN, triggers ALK polyubiquitination and degradation, including TKI-resistant ALK fusion proteins. TRI-611 inhibits ALK downstream signaling pathways, induces anti-proliferative effects in ALK-positive cancer cells. TRI-611 induces regression of ALK-positive non-small cell lung cancer tumors in preclinical xenograft models. TRI-611 can be used for the research of ALK-positive non-small cell lung cancer, including TKI-refractory tumors and central nervous system metastases. | ||||||||||||||||||||
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- [1]. Andrew R. Conery, et al. Abstract 5787: TRI-611, a development stage molecular glue degrader of ALK, promotes the degradation of TKI-resistant ALK fusion proteins and leads to regression of ALK TKI-refractory tumors. Cancer Res (2026) 86 (7_Supplement): 5787.
- [2]. Andrew R. Conery, et al. Abstract 4618: TRI-611, a development stage molecular glue degrader of ALK for the treatment of ALK-positive NSCLC including central nervous system metastases. Cancer Res (2026) 86 (7_Supplement): 4618.
- [3]. Andrew R. Conery, et al. Abstract B064: TRI-611, a selective, CNS-penetrant molecular glue degrader of ALK with anti-tumor activity against preclinical models of ALK-fusion positive non-small cell lung cancer including kinase inhibitor refractory tumors. Mol Cancer Ther (2025) 24 (10_Supplement): B064.
Keywords
