2736508-60-2
Chemical Structure
Catadegbrutinib
Synonym(s): BGB-16673; BTK-IN-29
- CAS No.: 2736508-60-2
- Formula:C47H54N12O4
- Molecular Weight:851.01
InChIKey: ZSOLMVZWDSGPDD-SSEXGKCCSA-N
SMILES: CC1=C([C@@H](C)NC(C2=NC(C(C)(C)C)=NO2)=O)C=CC(C3=C4C(NC(C5=CN=C(N6CCN(CC6)CC7CCN(C8=CC=C(N9C(NC(CC9)=O)=O)C=C8)CC7)C=C5)=C4)=NC=N3)=C1
Biological Activity: BGB-16673 (BGB-16673) is an orally active, selective BTK PROTAC degrader (IC50=0.69 nM). BGB-16673 ligates BTK to E3 ubiquitin ligase, causing BTK to undergo polyubiquitination, which is then recognized and degraded by the proteasome, thereby exerting efficient BTK degradation activity. BGB-16673 can be used in the research of B-cell malignancies such as chronic lymphocytic leukemia, small lymphocytic lymphoma, and mantle cell lymphoma[1][2][3].
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Catadegbrutinib | 99.18% | BGB-16673 (BGB-16673) is an orally active, selective BTK PROTAC degrader (IC50=0.69 nM). BGB-16673 ligates BTK to E3 ubiquitin ligase, causing BTK to undergo polyubiquitination, which is then recognized and degraded by the proteasome, thereby exerting efficient BTK degradation activity. BGB-16673 can be used in the research of B-cell malignancies such as chronic lymphocytic leukemia, small lymphocytic lymphoma, and mantle cell lymphoma. | ||||||||||||||||||||
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References
- [1]. Wang H, et al. BGB-16673, a selective BTK degrader, exhibits deeper inhibition of cancer cell signaling pathways and better efficacy in MCL models. Blood, 2024, 144: 5833.
- [2]. Wu Y, et al. Translational modelling to predict human pharmacokinetics and pharmacodynamics of a Bruton's tyrosine kinase-targeted protein degrader BGB-16673. Br J Pharmacol. 2024 Dec;181(24):4973-4987. [Content Brief]
- [3]. Hexiang Wang, et al. Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and methods of use. WO2021219070A1. 2021-11-04.
