Catadegbrutinib

BGB-16673 (BGB-16673; BTK-IN-29) is an orally active, selectively chimeric degradation activator compound (CDAC), targeting BTK (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].

Product Specifications

CAS Number

[2736508-60-2]

Product Name Alternative

BGB-16673; BTK-IN-29

UNSPSC

12352005

Target

Btk; PROTACs

Type

Reference compound

Related Pathways

PROTAC; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/btk-in-29.html

Purity

99.18

Solubility

DMSO : 125 mg/mL (ultrasonic)

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

Molecular Formula

C47H54N12O4

Molecular Weight

851.01

References & Citations

[1]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.|[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.|[3]Wang H, et al. Bgb-16673, a Selective BTK Degrader, Exhibits Deeper Inhibition of Cancer Cell Signaling Pathways and Better Efficacy in MCL Models[J]. Blood, 2024, 144: 5833.