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TBK1 PROTAC 1

Names

[ CAS No. ]:
2052306-13-3

[ Name ]:
TBK1 PROTAC 1

[Synonym ]:
N-[(3-{4-[3-(4-{[5-Bromo-4-({3-[(cyclobutylcarbonyl)(methyl)amino]propyl}amino)-2-pyrimidinyl]amino}phenoxy)propoxy]butoxy}propoxy)acetyl]-3-methylvalyl-(4R)-4-hydroxy-N-[4-(4-methyl-1,3-thiazol-5-yl)benzyl]prolinamide
Prolinamide, N-[2-[3-[4-[3-[4-[[5-bromo-4-[[3-[(cyclobutylcarbonyl)methylamino]propyl]amino]-2-pyrimidinyl]amino]phenoxy]propoxy]butoxy]propoxy]acetyl]-3-methylvalyl-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-, (4R)-

Biological Activity

[Description]:

A novel potent, selective TBK1 PROTAC with DC50 of 12 nM, selectively degrades TBK1 with excellent selectivity against a related kinase IKKε; a chemical tool to assess TBK1 as a target in mutant K-Ras cancer cells.

[References]

References 1. Crew AP, et al. J Med Chem. 2017 Jul 10. doi: 10.1021/acs.jmedchem.7b00635. View Related Products by Target PROTAC

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Molecular Formula ]:
C53H74BrN9O9S

[ Molecular Weight ]:
1093.179

[ Exact Mass ]:
1091.451294

[ LogP ]:
4.09

[ Index of Refraction ]:
1.604

Related Compounds