PROTAC BTK Degrader-2

Names

[ CAS No. ]:
2250382-66-0

[ Name ]:
PROTAC BTK Degrader-2

Biological Activity

[Description]:

PROTAC BTK Degrader-2 is a potent BTK PROTAC degrader. PROTAC BTK Degrader-2 effectively reduces BTK protein levels[1].

[Related Catalog]:

Research Areas >> Others
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Btk
Signaling Pathways >> PROTAC >> PROTAC

[In Vitro]

PROTAC BTK Degrader-2 (compound 10; 1 µM; 24 h; Ramos 细胞) 促进培养细胞中的 BTK 降解[1]。

[In Vivo]

PROTAC BTK Degrader-2 (compound 10; 0-175 mg/kg; s.c.) 在大鼠体内选择性降解 BTK[1]。 Animal Model: male Wistar Han rats[1] Dosage: 0, 0.35, 35, and 175 mg/kg Administration: subcutaneous injection Result: Degraded BTK in a dose-dependent and tissue-biased manner.

[References]

[1]. Zorba A, et, al. Delineating the role of cooperativity in the design of potent PROTACs for BTK. Proc Natl Acad Sci U S A. 2018 Jul 31;115(31):E7285-E7292.  

Chemical & Physical Properties

[ Molecular Formula ]:
C47H54F2N8O13

[ Molecular Weight ]:
976.97

Related Compounds