PROTAC BRAF-V600E degrader-2

Names

[ CAS No. ]:
2417296-82-1

[ Name ]:
PROTAC BRAF-V600E degrader-2

Biological Activity

[Description]:

PROTAC BRAF-V600E degrader-2 (compound 12) is a potent BRAF-V600E degrader with Kds of 14.4 nM and 9.5 nM for BRAF and BRAF-V600E, respectively. PROTAC BRAF-V600E degrader-2 selectively degraded the kinase domain of BRAF-V600E but not the wild-type BRAF. PROTAC BRAF-V600E degrader-2 inhibits melanoma cell growth[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> MAPK/ERK Pathway >> Raf
Signaling Pathways >> PROTAC >> PROTAC

[Target]

BRAF-V600E:9.5 nM (Kd)

Braf:14.4 nM (Kd)

Cereblon


[References]

[1]. Xiao-Ran Han, et al. Discovery of Selective Small Molecule Degraders of BRAF-V600E. J Med Chem. 2020 Apr 23;63(8):4069-4080.  

Chemical & Physical Properties

[ Molecular Formula ]:
C42H39F2N7O8S

[ Molecular Weight ]:
839.86

Related Compounds