PROTAC STAT3 degrader-2

Names

[ CAS No. ]:
2429877-78-9

[ Name ]:
PROTAC STAT3 degrader-2

Biological Activity

[Description]:

PROTAC STAT3 degrader-2 is a selective and efficacious PROTAC degrader of STAT3 protein with a DC50 of 3.54 μM in Molm-16 Cell. PROTAC STAT3 degrader-2 has the potential for cancer research[1].

[Related Catalog]:

Signaling Pathways >> Stem Cell/Wnt >> STAT
Research Areas >> Cancer
Signaling Pathways >> JAK/STAT Signaling >> STAT
Signaling Pathways >> PROTAC >> PROTAC

[Target]

STAT3:3.54 μM (ID50)


[In Vitro]

PROTAC STAT3 degrader-2 (compound 27; 4 天) 在 Molm-16 具有细胞生长抑制活性，IC50 为 0.582 μM，对 SU-DHL-1 细胞作用低，IC50>10 μM[1]。 PROTAC STAT3 degrader-2 在高达 5 μM 无法降低 SU-DHL-1 细胞中的 STAT3 和 pSTATSY705 蛋白水平[1]。

[References]

[1]. Haibin Zhou, et al. Structure-Based Discovery of SD-36 as a Potent, Selective, and Efficacious PROTAC Degrader of STAT3 Protein. J Med Chem. 2019 Dec 26;62(24):11280-11300.  

Chemical & Physical Properties

[ Molecular Formula ]:
C59H60F2N9O13P

[ Molecular Weight ]:
1172.13

Related Compounds