PROTAC ERα Degrader-4

PROTAC ERα Degrader-4 (Compound ZD12) is a highly potent and selectivePROTAC ERα degrader (Ki: 5.08 μM) . PROTAC ERα Degrader-4 contains OBHSAs, linker and E3 ligase ligands. PROTAC ERα Degrader-4 shows excellent cell inhibitory and ERα degradation activity against Tamoxifen-sensitive and -resistant ER+ breast cancer (BC) cells and ERα-mutated BC cells. PROTAC ERα Degrader-4 can induce apoptosis and can be used for cancer research.

Product Specifications

CAS Number

[2521299-80-7]

UNSPSC

12352005

Target

Apoptosis; Estrogen Receptor/ERR; PROTACs

Type

Reference compound

Related Pathways

Apoptosis; PROTAC; Vitamin D Related/Nuclear Receptor

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/protac-erα-degrader-4.html

Purity

99.06

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

CC1=C(C2=CC=C(C=C2)[C@@H](NC([C@@H]3C[C@H](CN3C([C@@H](NC(CCCCCOC4=CC=C(C=C4)N(CC(F)(F)F)S(C5C[C@@H]6C(C7=CC=C(C=C7)O)=C([C@H]5O6)C8=CC=C(C=C8)O)(=O)=O)=O)C(C)(C)C)=O)O)=O)C)SC=N1

Molecular Formula

C55H62F3N5O10S2

Molecular Weight

1074.23

References & Citations

[1]Xie B, et.al. Discovery of a Novel Class of PROTACs as Potent and Selective Estrogen Receptor α Degraders to Overcome Endocrine-Resistant Breast Cancer In Vitro and In Vivo. J Med Chem. 2023 May 25;66 (10) :6631-6651.