er-negative breast cancer

Palbociclib (PD 0332991) is a CDK inhibitor that inhibits CDK4 and CDK6 (IC50=11 16 nM) and is orally active. Palbociclib has anti-tumorigenic activity and has investigational potential for use in ER-positive and HER2-negative breast cancer.

ML179 is a potent and selective inverse agonist of liver receptor homolog-1 (LRH1, NR5A2) with IC50 of 320 nM.

H3B-6545 is a selective estrogen receptor covalent antagonist (SERCA) that is orally available. As a novel class of ERα antagonists, H3B-6545 is used in the study of metastatic breast cancers, such as estrogen receptor-positive (ER), human epidermal growth factor receptor 2-negative (HER2-) breast cancer.

Palbociclib-d8 (PD 0332991 D8) is the 2H-labeled form of Palbociclib. Palbociclib is an orally active CDK inhibitor that inhibits CDK4 and CDK6 (IC50=11 16 nM). Palbociclib has anti-tumor activity and is used in research for estrogen receptor-positive and HER2-negative breast cancer.

ERRα antagonist-2 (Compound 11) is a potential reverse agonist of ERRα (estrogen receptor-related receptor α) with an IC50 of 0.80 μM. It can inhibit the migration and invasion of ER-negative MDA-MB-231 cells and inhibits the growth of breast cancer in vivo.

Downregulate phosphorylation of STAT3, increase the expression of cleaved caspase-3, inhibit cell cycle progression and promote apoptosis in breast and pancreatic cancer cells with low micromolar to nanomolar IC50 values. Furthermore, HJC-0123 significantly suppressed estrogen receptor (ER)-negative breast cancer MDA-MB-231 xenograft tumor growth in vivo (p.o.), indicating its great potential as an efficacious and orally bioavailable drug candidate for human cancer therapy.