A full antagonist of estrogen ERβ receptors with 36-fold selectivity over ERα (relative binding affinities are 0.01 and 0.36

PHTPP – 5 mg

Brand:
Cayman
CAS:
805239-56-9
Storage:
-20
UN-No:
Non-Hazardous - 2811 / 6.1

PHTPP is a pyrazolo[1,5-α]pyrimidine-based ligand that acts as a full antagonist of estrogen ERβ receptors with 36-fold selectivity over ERα.{28105} It exhibits no significant agonism on ERα or ERβ.{28105} This compound has been used to selectively target ERβ in the study of the opposing effects of hormone therapy on tumors expressing either ER subtype. At 100 pM, PHTPP has been found to enhance SKOV3 and OV2008 ovarian cancer cell growth in in vitro assays.{28106}  

 

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Description

A full antagonist of estrogen ERβ receptors with 36-fold selectivity over ERα (relative binding affinities are 0.01 and 0.36, respectively); enhances SKOV3 and OV2008 ovarian cancer cell growth in in vitro assays at 100 pM

Formal name: 4-[2-phenyl-5,7-bis(trifluoromethyl)pyrazolo[1,5-a]pyrimidin-3-yl]-phenol

Synonyms: 

Molecular weight: 423.3

CAS: 805239-56-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cancer||Research Area|Endocrinology & Metabolism|Hormones & Receptors|Estrogens & Progestins

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