An estrogen ERβ receptor antagonist
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PHTPP

Item No. 16025

Technical Information
Formal Name
4-[2-phenyl-5,7-bis(trifluoromethyl)pyrazolo[1,5-a]pyrimidin-3-yl]-phenol
CAS Number
805239-56-9
Molecular Formula
C20H11F6N3O
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 50 mg/mlDMSO: 50 mg/mlDMSO:PBS(pH 7.2) (1:3): 0.25 mg/mlEthanol: 30 mg/ml
SMILES
OC(C=C1)=CC=C1C(C(C2=CC=CC=C2)=N3)=C4N3C(C(F)(F)F)=CC(C(F)(F)F)=N4
InChi Code
InChI=1S/C20H11F6N3O/c21-19(22,23)14-10-15(20(24,25)26)29-18(27-14)16(11-6-8-13(30)9-7-11)17(28-29)12-4-2-1-3-5-12/h1-10,30H
InChi Key
AEZPAUSGTAHLOQ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    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.1 It exhibits no significant agonism on ERα or ERβ.1 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.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Compton, D.R., Sheng, S., Carlson, K.E., et alPyrazolo[1,5-a]pyrimidines: Estrogen receptor ligands possessing estrogen receptor β antagonist activity. J. Med. Chem. 47(24), 5872-5893 (2004).

    2. Chan, K.K.L., Leung, T.H.Y., Chan, D.W., et alTargeting estrogen receptor subtypes (ERα and ERβ) with selective ER modulators in ovarian cancer. J. Endocrinol. 221(2), 325-336 (2014).