ChemicalBook > CAS DataBase List > 4-[2-PHENYL-5,7-BIS(TRIFLUOROMETHYL)PYRAZOLO[1,5-A]PYRIMIDIN-3-YL]PHENOL

4-[2-PHENYL-5,7-BIS(TRIFLUOROMETHYL)PYRAZOLO[1,5-A]PYRIMIDIN-3-YL]PHENOL

Product Name
4-[2-PHENYL-5,7-BIS(TRIFLUOROMETHYL)PYRAZOLO[1,5-A]PYRIMIDIN-3-YL]PHENOL
CAS No.
805239-56-9
Chemical Name
4-[2-PHENYL-5,7-BIS(TRIFLUOROMETHYL)PYRAZOLO[1,5-A]PYRIMIDIN-3-YL]PHENOL
Synonyms
PHTPP;4-[2-phenyl-5;PHTPP, 10 mM in DMSO;PHTPP, ERbeta antagonist;5-a]pyrimidin-3-yl]phenol;7-bis(trifluoromethyl)pyrazolo[1;4-[2-PHENYL-5,7-BIS(TRIFLUOROMETHYL)PYRA...;Inhibitor,inhibit,Estrogen Receptor/ERR,PHTPP;4-[2-PHENYL-5,7-BIS(TRIFLUOROMETHYL)PYRAZOLO[1,5-A]PYRIMIDIN-3-YL]PHENOL;Phenol, 4-[2-phenyl-5,7-bis(trifluoromethyl)pyrazolo[1,5-a]pyrimidin-3-yl]-
CBNumber
CB62453433
Molecular Formula
C20H11F6N3O
Formula Weight
423.31
MOL File
805239-56-9.mol
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4-[2-PHENYL-5,7-BIS(TRIFLUOROMETHYL)PYRAZOLO[1,5-A]PYRIMIDIN-3-YL]PHENOL Property

storage temp. 
2-8°C
solubility 
DMSO : 25 mg/mL (59.06 mM; Need ultrasonic)H2O : < 0.1 mg/mL (insoluble)
form 
powder
color 
yellow to orange
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Safety

RIDADR 
UN 2811 6.1 / PGIII
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Danger
Hazard statements

H301Toxic if swalloed

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML1355
Product name
PHTPP
Purity
≥98% (HPLC)
Packaging
5MG
Price
$129
Updated
2023/06/20
Sigma-Aldrich
Product number
SML1355
Product name
PHTPP
Purity
≥98% (HPLC)
Packaging
25MG
Price
$507
Updated
2023/06/20
Cayman Chemical
Product number
16025
Product name
PHTPP
Purity
≥98%
Packaging
5mg
Price
$97
Updated
2024/03/01
Cayman Chemical
Product number
16025
Product name
PHTPP
Purity
≥98%
Packaging
10mg
Price
$184
Updated
2024/03/01
Cayman Chemical
Product number
16025
Product name
PHTPP
Purity
≥98%
Packaging
25mg
Price
$433
Updated
2024/03/01
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4-[2-PHENYL-5,7-BIS(TRIFLUOROMETHYL)PYRAZOLO[1,5-A]PYRIMIDIN-3-YL]PHENOL Chemical Properties,Usage,Production

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

Uses

PHTPP can be used in pharmaceutical combination chemotherapy for treatment of cancer by exploiting estrogen receptor β (ERβ) and TP53 interaction.

Definition

ChEBI: 4-[2-phenyl-5,7-bis(trifluoromethyl)-3-pyrazolo[1,5-a]pyrimidinyl]phenol is a member of pyrazoles and a ring assembly.

Biological Activity

Selective estrogen ER β receptor antagonist that displays 36-fold selectivity over ER α . Exhibits full antagonism at ER β in a cotransfection assay in human endometrial cancer cells (HEC-1), with minimal effects on ER α .

Biochem/physiol Actions

PHTPP is a selective estrogen receptor β (ERβ) full antagonist with 36-fold selectivity for ERβ over ERα. PHTPP has been used to distinguish the various activites of the two estrogen receptors. Estrogen can have opposite effects in some tumors expressing ERα compared to Erβ, with Erα enhancing and Erβ suppressing tumor cell growth. PHTPP, a selective ERβ antagonist, significantly enhanced cell growth in ovarian cancer cell lines SKOV3 and OV2008 that express both receptors.

storage

Room temperature

4-[2-PHENYL-5,7-BIS(TRIFLUOROMETHYL)PYRAZOLO[1,5-A]PYRIMIDIN-3-YL]PHENOL Preparation Products And Raw materials

Raw materials

Preparation Products

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4-[2-PHENYL-5,7-BIS(TRIFLUOROMETHYL)PYRAZOLO[1,5-A]PYRIMIDIN-3-YL]PHENOL Suppliers

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805239-56-9, 4-[2-PHENYL-5,7-BIS(TRIFLUOROMETHYL)PYRAZOLO[1,5-A]PYRIMIDIN-3-YL]PHENOLRelated Search:


  • 4-[2-PHENYL-5,7-BIS(TRIFLUOROMETHYL)PYRAZOLO[1,5-A]PYRIMIDIN-3-YL]PHENOL
  • PHTPP
  • 4-[2-phenyl-5
  • 5-a]pyrimidin-3-yl]phenol
  • 7-bis(trifluoromethyl)pyrazolo[1
  • Phenol, 4-[2-phenyl-5,7-bis(trifluoromethyl)pyrazolo[1,5-a]pyrimidin-3-yl]-
  • 4-[2-PHENYL-5,7-BIS(TRIFLUOROMETHYL)PYRA...
  • Inhibitor,inhibit,Estrogen Receptor/ERR,PHTPP
  • PHTPP, ERbeta antagonist
  • PHTPP, 10 mM in DMSO
  • 805239-56-9
  • C20H11F6N3O