PHTPP

Catalog No.S8686 Batch:S868601

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Technical Data

Formula

C20H11F6N3O
Molecular Weight 423.31 CAS No. 805239-56-9
Solubility (25°C)* In vitro Ethanol 84 mg/mL (198.43 mM)
DMSO 50 mg/mL (118.11 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description PHTPP is an ERβ selective antagonist with 36-fold selective for ER βover ERα.
Targets
ERβ [1]
(Cell-free)
In vitro PHTPP is fully effective as an ERβ antagonist while exhibiting no significant agonism on ERα or Erβ[1]. Treating cells with PHTPP reduces bladder cancer (BCa) cell growth and invasion, as well as MCM5 expression[2].
In vivo PHTPP can inhibit bladder cancer growth and invasion, resulting in better survival rate in carcinogen N-butyl-N-(4-hydroxybutyl) nitrosamine (BBN)-induced BCa mouse model[2].

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    HEK 293 cells

  • Concentrations

    1 μM and 10 μM

  • Incubation Time

    24 h

  • Method

    HEK 293 cells are incubated in DMEM supplemented with 10% of charcoal-stripped fetal bovine serum for 24 h and then are transfected with Erβ expressing vector (pcDNA3-ERβ), estrogen response element (ERE) firefly luciferase reporter and SV40-driven renilla expressing vector as control for 8 h followed by addition of DMSO, or 10 nM 2,3-bis(4-hydroxyphenyl)-propionitrile (DPN) with different concentrations of PHTPP. After 24 h, cells are lysed with lysis buffer and assayed.
Animal Study:

[2]
  • Animal Models

    Female B6 mice

  • Dosages

    10 μl of 10 mM PHTPP per mouse

  • Administration

    i.p.

Selleck's PHTPP has been cited by 3 publications

Different Susceptibilities of Human Melanoma Cell Lines to G2/M Blockage and Cell Death Activation in Response to the Estrogen Receptor β agonist LY500307 [ J Cancer, 2022, 13(5):1573-1587] PubMed: 35371312
Kamishoyosan (a Japanese traditional herbal formula), which effectively reduces the aggressive biting behavior of male and female mice, and potential regulation through increase of Tph1, Tph2, and Esr2 mRNA levels [ Brain Res, 2021, 1768:147580] PubMed: 34260963
Bisphenol A induces apoptosis through GPER-dependent activation of the ROS/Ca2+-ASK1-JNK pathway in human granulosa cell line KGN [ Ecotoxicol Environ Saf, 2020, 208:111429] PubMed: 33039870

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.