Name: PHTPP
Brand: Selleck Chemicals
SKU: S8686
Rating: 5 (3 reviews)

PHTPP is an ERβ selective antagonist with 36-fold selective for ER βover ERα.

PHTPP Chemical Structure

CAS: 805239-56-9

Selleck's PHTPP has been cited by 3 publications

Purity & Quality Control

Batch: S868601 Ethanol] 84 mg/mL] false] DMSO] 50 mg/mL] false] Water] Insoluble] false Purity: 99.81%

99.81

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Signaling Pathway

Estrogen/progestogen Receptor Signaling Pathway

Choose Selective Estrogen/progestogen Receptor Inhibitors

Biological Activity

Description

PHTPP is an ERβ selective antagonist with 36-fold selective for ER βover ERα.

Targets

ERβ ^[1]
(Cell-free)

In vitro
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].
Cell Research	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.

In Vivo
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].
Animal Research	Animal Models	Female B6 mice
	Dosages	10 μl of 10 mM PHTPP per mouse
	Administration	i.p.

References

Chemical Information & Solubility

Molecular Weight	423.31	Formula	C₂₀H₁₁F₆N₃O
CAS No.	805239-56-9	SDF	--
Smiles	C1=CC=C(C=C1)C2=NN3C(=CC(=NC3=C2C4=CC=C(C=C4)O)C(F)(F)F)C(F)(F)F
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

Ethanol : 84 mg/mL

DMSO : 50 mg/mL ( (118.11 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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