PHTPP Estrogen/progestogen Receptor antagonist

Cat.No.S8686

PHTPP is an ERβ selective antagonist with 36-fold selective for ER βover ERα.
PHTPP Estrogen/progestogen Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 423.31

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Quality Control

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

Solubility

In vitro
Batch:

Ethanol : 84 mg/mL

DMSO : 50 mg/mL (118.11 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

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In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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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
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Chemical Information, Storage & Stability

Molecular Weight 423.31 Formula

C20H11F6N3O

Storage (From the date of receipt)
CAS No. 805239-56-9 -- Storage of Stock Solutions

Synonyms N/A Smiles C1=CC=C(C=C1)C2=NN3C(=CC(=NC3=C2C4=CC=C(C=C4)O)C(F)(F)F)C(F)(F)F

Mechanism of Action

Targets/IC50/Ki
ERβ
(Cell-free)
In vitro
PHTPP is fully effective as an ERβ antagonist while exhibiting no significant agonism on ERα or Erβ. Treating cells with this compound reduces bladder cancer (BCa) cell growth and invasion, as well as MCM5 expression.
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.
References

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