Home DNA Damage/DNA Repair G-quadruplex stabilizer Pyridostatin Trifluoroacetate Salt

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Pyridostatin Trifluoroacetate Salt G-quadruplexe Stabilizer

Cat.No.S7444

Pyridostatin Trifluoroacetate Salt is a G-quadruplexe stabilizer with Kd of 490 nM in a cell-free assay, which targets a series of proto-oncogenes.
Pyridostatin Trifluoroacetate Salt G-quadruplex stabilizer Chemical Structure

Chemical Structure

Molecular Weight: 710.7

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability

Quality Control

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MRC5 Cytotoxicity assay 72 hrs Cytotoxicity against human MRC5 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50=5.38μM. 29323491
KB-3-1 qHTS assay P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen 31515284
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight 710.7 Formula

C31H32N8O5·C2HF3O2

 Storage (From the date of receipt)
CAS No. 1472611-44-1 Download SDF Storage of Stock Solutions

Synonyms RR82 Trifluoroacetate Salt Smiles C1=CC=C2C(=C1)C(=CC(=N2)NC(=O)C3=CC(=CC(=N3)C(=O)NC4=NC5=CC=CC=C5C(=C4)OCCN)OCCN)OCCN.C(=O)(C(F)(F)F)O

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (140.7 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 30 mg/mL

Ethanol : 9 mg/mL

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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

mg/kg
g
μL

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
% DMSO
+
%

Calculation results:

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.

Mechanism of Action

Targets/IC50/Ki
G-quadruplexe [1]
(Cell-free assay)
490 nM(Kd)
In vitro

Pyridostatin decreases the proliferation of MRC-5–SV40 cells and various cancer cell lines, and induces cell-cycle arrest by DNA-damage checkpoint activation. Pyridostatin also reduces SRC-dependent cell motility in MDA-MB-231 cells by interacting with G-quadruplex motifs in SRC. [2]

Pyridostatin decreases EBNA1 synthesis via inhibition of G-quadruplexes. [3]
In vivo

References

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