Home DNA Damage/DNA Repair PARP inhibitor AZD2461

research use only

AZD2461 PARP inhibitor

Cat.No.S7029

AZD2461 is a novel PARP inhibitor with low affinity for Pgp. Phase 1.
AZD2461 PARP inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 395.43

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S702901 DMSO]79 mg/mL]false]Ethanol]31 mg/mL]false]Water]Insoluble]false Purity: 99.89%
99.89

Chemical Information, Storage & Stability

Molecular Weight 395.43 Formula

C22H22FN3O3

 Storage (From the date of receipt)
CAS No. 1174043-16-3 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles COC1CCN(CC1)C(=O)C2=C(C=CC(=C2)CC3=NNC(=O)C4=CC=CC=C43)F

Solubility

In vitro
Batch:

DMSO : 79 mg/mL (199.78 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 31 mg/mL

Water : Insoluble

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
PARP [1]
In vitro

AZD2461 has lower affinity for Pgp. [1]
In vivo

AZD2461 has an 80-fold increased Mdr1b expression on -resistant KB1P tumor T6-28, without inhibition of Pgp. This compound induces loss of 53BP1 expression in mice with KB1P tumors with short-term treatment. Long-term treatment with this chemical is well tolerated and doubled the median relapse-free survival. [1]
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01247168 Completed
Refractory Solid Tumors|Cancer Tumor
AstraZeneca
 November 2010 Phase 1

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.

Frequently Asked Questions

Question 1:
I need to formulate it for in vivo use. How to dissolve this compound for injections?

Answer:
The IP formula of this compound is 3% DMSO+40% PEG+2% Tween-80+H2O, the concentration of which can be up to 5 mg/ml. And you must add solvents to it in order and individually.

Signaling Pathway Map