Home DNA Damage/DNA Repair PARP inhibitor AZD2461 For research use only.

AZD2461

AZD2461 is a novel PARP inhibitor with low affinity for Pgp than Olaparib. Phase 1.

AZD2461 Chemical Structure

AZD2461 Chemical Structure

CAS: 1174043-16-3

Selleck's AZD2461 has been cited by 7 Publications

2 Customer Reviews

Purity & Quality Control

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

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Biological Activity

Description AZD2461 is a novel PARP inhibitor with low affinity for Pgp than Olaparib. Phase 1.
Targets
PARP [1]
In vitro
In vitro AZD2461 has lower affinity for Pgp than does Olaparib. [1]
In Vivo
In vivo AZD2461 has an 80-fold increased Mdr1b expression on Olaparib-resistant KB1P tumor T6-28, without inhibition of Pgp. AZD2461 induces loss of 53BP1 expression in mice with KB1P tumors with short-term treatment. Long-term AZD2461 treatment is well tolerated and doubled the median relapse-free survival. [1]
Animal Research Animal Models Olaparib-resistant tumors from KB1PM1, KB1PM3, and KB1PM4 in female mice
Dosages 100 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01247168 Completed Refractory Solid Tumors|Cancer Tumor AstraZeneca November 2010 Phase 1

Chemical lnformation & Solubility

Molecular Weight 395.43 Formula

C22H22FN3O3
CAS No. 1174043-16-3 SDF Download AZD2461 SDF
Smiles COC1CCN(CC1)C(=O)C2=C(C=CC(=C2)CC3=NNC(=O)C4=CC=CC=C43)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 79 mg/mL ( (199.78 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 31 mg/mL

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

Mass Concentration Volume Molecular Weight

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.

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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Frequently Asked Questions

Question 1:
I need to formulate the drug for in vivo use. How to dissolve the drug for injections?

Answer:
The IP formula of S702901 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 the product in order and individually.

PARP Signaling Pathway Map

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