Bentamapimod (AS602801)

Catalog No.S8867

For research use only.

Bentamapimod (AS602801) is a novel, orally active JNK inhibitor with IC50 values of 80 nM, 90 nM and 230 nM for JNK1, JNK2 and JNK3 respectively.

Bentamapimod (AS602801) Chemical Structure

CAS No. 848344-36-5

Selleck's Bentamapimod (AS602801) has been cited by 1 Publication

Purity & Quality Control

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Biological Activity

Description Bentamapimod (AS602801) is a novel, orally active JNK inhibitor with IC50 values of 80 nM, 90 nM and 230 nM for JNK1, JNK2 and JNK3 respectively.
Targets
JNK1 [1]
(Cell-free assay)
JNK2 [1]
(Cell-free assay)
JNK3 [1]
(Cell-free assay)
80 nM 90 nM 230 nM
In vitro

In vitro, AS602801 exhibits cytotoxicity against both serum-cultured non-stem cancer cells and cancer stem cells derived from human pancreatic cancer, non-small cell lung cancer, ovarian cancer and glioblastoma at concentrations that does not decrease the viability of normal human fibroblasts. AS602801 also inhibits the self-renewal and tumor-initiating capacity of cancer stem cells surviving AS602801 treatment[2].

Assay
Methods Test Index PMID
Western blot Noch-1 / p-JNK / active caspase-3 27655677
Growth inhibition assay Cell viability 27655677
In vivo

Cancer stem cells in established xenograft tumors are reduced by systemic administration of AS602801 at a dose and schedule that did not adversely affect the health of the tumor-bearing mice[2].

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 24 mg/mL
(52.45 mM)
Water Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 457.55
Formula
C25H23N5O2S
 
CAS No. 848344-36-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1COCCN1CC2=CC=C(C=C2)COC3=NC=CC(=N3)C(C#N)C4=NC5=CC=CC=C5S4

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
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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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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