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Bentamapimod (AS602801) JNK inhibitor

Name: Bentamapimod (AS602801)
Brand: Selleck Chemicals
SKU: S8867
Availability: InStock
Rating: 5 (2 reviews)

Cat.No.S8867

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.

Chemical Structure

Molecular Weight: 457.55

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

Quality Control

Batch: S886701 DMSO]24 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.8%

99.8

Related Targets	Ras ERK p38 MAPK Raf MEK S6 Kinase MAP4K TAK1 Mixed Lineage Kinase ASK MNK MAPKAPK2 KLF TOPK
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Chemical Information, Storage & Stability

Molecular Weight	457.55	Formula	C₂₅H₂₃N₅O₂S	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	848344-36-5	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1COCCN1CC2=CC=C(C=C2)COC3=NC=CC(=N3)C(C#N)C4=NC5=CC=CC=C5S4

Solubility

In vitro
Batch:

DMSO : 24 mg/mL (52.45 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.4mg/ml (0.87mM)	Taking the 1 mL working solution as an example, add 50 μL of 8 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.1mg/ml (0.22mM)	Taking the 1 mL working solution as an example, add 50 μL of 2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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	JNK1 ^[1] (Cell-free assay) 80 nM JNK2 ^[1] (Cell-free assay) 90 nM JNK3 ^[1] (Cell-free assay) 230 nM
In vitro	AS602801 (Bentamapimod) exhibits cytotoxicity in vitro 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 do not decrease the viability of normal human fibroblasts. It also inhibits the self-renewal and tumor-initiating capacity of cancer stem cells surviving treatment with this compound^[2].
In vivo	Systemic administration of Bentamapimod (AS602801) at a dose and schedule that did not adversely affect the health of the tumor-bearing mice reduced cancer stem cells in established xenograft tumors^[2].
References	[1] https://pubmed.ncbi.nlm.nih.gov/29267206/ [2] https://pubmed.ncbi.nlm.nih.gov/27027242/

Applications

Methods	Biomarkers	Images	PMID
Western blot	Noch-1 / p-JNK / active caspase-3		27655677
Growth inhibition assay	Cell viability		27655677

Tech Support

Handling Instructions

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