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AS 602801 (Synonyms: AS-602801)

Catalog No.GC12882

A selective, orally bioavailable JNK inhibitor

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AS 602801 Chemical Structure

Cas No.: 848344-36-5

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10mM (in 1mL DMSO) Please Inquire Please Inquire
200mg
1,00 $US
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10mg
108,00 $US
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50mg
225,00 $US
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500mg
1 350,00 $US
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Kinase experiment [1]:

Kinase assays

Purified kinase domains were incubated with AS602801 at two-fold dilutions over a concentration range of 100 uM to 0.006 uM or with vehicle (0.1% DMSO) in the presence of 10 uM ATP, 2.5 uCi of [γ-32P]ATP and substrate. Reactions were terminated by spotting onto nitrocellulose membranes; membrane was then washed four times to remove unbound radioactivity and dried. Transferred radioactivity was quantitated by phosphorimaging, and IC50 values were calculated by fitting the data to a sigmoidal dose-response.

Cell experiment [2]:

Cell lines

PANC-1, A549, A2780 cell lines

Preparation method

The solubility of this compound in DMSO is >11.5 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

7.5 μM, 3 days

Applications

AS602801 had selective cytotoxic activity against neoplastic cells and had anticancer effects. AS602801 treatment induced three serum-cultured human cancer cell lines (PANC-1, pancreatic cancer; A594, lung cancer; A2780, ovarian cancer) death and accordingly decreased the number of viable cells.

Animal experiment [2]:

Animal models

BALB/cAJcl-nu/nu mice xenograft (PANC-1 CSLCs (primary tumors))

Dosage form

ip, 40 mg/kg daily for 10 consecutive days.

Application

Systemic AS602801 treatment reduced the proportion of tumor-initiating cells within the primary tumors (PANC-1 CSLCs).

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Olusegun Williams, et al. Discovery of dual inhibitors of the immune cell PI3Ks p110δ and p110γ: a prototype for new anti-inflammatory drugs. Chem Biol. 2010 Feb 26; 17(2): 123–134.

[2] Masashi Okada, et al. The novel JNK inhibitor AS602801 inhibits cancer stem cells in vitro and in vivo. Oncotarget. 2016 May 10; 7(19): 27021–27032.

Background

Kinases represent one of the most popular and promising target class in drug discovery. Success in finding new therapeutics will depend on the validation of the kinase chosen with respect to the disease of interest, and on the ability of chemists to design and synthesize inhibitors. AS602801 is a potent and selective JNK inhibitor with therapeutic potential inMS and fibrosis.

In vitro: AS602801 blocked T-lymphocyte proliferation and induced apoptosis. In RRMS CD4t and CD8t cells, AS602801 induced apoptosis genes and expression of surface markers, while in RRMS CD11bt cells it induced expression of innate immunity receptors and co-stimulatory molecules [1].

In vivo: AS602801, the best JNK inhibitors identified so far, were currently evaluated in preclinical studies, based on preliminary promising results in animal model of auto-immune diseases and neuronal apoptosis [1].

Clinical trial: Recently, a phase IIa proof of concept study of the pan-JNK inhibitor bentamapimod (PGL5001, AS602801) for the treatment of inflammatory endometriosis had been terminated.

Reference:
[1] Ferrandi C, Richard F, Tavano P, Hauben E, Barbié V, Gotteland JP, Greco B, Fortunato M, Mariani MF, Furlan R, Comi G, Martino G, Zaratin PF.  Characterization of immune cell subsets during the active phase of multiple sclerosis reveals disease and c-Jun N-terminal kinase pathway biomarkers. Mult Scler. 2011;17(1):43-56.

Chemical Properties

Cas No. 848344-36-5 SDF
Synonymes AS-602801
Chemical Name 2-(1,3-benzothiazol-2-yl)-2-[2-[[4-(morpholin-4-ylmethyl)phenyl]methoxy]pyrimidin-4-yl]acetonitrile
Canonical SMILES C1COCCN1CC2=CC=C(C=C2)COC3=NC=CC(=N3)C(C#N)C4=NC5=CC=CC=C5S4
Formula C25H23N5O2S M.Wt 457.55
Solubility ≥ 11.45mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.1856 mL 10.9278 mL 21.8555 mL
5 mM 0.4371 mL 2.1856 mL 4.3711 mL
10 mM 0.2186 mL 1.0928 mL 2.1856 mL
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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.
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3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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