- CC-401 hydrochloride
- CC-930
- DB07268
- JNK-IN-7
- JNK-IN-8
| AS 602801Jun Kinase Inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
- View current batch:
- Purity = 98.72%
- COA (Certificate Of Analysis)
- HPLC
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
| 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. | |
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| Cas No. | 848344-36-5 | SDF | Download SDF |
| Synonyms | Bentamapimod;AS602801;AS-602801 | ||
| Chemical Name | 2-(benzo[d]thiazol-2-yl)-2-(2-((4-(morpholinomethyl)benzyl)oxy)pyrimidin-4-yl)acetonitrile | ||
| Canonical SMILES | N#CC(C1=NC(OCC2=CC=C(C=C2)CN3CCOCC3)=NC=C1)C4=NC5=CC=CC=C5S4 | ||
| Formula | C25H23N5O2S | M.Wt | 457.55 |
| Solubility | ≥11.45mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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.
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