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AS 602801 Sale

(Synonyms: 本塔马莫,Bentamapimod;AS602801;AS-602801) 目录号 : GC12882

A selective, orally bioavailable JNK inhibitor

AS 602801 Chemical Structure

Cas No.:848344-36-5

规格 价格 库存 购买数量
10mM (in 1mL DMSO) 待询 待询
10mg
¥1,080.00
现货
50mg
¥2,250.00
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200mg 待询 待询
500mg
¥13,500.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

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.

产品描述

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
别名 本塔马莫,Bentamapimod;AS602801;AS-602801
化学名 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
分子式 C25H23N5O2S 分子量 457.55
溶解度 ≥ 11.45mg/mL in DMSO 储存条件 Store at -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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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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