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CAS No.: 848344-36-5

Bentamapimod Catalog No. CSN18465

Synonyms: AS 602801;PGL-5001

AS-602801 is an ATP-competitive JNK inhibitor with IC50 of 80 nM, 90 nM, and 230 nM for JNK1, JNK2, and JNK3, respectively.

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生物活性

实验方案

技术信息

生物活性

描述AS602801 is a potent and selective JNK inhibitor for the treatment of inflammatory endometriosis. AS602801 can work as an anticancer stem cell candidate drug. AS602801 at concentration of 2.5, 5 and 7.5μM exhibited cytotoxicity against both serum-cultured non-stem cancer cells and cancer stem cells derived from human pancreatic cancer cell PANC-1, non-small cell lung cancer cell A594, ovarian cancer cell A2780 and glioblastoma GS-Y01 at concentrations that did not decrease the viability of normal human fibroblasts IMR90, as well as caused loss of stem cell marker expression. Also it inhibited the self-renewal and tumor-initiating capacity of cancer stem cells surviving AS602801 treatment. Systemic administration of AS602801 reduced cancer stem cells in established xenograft tumors at a dose and schedule that did not adversely affect the health of the tumor-bearing mice.
作用机制AS-602801 is an ATP competitive JNK inhibitor.^[1]
动物研究
剂量
Mice: 10 mg/kg, 30 mg/kg^[3] (p.o.)

给药途径
p.o.
临床研究

动物研究
剂量	Mice: 10 mg/kg, 30 mg/kg^[3] (p.o.)
给药途径	p.o.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01630252	Endometriosis	Phase 2	Completed	-	Poland ... more >> Prywatna Klinika Połozniczo-Ginekologiczna Sp z o.o. Bialystok, Poland, 15-224 Collapse <<

参考文献

[1] Designing heterocyclic selective kinase inhibitors: from concept to new drug candidates
[2] Okada M, Kuramoto K, et al. The novel JNK inhibitor AS602801 inhibits cancer stem cells in vitro and in vivo. Oncotarget. 2016 May 10;7(19):27021-32.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1856 mL
- 10.9278 mL
- 21.8557 mL
- 5 mM
- 0.4371 mL
- 2.1856 mL
- 4.3711 mL
- 10 mM
- 0.2186 mL
- 1.0928 mL
- 2.1856 mL

技术信息

CAS号

848344-36-5

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H23N5O2S

运输

蓝冰

分子量

457.55

别名

AS 602801;PGL-5001

溶解度

DMSO	11.0 mg/mL (24.0 mM)
Water	insoluble

动物实验配方

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