|2-((4-(苯并[d]噻唑-5-基氨基)-6-(叔丁基磺酰基)喹唑啉-7-基)氧基)乙基磷酸二氢酯|CsnPharm

CAS No.: 1579965-12-0

GSK2983559 free acid Catalog No. CSN25270

Synonyms: RIP2 kinase inhibitor 1;RIPK2-IN-1;RIPK2 inhibitor 3

GSK2983559 free acid is a small-molecule inhibitor of RIP2 kinase. GSK2983559 free acid potently binds to RIP2 kinase with good kinase specificity and has excellent activity in blocking many proinflammatory cytokine responses in vivo .

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Receptor-interacting-protein kinase 2 (RIP2) has been identified as a key signal transduction partner in the nucleotide oligomerization domain 2 (NOD2) pathway contributing to a variety of human pathologies, including immune-mediated inflammatory diseases. GSK2983559 is the first RIP2 kinase inhibitor to enter clinical trials, currently under phase 1 evaluation. VEGFR3 was the only kinase inhibited by more than 90% by GSK2983559. An additional 11 kinases were inhibited in the range of 70−89%. In a screen against non-kinase targets (Eurofins, 104 receptor and ion channel binding assays and 35 enzyme and cell-based assays), GSK2983559 was highly selective, inhibiting only melatonin receptor MT3 at a concentration under 10 μM. The in vivo efficacy of GSK2983559 was evaluated in a murine 2,4,6-trinitrobenzenesulfonic acid (TNBS) induced colitis model. Mice were dosed orally from days −2 to 5 at 0.25, 7.5, and 145 mg/kg b.i.d. which corresponds to predicted 10%, 50%, and 90% inhibition at 24 h, respectively. Further, administration of GSK2983559 at the 7.5 and 145 mg/kg b.i.d. doses exhibited efficacy similar to that of prednisolone as measured by summed colon scores^[1].
参考文献

[1] Haile PA, Casillas LN, Votta BJ, et al. Discovery of a First-in-Class Receptor Interacting Protein 2 (RIP2) Kinase Specific Clinical Candidate, 2-((4-(Benzo[d]thiazol-5-ylamino)-6-(tert-butylsulfonyl)quinazolin-7-yl)oxy)ethyl Dihydrogen Phosphate, for the Treatment of Inflammatory Diseases. J Med Chem. 2019;62(14):6482-6494

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
- 1.8569 mL
- 9.2845 mL
- 18.5689 mL
- 5 mM
- 0.3714 mL
- 1.8569 mL
- 3.7138 mL
- 10 mM
- 0.1857 mL
- 0.9284 mL
- 1.8569 mL

技术信息

CAS号

1579965-12-0

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H23N4O7PS2

运输

蓝冰

分子量

538.53

别名

RIP2 kinase inhibitor 1;RIPK2-IN-1;RIPK2 inhibitor 3;GSK-2983559

溶解度

DMSO	5.0 mg/mL (9.3 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

GSK2983559 free acid Catalog No. CSN25270

靶点选择性

请登录您的专属账户

确认信息