|顺式-4 - ((2 - ((1H-苯并[d]咪唑-6-基)氨基)喹唑啉-8-基)氧基)环己醇|CsnPharm

CAS No.: 1792999-26-8

NCB-0846 Catalog No. CSN20456

Synonyms: NCB-0846

NCB-0846 is an TNIK inhibitor with IC50 value of 21 nM.

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

靶点 TNIK

IC50:21nM
描述Wnt signaling plays important roles in carcinogenesis and embryonic development. TNIK is a serine/threonine kinase that functions as an activator of the Wnt signaling pathway. TNIK is recruited to promoters of Wnt target genes and required to activate their expression. TCF4 is a substrate of the TNIK enzyme. TNIK phosphorylates TCF4 and regulates its transcriptional activity. TNIK together with NEDD4 and RAP2A form a signaling complex which regulates neuronal dendrite extension and arborization during development. TNIK may also play a role in cytoskeletal rearrangements and regulate cell spreading^[3]. NCB-0846 is a TNIK inhibitor. The inhibitory IC₅₀ of NCB-0846 against TNIK kinase was 21 nM^[4]. In an experiment system of recombinant TCF4 and TNIK proteins, NCB-0846 induced faster migration of TCF4 phosphorylated by TNIK within a concentration range of 0.1 - 0.3 μM and completely inhibited the phosphorylation of TCF4 at a concentration of 3 μM . Furthermore, NCB-0846 blocked the autophosphorylation of TNIK in hct116 cells. At the concentrations of 3 μM or 10 μM, NCB-0846 reduced the expression of the Wnt target genes AXIN2 and MYC as well as that of TNIK in hct116 cells. NCB-0846 also reduced the expression of TNIK, AXIN2 and cMYC at the protein level at the concentration range of 1 – 10 μM in hct116 and DLD-1 cells^[4]. According to another report, NCB-0846 at the concentrations of 1 μM or 3 μM reduced colony formation of cells derived from patients of prostate cancer^[5]. In a hct116 xenograft model established in balb/c nude mice, NCB-0846 was administrated to the mice orally at the doses of 40 mg/kg or 80 mg/kg bid. Both doses of NCB-0846 suppressed tumor growth^[4]. In a Wnt-driven tumorigenesis model utilizing Apc^min/+ mice, 3 doses of NCB-0846, including 22.5 mg/kg, 45 mg/kg, 90 mg/kg were administrated. NCB-0846 dose dependently reduced the multiplicity and dimensions of tumours that developed in the small intestine of mice^[4].
动物研究
剂量
BALB/c nude mice: 40 mg/kg, 80 mg/kg^[2] (p.o., BID)

给药途径
p.o.
参考文献

动物研究
剂量	BALB/c nude mice: 40 mg/kg, 80 mg/kg^[2] (p.o., BID)
给药途径	p.o.

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
- 2.6637 mL
- 13.3183 mL
- 26.6366 mL
- 5 mM
- 0.5327 mL
- 2.6637 mL
- 5.3273 mL
- 10 mM
- 0.2664 mL
- 1.3318 mL
- 2.6637 mL

技术信息

CAS号

1792999-26-8

储存条件

粉末: Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H21N5O2

运输

蓝冰

分子量

375.42

别名

NCB-0846

溶解度

DMSO	73.0 mg/mL (194.4 mM) warming
Water	Insoluble
Ethanol	2.0 mg/mL (5.3 mM) warming

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

NCB-0846 Catalog No. CSN20456

靶点选择性

请登录您的专属账户

确认信息