GlpBio

NCB-0846

目录号: GC19260纯度: >98.00%同义词: 顺式-4-((2-((1H-苯并[D]咪唑-6-基)氨基)喹唑啉-8-基)氧基)环己醇
A TNIK inhibitor
NCB-0846
Cas No.: 1792999-26-8
规格价格库存数量操作
5mg¥810.00现货
1
10mg¥1,350.00现货
1
25mg¥2,880.00现货
1
50mg¥4,860.00现货
1
100mg¥8,460.00现货
1
10mM (in 1mL DMSO)¥891.00现货
1
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产品描述 Description

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

NCB-0846 has anti-Wnt activity. NCB-0846 binds to TNIK in an inactive conformation, and this binding mode seems to be essential for Wnt inhibition. NCB-0846 shows inhibitory activity against TNIK with an IC50 of 21 nM. NCB-0846 also inhibits FLT3, JAK3, PDGFRα, TRKA, CDK2/CycA2, and HGK. NCB-0846 induces faster migration of TCF4 phosphorylated by TNIK within a concentration range of 0.1-0.3 uM and completely inhibits the phosphorylation of TCF4 at a concentration of 3 uM. NCB-0846 inhibits HCT116 cell growth and shows much higher (-20-fold) inhibitory activity against colony formation by the same cells in soft agar[1].

NCB-0846 suppresses the growth of tumors established by inoculating HCT116 cells into immunodeficient mice. The expression of Wnt-target genes (AXIN2, MYC and CCND1) in xenografts is reduced following the administration of NCB-0846. NCB-0846 induces an increase in the sub-G1 cell population. Cleavage of poly (ADP-ribose) polymerase 1 indicates the induction of apoptosis[1].

References:
[1]. Masuda M, et al. TNIK inhibition abrogates colorectal cancer stemness. Nat Commun. 2016 Aug 26;7:12586.

实验参考方法 Experimental Reference Method

Animal experiment:

Mice: NCB-0846 is suspended in DMSO/polyethylene glycol#400/30% 2-hydroxypropyl-β-cyclodextrin solution (10:45:45v/v). Five million HCT116 cells suspended in medium containing 25% Matrigel are inoculated into the subcutaneous tissues of 9-week-old female BALB/c nude mice. Mice are randomized according to tumour volume (9 mice per group). NCB-0846 was administered daily by oral gavage at 0 (vehicle alone), 40 or 80 mg/kg (body weight) BID (bis in die) for 14 days[1].

References:

[1]. Masuda M, et al. TNIK inhibition abrogates colorectal cancer stemness. Nat Commun. 2016 Aug 26;7:12586.

产品文档 Product Documents

Purity:>98.00%

化学性质Chemical Properties

CAS 号
1792999-26-8
同义词
顺式-4-((2-((1H-苯并[D]咪唑-6-基)氨基)喹唑啉-8-基)氧基)环己醇
SMILES
O[C@@H](CC1)CC[C@@H]1OC2=CC=CC(C=N3)=C2N=C3NC4=CC=C(N=CN5)C5=C4
分子式
C21H21N5O2
分子量
375.42 g/mol
溶解性
DMSO : ≥ 30 mg/mL (79.91 mM)
保存条件
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°C，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。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol