TNIK-IN-3

目录号: PL04070 纯度: ≥99%
TNIK-IN-3 (化合物 21k) 是一种有效,选择性和具有口服活性的 TNIK 抑制剂,IC50 值为 0.026 μM。TNIK-IN-3 还可以抑制 Flt4 (IC50=0.030 μM),Flt1 (IC50=0.191 μM) 和 DRAK1 (IC50=0.411 μM)。TNIK-IN-3 可用于结直肠癌的研究。
CAS No. :2754265-25-1
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中文名称
TNIK-IN-3
英文名称
TNIK-IN-3
英文别名
1,4-Benzoxazepin-5(2H)-one, 4-[(4-fluorophenyl)methyl]-3,4-dihydro-8-(1H-pyrrolo[2,3-b]pyridin-5-yl)-;TNIK-IN-3
Cas No.
2754265-25-1
分子式
C23H18FN3O2
分子量
387.41
包装储存
Powder -20°C 3 years;4°C 2 years
详情描述

TNIK-IN-3 (化合物 21k) 是一种有效,选择性和具有口服活性的 TNIK 抑制剂,IC50 值为 0.026 μM。TNIK-IN-3 还可以抑制 Flt4 (IC50=0.030 μM),Flt1 (IC50=0.191 μM) 和 DRAK1 (IC50=0.411 μM)。TNIK-IN-3 可用于结直肠癌的研究。

产品详情
TNIK-IN-3 (化合物 21k) 是一种有效,选择性和具有口服活性的 TNIK 抑制剂,IC50 值为 0.026 μM。TNIK-IN-3 还可以抑制 Flt4 (IC50=0.030 μM),Flt1 (IC50=0.191 μM) 和 DRAK1 (IC50=0.411 μM)。TNIK-IN-3 可用于结直肠癌的研究。
生物活性
TNIK-IN-3 is a potent, selective and orally active inhibitor of Traf2- and Nck-interacting protein kinase (TNIK), with an IC 50 of 0.026 μM. TNIK-IN-3 could also inhibit Flt4 (IC 50 =0.030 μM), Flt1 (IC 50 =0.191 μM) and DRAK1 (IC 50 =0.411 μM). TNIK-IN-3 can be used for the research of colorectal cancer.
性状
Solid
IC50 & Target[1][2]
IC50: 0.026 μM (TNIK), 0.030 μM (Flt4), 0.191 μM (Flt1), 0.411 μM (DRAK1)
体外研究(In Vitro)
TNIK-IN-3 (compound 21k) inhibits Aurora-A, GCK, and MLK3 with IC50s of 0.517 μM, 3.657 μM, and 4.552 μM, respectively.
TNIK-IN-3 (0.1-100 μM; 3 days) inhibits the viability of HCT116 and DLD-1 cells, with IC50s of 4.26 μM and 8.00 μM, respectively.
TNIK-IN-3 (2.5-40 μM; 10 days) dose-dependently inhibits the colony formation of HCT116 and DLD-1 cells.
TNIK-IN-3 (5-20 μM; 48 h) inhibits the migration of HCT116 and DLD-1 cells.
TNIK-IN-3 (5-40 μM; 48 h) dose-dependently inhibits the expression ofLRP5 and LRP6 proteins, Wnt target genes AXIN2 and c-Myc in HCT116 cells.
TNIK-IN-3 (5-20 μM; 48 h) significantly suppresses the phosphorylation of JNK1/2 in Hela cells. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
TNIK-IN-3 (compound 21k) (100-150 mg/kg; p.o. twice daily for 18 days) inhibits tumor growth in a dose-dependent manner.
has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Li Y, et, al. Discovery of 3,4-Dihydrobenzo[ f][1,4]oxazepin-5(2 H)-one Derivatives as a New Class of Selective TNIK Inhibitors and Evaluation of Their Anti-Colorectal Cancer Effects. J Med Chem. 2022 Jan 5.
溶解度数据
In Vitro: DMSO : 83.33 mg/mL (215.10 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)
[1]. Li Y, et, al. Discovery of 3,4-Dihydrobenzo[ f][1,4]oxazepin-5(2 H)-one Derivatives as a New Class of Selective TNIK Inhibitors and Evaluation of Their Anti-Colorectal Cancer Effects. J Med Chem. 2022 Jan 5.

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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