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CAS No.: 443797-96-4

JNJ-7706621 Catalog No. CSN12858

Synonyms: Aurora A Inhibitor I;Aurora Kinase/CDK Inhibitor

JNJ-7706621 is a pan-CDK inhibitor that inhibits CDK1/2 with IC50 of 9/4 nM, also potently inhibits Aurora A/B.

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实验方案

技术信息

生物活性

描述Cyclin-dependent kinases (CDKs) are a family of serine/threonine protein kinases that participate in cell cycle regulation. The functionally distinct kinase complexes are formed by the combination of catalytic kinase subunits (such as CDK1, CDK2, CDK4, or CDK6) with regulatory cyclin subunits (such as cyclin A, B, D1, D2, D3, or E). Coordinated activation of these complexes at specific times drives cells through the cell cycle and ensures the fidelity of cell division. The Aurora kinases also have a critical role in controlling chromosome movement and organization, thus regulating cell cycle. Aurora-A contributes to formation of the mitotic spindle apparatus that guarantees accurate segregation of chromosomes into daughter cells; Aurora-B is required for cytokinesis and proper chromosome architecture during mitosis. JNJ-7706621 is a dual CDK and aurora inhibitor. Based on results from in vitro kinase assays utilizing human recombinant enzymes, JNJ-7706621 inhibited CDK1/Cyclin B, CDK2/Cyclin A, CDK2/Cyclin E, Aurora-A and Aurora-B with IC50s of 9 nM, 4 nM, 3 nM, 11 nM and 15 nM, respectively. JNJ-7706621 showed potent growth inhibition in vitro on human cancer cell lines of Hela, HCT-116, SKOV-3, PC3, A375, MDA-MB-231, DU145 with IC50 values ranging from 112 to 514 nM. Cell cycle analysis on Hela cells synchronized in G1 showed that cells treated with 3 μM JNJ-7706621 did not enter the S phase until 16 hours after G1 synchronization, indicating that JNJ-7706621 delayed exit from G1 and arrested cells in G2-M. In a human tumor xenograft model established by implantation of A375 tumor fragments in female nu/nu mice, JNJ-7706621 given i.p. when the tumors reached approximately 62 to 126 mg at the dose of 125 mg/kg with the 7 on/7 off schedule or the 100 mg/kg daily schedule both produced identical tumor growth inhibition values of 93%^[3].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
HCT116 cells	-	Function assay	-	In vitro inhibitory concentration against cell proliferation in human HCT116 (colon carcinoma) tumor cells, IC50=0.25 μM	15974571
human A375 cells	-	Proliferation assay	-	Antiproliferative activity against human A375 cells, IC50=0.447 μM	16682186
human HeLa cells	-	Function assay	-	In vitro inhibitory concentration against cell proliferation in human HeLa (cervical adenocarcinoma) tumor cells, IC50=0.28 μM	15974571

更多
动物研究
剂量
Mice: 30 mg/kg^[3] (i.p.), 125 mg/kg^[2] (i.p.); 3.25 mg/kg^[4] (i.v.)

给药途径
i.p., i.v.
参考文献

动物研究
剂量	Mice: 30 mg/kg^[3] (i.p.), 125 mg/kg^[2] (i.p.); 3.25 mg/kg^[4] (i.v.)
给药途径	i.p., i.v.

[1] Seamon JA, Rugg CA, et al. Role of the ABCG2 drug transporter in the resistance and oral bioavailability of a potent cyclin-dependent kinase/Aurora kinase inhibitor. Mol Cancer Ther. 2006 Oct;5(10):2459-67.
[2] Emanuel S, Rugg CA, et al. The in vitro and in vivo effects of JNJ-7706621: a dual inhibitor of cyclin-dependent kinases and aurora kinases. Cancer Res. 2005 Oct 1;65(19):9038-46.
[3] Emanuel S, Rugg CA, Gruninger RH, Lin R, Fuentes-Pesquera A, Connolly PJ, Wetter SK, Hollister B, Kruger WW, Napier C, Jolliffe L, Middleton SA. The in vitro and in vivo effects of JNJ-7706621: a dual inhibitor of cyclin-dependent kinases and aurora kinases. Cancer Res. 2005 Oct 1;65(19):9038-46.

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
- 2.5358 mL
- 12.6789 mL
- 25.3578 mL
- 5 mM
- 0.5072 mL
- 2.5358 mL
- 5.0716 mL
- 10 mM
- 0.2536 mL
- 1.2679 mL
- 2.5358 mL

技术信息

CAS号

443797-96-4

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C15H12F2N6O3S

运输

蓝冰

分子量

394.36

别名

Aurora A Inhibitor I;Aurora Kinase/CDK Inhibitor

溶解度

DMSO	500.0 mg/mL (1267.9 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+30% PEG300+water	10 mg/mL	clear
PO	0.5% CMC-Na	52 mg/mL	suspension

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