|4-甲基-5-(2-((4-吗啉苯基)氨基)嘧啶-4-基)噻唑-2-胺|CsnPharm

CAS No.: 693228-63-6

4-Methyl-5-(2-((4-morpholinophenyl)amino)pyrimidin-4-yl)thiazol-2-amine Catalog No. CSN17118

Synonyms: N/A

CYC116 is a potent inhibitor of Aurora with Ki of 8.0 nM/9.2 nM for Aurora A/B.

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400-920-2911

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技术信息

生物活性

描述The aurora kinases, consisting of aurora A, B, and C, are a family of serine-threonine kinases that regulate centrosome maturation, bipolar spindle assembly, chromosome segregation, and cytokinesis. CYC-116 is a potent inhibitor for both aurora A and B with K_i values of 8.0 and 9.2nM, respectively. CYC-116 also inhibited CDK2/cyclin E, CDK4/cyclin D, CDK9/cyclin T, Flt-3, p70 S6, Src, Lck and VEGFR2 with K_i values of 0.39, 1.09, 0.48, 0.044, 0.54, 0.82, 2.80, and 0.044μM, respectively. iIn an MTT assay, CYC-116 inhibited A2780 and MiaPaCa-2 cell growth with IC50 values of 170 and 278nM, respectively. CYC-116 also exhibited anti-proliferative activity against MCF-7, Hela, Colo205, K562, NCI-H460, Saos-2, and Messa cell lines with IC50 values of 0.599, 0.590, 0.241, 1.375, 0.681, 0.110, and 0.090μM, respectively. In a murine P388/D1 leukemia model, oral administration of CYC-116 at 45 and 67mg/kg twice daily resulted in a significant increase in lifespan of 172% and 183%, respectively, as compared to the vehicle control group. In mice bearing subcutaneous NCI-H460 xenografts, oral dosing of CYC-116 at 75 and 100mg/kg/day caused tumor growth delays of 2.3 and 5.8 days, respectively.^[3]
作用机制CYC-116 is an inhibitor for aurora A and B that possesses anticancer activity.^[3]
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
A2780 cells	-	Cytotoxicity assay	96 h	Cytotoxicity against human A2780 cells after 96 hrs by MTT assay	20462263
A549 cells	0.5-2 μM	Function assay	7 h	Cell cycle arrest in asynchronous human A549 cells assessed as accumulation of cyclin B1-negative tetraploid cells at G1 phase at 0.5 to 2 uM after 7 hrs by FACS analysis	20462263
A549 cells	-	Function assay	7 h	Inhibition of Aurora kinase in human A549 cells assessed as concentration required for half-maximal inhibition of histone H3 serine-10 phosphorylation after 7 hrs immunofluorescence microscopy	20462263

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临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00560716	Solid Tumors	Phase 1	Terminated(Sponsor decision)	November 2009	United States, New York ... more >> Roswell Park Cancer Institute Buffalo, New York, United States, 14263 United States, Texas South Texas Accelerated Research Therapeutics San Antonio, Texas, United States, 78229 Collapse <<

参考文献

[1] Kamei H, Jackson RC, et al. An integrated pharmacokinetic-pharmacodynamic model for an Aurora kinase inhibitor. J Pharmacokinet Pharmacodyn. 2010 Aug;37(4):407-34.
[2] Wang S, Midgley CA, et al. Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors. J Med Chem. 2010 Jun 10;53(11):4367-78.
[3] Wang S, Midgley CA, Scaërou F, et al. Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors. J Med Chem. 2010;53(11):4367-4378. doi:10.1021/jm901913s

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
- 2.7140 mL
- 13.5701 mL
- 27.1403 mL
- 5 mM
- 0.5428 mL
- 2.7140 mL
- 5.4281 mL
- 10 mM
- 0.2714 mL
- 1.3570 mL
- 2.7140 mL

技术信息

CAS号

693228-63-6

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

C18H20N6OS

运输

蓝冰

分子量

368.46

别名

N/A

溶解度

DMSO	5.0 mg/mL (13.6 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+water	0.1 mg/mL	clear
PO	0.5% CMC-Na	71 mg/mL	suspension

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Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

A2780 cells	-	Cytotoxicity assay	96 h	Cytotoxicity against human A2780 cells after 96 hrs by MTT assay	20462263
A549 cells	0.5-2 μM	Function assay	7 h	Cell cycle arrest in asynchronous human A549 cells assessed as accumulation of cyclin B1-negative tetraploid cells at G1 phase at 0.5 to 2 uM after 7 hrs by FACS analysis	20462263
A549 cells	-	Function assay	7 h	Inhibition of Aurora kinase in human A549 cells assessed as concentration required for half-maximal inhibition of histone H3 serine-10 phosphorylation after 7 hrs immunofluorescence microscopy	20462263
BxPC3 cells	-	Cytotoxicity assay	96 h	Cytotoxicity against human BxPC3 cells after 96 hrs by MTT assay	20462263
CCRF-CEM cells	-	Cytotoxicity assay	96 h	Cytotoxicity against human CCRF-CEM cells after 96 hrs by MTT assay	20462263
COLO205 cells	-	Cytotoxicity assay	96 h	Cytotoxicity against human COLO205 cells after 96 hrs by MTT assay	20462263
HCT116 cells	-	Cytotoxicity assay	96 h	Cytotoxicity against human HCT116 cells after 96 hrs by MTT assay	20462263
HeLa cells	-	Cytotoxicity assay	96 h	Cytotoxicity against human HeLa cells after 96 hrs by MTT assay	20462263
HeLa cells	1.25 μM	Function assay	7 h	Inhibition of Aurora kinase in human HeLa cells assessed as complete inhibition of histone H3 phosphorylation at 1.25 uM after 7 hrs by Western blot analysis	20462263
HL60 cells	-	Cytotoxicity assay	96 h	Cytotoxicity against human HL60 cells after 96 hrs by MTT assay	20462263
HT-29 cells	-	Cytotoxicity assay	96 h	Cytotoxicity against human HT-29 cells after 96 hrs by MTT assay	20462263
HUPT4 cells	-	Cytotoxicity assay	96 h	Cytotoxicity against human HUPT4 cells after 96 hrs by MTT assay	20462263
K562 cells	-	Cytotoxicity assay	96 h	Cytotoxicity against human K562 cells after 96 hrs by MTT assay	20462263
MCF7 cells	-	Cytotoxicity assay	96 h	Cytotoxicity against human MCF7 cells after 96 hrs by MTT assay	20462263
MESSA cells	-	Cytotoxicity assay	96 h	Cytotoxicity against human MESSA cells after 96 hrs by MTT assay	20462263
MIAPaCa2 cells	-	Cytotoxicity assay	96 h	Cytotoxicity against human MIAPaCa2 cells after 96 hrs by MTT assay	20462263
MV4-11 cells	-	Cytotoxicity assay	96 h	Cytotoxicity against human MV4-11 cells after 96 hrs by MTT assay	20462263
NCI-H460 cells	-	Cytotoxicity assay	96 h	Cytotoxicity against human NCI-H460 cells after 96 hrs by MTT assay	20462263
Saos2 cells	-	Cytotoxicity assay	96 h	Cytotoxicity against human Saos2 cells after 96 hrs by MTT assay	20462263
SW620 cells	1 μM	Function assay	48 h	Effect on mitotic index in human SW620 cells assessed as appearance of polyploid cells at 1 uM after 48 hrs by propidium iodide staining-based FACS analysis	20462263
U2OS cells	0.07-10 uM	Function assay	2 h	Inhibition of Aurora kinase in nocodazole-synchronized human U2OS cells assessed as reduction of histone H3 serine-10 phosphorylation at 0.07 to 10 uM after 2 hrs immunofluorescence microscopy	20462263

4-Methyl-5-(2-((4-morpholinophenyl)amino)pyrimidin-4-yl)thiazol-2-amine Catalog No. CSN17118

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