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★【Medlife】CYC116

发表时间:2024-11-26
中文名称 
CYC116
中文别名 
4-(2-氨基-4-甲基-5-噻唑基)-N-[4-(4-吗啉基)苯基]-2-嘧啶胺;CYC-116;4-(2-氨基-4-甲基-5-噻唑基)-N-[4-(4-吗啉基)苯基]-2-嘧啶胺
英文名称 
CYC116
英文别名 
4-(2-Amino-4-methyl-5-thiazolyl)-N-[4-(4-morpholinyl)phenyl]-2-pyrimidinamine;CYC116;4-Methyl-5-(2-((4-morpholinophenyl)amino)-pyrimidin-4-yl)thiazol-2-amine;Chemical Biology Probes ;CYC-116;2c5t;AC1O4WKE;CHEBI:620120;CHEMBL482967;CYC-116, CYC116;Kinome_636;S1171_Selleck;4-methyl-5-(2-(4-morpholinophenylamino)pyrimidin-4-yl)thiazol-2-amine;4-methyl-5-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]-1,3-thiazol-2-amine;4-(2-amino-4-methylthiazol-5-yl)-N-(4-morpholinophenyl)pyrimidin-2-amine;4-methyl-5-(2-((4-morpholinophenyl)amino)pyrimidin-4-yl)thiazol-2-amine;2uue;CYC 116;GPSZYOIFQZPWEJ-UHFFFAOYSA-N;MLS006011244;SYN
Cas No. 
693228-63-6
分子式 
C18H20N6Os
分子量 
368.46
包装储存 
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months

-20°C 1 month

生物活性 
CYC-116 is a potent aurora A and aurora B inhibitor with Kis of 8 and 9 nM, respectively.
性状 
Solid
IC50 & Target[1][2] 
Aurora A
8 nM (Ki)
Aurora B
9.2 nM (Ki)
体外研究(In Vitro) 
CYC-116 also inhibits VEGFR2, Src, Lck AND FLT3 with with Kis of 44, 82, 280, 44 nM, respectively. CYC-116 may have broad-spectrum antitumor activity. CYC-116 shows potent antiproliferative activity against cancer cell lines with with IC50s of 0.599, 0.59, 0.241, 0.34, 0.725, 1.375, 0.471, 0.034, 0.372, 0.681, 0.151, 1.626, 0.775, 0.308, 0.110, 0.09 for MCF7, HeLa, Colo205, HCT-116, HT29, K562, CCRF-CEM, MV4-11, HL60, NCI-H460, A2780, BxPC3, HuPT4, Mia-Paca-2, Saos-2, Messa cells. Treatment with 1.25 μM CYC-116 for 7 h results in complete inhibition of histone H3 phosphorylation in HeLa cell lysates.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo) 
Oral administration of CYC-116 at dose levels of 75 and 100 mg/kg q.d. causes tumor growth delays of 2.3 and 5.8 days, which translates into specific growth delays of 0.32 and 0.81, respectively. The mean relative tumor volumes of mice receiving CYC-116 at both dose levels are less than those of vehicle-treated mice for the duration of the study period. At 100 mg/kg po q.d., the reduction in growth is statistically significant on days 6 and 9.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件 
Room temperature or refrigerated transportation.
储存方式 
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
ClinicalTrial 
参考文献 
[1]. Wang S, 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.  [Information]



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