CYC116
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50:对癌细胞中Aurora A和B分别为44 nM和19 nM。
Ki:对Aurora A和B分别为8 nM和9.2 nM。
Aurora激酶是一个丝氨酸-苏氨酸激酶家族,可与有丝分裂器的部件相互作用,并可调节中心体成熟、双极纺锤体组装、染色体分离和胞质分裂的各方面。CYC116是一种新的N-二苯基-4-(1,2,4-三唑-5-基)嘧啶-2-胺类aurora激酶抑制剂。
在体外:CYC116可抑制细胞内的aurora A和B,从而增加多倍体,导致有丝分裂失败,诱导细胞死亡,因而具有抗癌效果。此外,CYC116对其他激酶的效果也进行了评估[1]。
在体内:初步体内评估表明CYC116具有口服生物利用度,且具有抗癌活性。在研究中,使用两种剂量水平CYC116的小鼠的平均相对肿瘤体积比服用溶剂对照的小鼠都要小[1]。
临床试验:CYC116目前正在I期临床试验中接受评估。
参考文献:
[1] Wang S, Midgley CA, Scarou F, Grabarek JB, Griffiths G, Jackson W, Kontopidis G, McClue SJ, McInnes C, Meades C, Mezna M, Plater A, Stuart I, Thomas MP, Wood G, Clarke RG, Blake DG, Zheleva DI, Lane DP, Jackson RC, Glover DM, Fischer PM. Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors. J Med Chem. 2010;53(11):4367-78.
Storage | Store at -20°C |
M.Wt | 368.46 |
Cas No. | 693228-63-6 |
Formula | C18H20N6OS |
Solubility | insoluble in EtOH; insoluble in H2O; ≥18.4 mg/mL in DMSO with gentle warming |
Chemical Name | 4-methyl-5-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]-1,3-thiazol-2-amine |
SDF | Download SDF |
Canonical SMILES | CC1=C(SC(=N1)N)C2=NC(=NC=C2)NC3=CC=C(C=C3)N4CCOCC4 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
Description | CYC116是一种有效的Aurora A和B的抑制剂,Ki值分别为8 nM和9.2 nM。 | |||||
靶点 | Aurora A | Aurora B | ||||
IC50 | 8 nM | 9.2 nM |
质量控制和MSDS
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