SNS-314 Mesylate
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.
SNS-314是一种ATP-竞争性和选择性的有丝分裂激酶(aurora)抑制剂,对Aurora A\ Aurora B和Aurora C的IC50值分别为9 nM\31 nM和3 nM[1,2].
有丝分裂激酶是调控细胞有丝分裂的丝氨酸/苏氨酸激酶.它们与癌症的发生和扩散相关,在多种肿瘤细胞中过表达,如黑色素瘤\卵巢癌\结肠癌\胰腺癌和乳腺癌.因此,有丝分裂激酶被认为是癌症治疗潜在的靶点.作为一种有效的有丝分裂激酶抑制剂,SNS-314抑制多种肿瘤细胞的增殖,并且在HCT116荷瘤小鼠中显示出较强的抗肿瘤活性.SNS-314的作用机制发现是抑制组蛋白H3 Ser10的磷酸化作用[1,2].
在基于FRET的生化试验中,SNS-314抑制有丝分裂激酶A\B\C的活性,IC50值分别为9 nM\31 nM和3 nM.当对219种激酶测试,SNS-314只抑制其中的24种激酶的活性,抑制率在65%或以上.这表明SNS-314是一种选择性的有丝分裂激酶抑制剂.在细胞试验中,SNS-314阻断肿瘤细胞的增殖,IC50值范围为1.8 nM(A2780)到24 nM(HT29).在HCT-116细胞中,用SNS-314处理16小时,导致明显的细胞周期缺陷[2].
在人类肿瘤异种移植小鼠模型中,SNS-314对多种肿瘤显示出显著的抗肿瘤活性,包括PC-3\H1299\A2780\MDA-MB-231和A375细胞的异种移植物.剂量为170 mg/kg时,TGI值在54%和91%之间.同时也持续抑制有丝分裂激酶B的底物pHH3[2].
参考文献：
[1] Oslob J D, Romanowski M J, Allen D A, et al. Discovery of a potent and selective aurora kinase inhibitor. Bioorganic & medicinal chemistry letters, 2008, 18(17): 4880-4884.
[2] Arbitrario J P, Belmont B J, Evanchik M J, et al. SNS-314, a pan-Aurora kinase inhibitor, shows potent anti-tumor activity and dosing flexibility in vivo. Cancer chemotherapy and pharmacology, 2010, 65(4): 707-717.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 527.04 |
| Cas No. | 1146618-41-8 |
| Formula | C18H15ClN6OS2·CH4O3S |
| Solubility | ≥26.35 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH |
| Chemical Name | 1-(3-chlorophenyl)-3-[5-[2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl]-1,3-thiazol-2-yl]urea;methanesulfonic acid |
| SDF | Download SDF |
| Canonical SMILES | CS(=O)(=O)O.C1=CC(=CC(=C1)Cl)NC(=O)NC2=NC=C(S2)CCNC3=NC=NC4=C3SC=C4 |
| 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 | SNS-314 Mesylate是一种有效的Aurora A/B/C选择性抑制剂,IC50值分别为9 nM\31 nM和3 nM. | |||||
| 靶点 | Aurora C | Aurora A | Aurora B | |||
| IC50 | 3 nM | 9 nM | 31 nM | |||
质量控制和MSDS
- 批次:
化学结构
