MLN0905
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.
MLN0905是高效PLK1抑制剂,IC50值的范围为3-24 nM [1].
Polo样激酶1(PLK1)属于保守丝氨酸/苏氨酸激酶家族,在调节细胞周期中起重要作用.有证据表明PLK1通过触发G2/M过渡从而驱动细胞周期进程,并作为促癌基因在肿瘤细胞中过表达[2].
MLN0905是选择性PLK1抑制剂,具有和RNAi抑制类似的作用.在HT-29细胞中,MLN0905处理能显著增加pHisH3表达,表明通过抑制PLK1表达,细胞停滞于G2/M期[1].
在人弥漫性大B细胞淋巴瘤(DLBCL)细胞系OCILY-19皮下异种移植的小鼠模型中, MLN0905和利妥昔单抗(rituximab)联合给药能够通过抑制PLK1,导致有丝分裂停滞,从而显著降低肿瘤体积,提高存活时间[1].在人结肠癌HT29异种移植的裸鼠模型中也得到了相同的结果,MLN0905处理显著抑制肿瘤的生长或进程[3].
参考文献：
[1]. Shi, J.Q., et al., MLN0905, a small-molecule plk1 inhibitor, induces antitumor responses in human models of diffuse large B-cell lymphoma. Mol Cancer Ther, 2012. 11(9): p. 2045-53.
[2]. Espeut, J., et al., Natural Loss of Mps1 Kinase in Nematodes Uncovers a Role for Polo-like Kinase 1 in Spindle Checkpoint Initiation. Cell Rep, 2015.
[3]. Duffey, M.O., et al., Discovery of a potent and orally bioavailable benzolactam-derived inhibitor of Polo-like kinase 1 (MLN0905). J Med Chem, 2012. 55(1): p. 197-208.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 486.56 |
| Cas No. | 1228960-69-7 |
| Formula | C24H25F3N6S |
| Solubility | ≥24.35 mg/mL in DMSO |
| Chemical Name | 2-[[5-[3-(dimethylamino)propyl]-2-methylpyridin-3-yl]amino]-9-(trifluoromethyl)-5,7-dihydropyrimido[5,4-d][1]benzazepine-6-thione |
| SDF | Download SDF |
| Canonical SMILES | CC1=C(C=C(C=N1)CCCN(C)C)NC2=NC=C3CC(=S)NC4=C(C3=N2)C=CC(=C4)C(F)(F)F |
| 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 | MLN0905是高效PLK1抑制剂,IC50值为2 nM. | |||||
| 靶点 | PLK1 | |||||
| IC50 | 2 nM | |||||
化学结构
