BS-181
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.
正常的细胞周期进程需要细胞周期蛋白依赖性激酶(CDK1、CDK2、CDK4和CDK6)的顺序作用。CDK活性异常几乎是所有癌症的一个特征,这使得CDK抑制剂发展成为抗癌药物。因此,CDK7是抗癌药物开发的靶点。CDK7的计算机模拟用于设计潜在的强效CDK7抑制剂BS-181。
体外:其他CDKs以及另外69种激酶的测试表明,浓度低于1 μM的BS-181仅抑制CDK2,比CDK7的效力(IC50 880 nM)弱35倍。BS-181抑制MCF-7细胞中CDK7底物的磷酸化,导致细胞周期停滞和细胞凋亡,从而抑制癌细胞系的生长,并在体内显示抗肿瘤作用[1]。
体内:10 mg kg-1的BS-181腹腔内给药后在体内稳定。相同剂量的药物抑制裸鼠中MCF-7人异种移植物的生长。BS-181是第一个强效的和选择性的CDK7抑制剂实例,具有作为抗癌剂的潜力[1]。
临床试验:目前没有临床数据可用。
参考文献:
[1] Ali S, Heathcote DA, Kroll SH, Jogalekar AS, Scheiper B, Patel H, Brackow J, Siwicka A, Fuchter MJ, Periyasamy M, Tolhurst RS, Kanneganti SK, Snyder JP, Liotta DC, Aboagye EO, Barrett AG, Coombes RC. The development of a selective cyclin-dependent kinase inhibitor that shows antitumor activity. Cancer Res. 2009;69(15):6208-15.
Storage | Store at -20°C |
M.Wt | 380.53 |
Cas No. | 1092443-52-1 |
Formula | C22H32N6 |
Synonyms | BS 181; BS181 |
Solubility | Soluble in DMSO |
Chemical Name | 5-N-(6-aminohexyl)-7-N-benzyl-3-propan-2-ylpyrazolo[1,5-a]pyrimidine-5,7-diamine |
SDF | Download SDF |
Canonical SMILES | CC(C)C1=C2N=C(C=C(N2N=C1)NCC3=CC=CC=C3)NCCCCCCN |
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。 |