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BS-181

现货
Catalog No.
A3266
CDK7抑制剂
组合的产品项目
规格价格库存 数量
5mg
¥ 1,000.00
Ship with 10-15 days
25mg
¥ 3,000.00
Ship with 10-15 days
100mg
¥ 7,500.00
Ship with 10-15 days

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Background

Normal progression through the cell cycle requires the sequential action of cyclin-dependent kinases (CDK1, CDK2, CDK4 and CDK6). Deregulation of CDK activity is a feature of almost all cancers and has led to the development of CDK inhibitors as anticancer agents. As such, CDK7 is an target for the anticancer drug development. Computer modeling of CDK7 was used to design potential potent CDK7 inhibitor, which is BS-181.
In vitro: Testing of other CDKs as well as another 69 kinases showed that BS-181 only inhibited CDK2 at concentrations lower than 1 μM, with 35-fold less potently (IC50 880 nM) than CDK7. BS-181 inhibited the phosphorylation of CDK7 substrates in MCF-7 cells, led to cell cycle arrest and apoptosis to inhibit the growth of cancer cell lines, and showed antitumor effects in vivo [1].
In vivo: BS-181 was stable in vivo after i.p. administration of 10 mg kg-1. The same dose of drug inhibited the growth of MCF-7 human xenografts in nude mice. BS-181 is the first example of a potent and selective CDK7 inhibitor with potential as an anticancer agent [1].
Clinical trial: Currently no clinical data are available.
Reference:
[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.

Chemical Properties

StorageStore at -20°C
M.Wt380.53
Cas No.1092443-52-1
FormulaC22H32N6
SynonymsBS 181; BS181
SolubilitySoluble in DMSO
Chemical Name5-N-(6-aminohexyl)-7-N-benzyl-3-propan-2-ylpyrazolo[1,5-a]pyrimidine-5,7-diamine
SDFDownload SDF
Canonical SMILESCC(C)C1=C2N=C(C=C(N2N=C1)NCC3=CC=CC=C3)NCCCCCCN
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。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。

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批次:

化学结构

BS-181