Home >> BS-181
Related Products
BS-181 CDK7 inhibitor,highly selective

Catalog No.A3266
Size Price Stock Qty
5mg
$100.00
In stock
25mg
$300.00
In stock
100mg
$750.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

      

Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & MSDS

View current batch:

Chemical structure

BS-181

BS-181 Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

BS-181 Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Chemical Properties

Cas No. 1092443-52-1 SDF Download SDF
Synonyms BS 181; BS181
Chemical Name 5-N-(6-aminohexyl)-7-N-benzyl-3-propan-2-ylpyrazolo[1,5-a]pyrimidine-5,7-diamine
Canonical SMILES CC(C)C1=C2N=C(C=C(N2N=C1)NCC3=CC=CC=C3)NCCCCCCN
Formula C22H32N6 M.Wt 380.53
Solubility Soluble in DMSO Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

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.