GSK-461364
Product Detail
Product Tags
| Pack Size | Availability | Price (USD) |
| 100mg | In Stock | 400 |
| 500mg | In Stock | 1400 |
| More Sizes | Get Quotes | Get Quotes |
Chemical Name:
(R)-5-(6-((4-methylpiperazin-1-yl)methyl)-1H-benzo[d]imidazol-1-yl)-3-(1-(2-(trifluoromethyl)phenyl)ethoxy)thiophene-2-carboxamide
SMILES Code:
O=C(C1=C(O[C@@H](C2=CC=CC=C2C(F)(F)F)C)C=C(N3C=NC4=CC=C(CN5CCN(C)CC5)C=C34)S1)N
InChi Code:
InChI=1S/C27H28F3N5O2S/c1-17(19-5-3-4-6-20(19)27(28,29)30)37-23-14-24(38-25(23)26(31)36)35-16-32-21-8-7-18(13-22(21)35)15-34-11-9-33(2)10-12-34/h3-8,13-14,16-17H,9-12,15H2,1-2H3,(H2,31,36)/t17-/m1/s1
InChi Key:
ZHJGWYRLJUCMRT-QGZVFWFLSA-N
Keyword:
GSK-461364, GSK461364, GSK 461364, GSK-461364A, GSK 461364A, GSK461364A, 929095-18-1
Solubility: Soluble in DMSO
Storage: 0 - 4°C for short term (days to weeks), or -20°C for long term (months)
Description:
Polo-like kinases (Plks) are serine/threonine kinases with key roles in cell cycling. GSK461364 is a potent, reversible inhibitor of Plk1 (Ki = 2.2 nM). It is less effective against Plk2 and Plk3 (Kis = 860 and 1,000 nM, respectively) and at least 1,000-fold selective for Plk1 over a panel of 48 other kinases. GSK461364 dose-dependently halts cell cycling in diverse proliferating cancer cell lines and, at higher doses, triggers apoptosis. It appears to be more effective against p53-deficient tumors and is able to cross the blood-brain barrier. GSK461364 is effective in vivo, inducing tumor growth inhibition or growth delay in xenograft models in mice.
Target: Plk1
