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SML1912

Sigma-Aldrich

GSK461364A

≥98% (HPLC)

Sinônimo(s):

(R)-5-(6-((4-methylpiperazin-1-yl)methyl)-1H-benzo[d]imidazol-1-yl)-3-(1-(2-(trifluoromethyl)phenyl)ethoxy)thiophene-2-carboxamide, 5-[6-[(4-Methyl-1-piperazinyl)methyl]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]-2-thiophenecarboxamide, GSK461364

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About This Item

Fórmula empírica (Notação de Hill):
C27H28F3N5O2S
Número CAS:
929095-18-1
Peso molecular:
543.60
Número MDL:
MFCD12755419
Código UNSPSC:
12352200
NACRES:
NA.77

Nível de qualidade

100

Ensaio

≥98% (HPLC)

forma

powder

cor

white to beige

solubilidade

DMSO: 25 mg/mL, clear

temperatura de armazenamento

2-8°C

cadeia de caracteres SMILES

CN1CCN(CC2=CC3=C(N=CN3C4=CC(O[C@@H](C5=C(C=CC=C5)C(F)(F)F)C)=C(C(N)=O)S4)C=C2)CC1

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

chave InChI

ZHJGWYRLJUCMRT-QGZVFWFLSA-N

Ações bioquímicas/fisiológicas

GSK461364 is an imidazotriazine derivate that inhibits polo-like kinase 1 (Plk1) in a potent, reversible, ATP-competitive, and highly selective manner (Kiapp <0.5 nM vs. 0.86 μM for Plk2 and 200 μM for Plk3; ATP Kmapp = 16 μM), exhibiting much reduced or little potency toward a panel of 262 kinases. GSK461364A inhibits the growth of various cancer cultures (IG50 <100 nM) as a result of either growth arrest (cytostasis) or cytotoxicity in vitro and effectively suppresses the expansion of various human tumor exnografts in mice in vivo (25 or 50 mg/kg i.p. q2dx12).

Código de classe de armazenamento

11 - Combustible Solids

Classe de risco de água (WGK)

WGK 3

Ponto de fulgor (°F)

Not applicable

Ponto de fulgor (°C)

Not applicable

Certificados de análise (COA)

Busque Certificados de análise (COA) digitando o Número do Lote do produto. Os números de lote e remessa podem ser encontrados no rótulo de um produto após a palavra “Lot” ou “Batch”.

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Yongzhen Qian et al.
Clinical & experimental metastasis, 28(8), 899-908 (2011-09-29)
Few therapeutic strategies exist for the treatment of metastatic tumor cells in the brain because the blood-brain barrier (BBB) limits drug access. Thus the identification of molecular targets and accompanying BBB permeable drugs will significantly benefit brain metastasis patients. Polo-like
Aidan G Gilmartin et al.
Cancer research, 69(17), 6969-6977 (2009-08-20)
Polo-like kinase 1 (Plk1) is a conserved serine/threonine kinase that plays an essential role in regulating the many processes involved in mitotic entry and progression. In humans, Plk1 is expressed primarily during late G(2) and M phases and, in conjunction
Yan Degenhardt et al.
Molecular cancer therapeutics, 9(7), 2079-2089 (2010-06-24)
Polo-like kinases are a family of serine threonine kinases that are critical regulators of cell cycle progression and DNA damage response. Predictive biomarkers for the Plk1-selective inhibitor GSK461364A were identified by comparing the genomics and genetics of a panel of

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