Merck
  • SML1912
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SML1912

Sigma-Aldrich

GSK461364A

≥98% (HPLC)

Synonym(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
Empirical Formula (Hill Notation):
C27H28F3N5O2S
CAS Number:
Molecular Weight:
543.60
MDL番号:
NACRES:
NA.77

品質水準

アッセイ

≥98% (HPLC)

形状

powder

white to beige

溶解性

DMSO: 25 mg/mL, clear

保管温度

2-8°C

SMILES string

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

InChI key

ZHJGWYRLJUCMRT-QGZVFWFLSA-N

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GSK461364A ≥98% (HPLC)

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assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

form

powder

form

powder

form

solid

form

powder

color

white to beige

color

white to beige

color

white

color

white to beige

solubility

DMSO: 25 mg/mL, clear

solubility

DMSO: 20 mg/mL, clear

solubility

DMSO: >10 mg/mL

solubility

DMSO: 20 mg/mL, clear

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

−20°C

storage temp.

2-8°C

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

生物化学的/生理学的作用

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).

保管分類コード

11 - Combustible Solids

WGK

WGK 3

引火点(°F)

Not applicable

引火点(℃)

Not applicable


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