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GSK461364A

SIGMA/SML1912 - ≥98% (HPLC)

Synonym: (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

CAS Number: 929095-18-1
Empirical Formula (Hill Notation): C27H28F3N5O2S
Molecular Weight: 543.60
MDL Number: MFCD12755419
Linear Formula: C27H28F3N5O2S
Product Type: Chemical
Catalog Number PKG Qty. Price Quantity
45-SML1912-5MG 5 mg
 $123.00
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This image depicts SML1912-5MG.

 

assay ≥98% (HPLC)
color white to beige
form powder
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
Quality Level 100 
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
solubility DMSO: 25 mg/mL, clear
storage temp. 2-8°C
Biochem/physiol Actions: A potent, reversible, ATP-competitive, and highly selective polo-like kinase 1 (Plk1) inhibitor with in vitro and in vivo anti-cancer efficacy.
Biochem/physiol Actions: 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).
RIDADR NONH for all modes of transport
WGK Germany WGK 3
Flash Point(F) Not applicable
Flash Point(C) Not applicable
Purity ≥98% (HPLC)
Storage Temp. 2-8°C
UNSPSC 12352200

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