Skip to Content
Merck
CN

Key Documents

View All Documentation

SML1912

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

Sign In to View Organizational & Contract Pricing.

Select a Size

Change View

About This Item

Empirical Formula (Hill Notation):
C27H28F3N5O2S
CAS Number:
929095-18-1
Molecular Weight:
543.60
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD12755419
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
100
Technical Service
Need help? Our team of experienced scientists is here for you.
Let Us Assist

Quality Level

100

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 25 mg/mL, clear

storage temp.

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

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.
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).

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Choose from one of the most recent versions:

Certificates of Analysis (COA)

Lot/Batch Number

It looks like we've run into a problem, but you can still download Certificates of Analysis from our Documents section.

If you need assistance, please contact Customer Support

Already Own This Product?

Find documentation for the products that you have recently purchased in the Document Library.

Visit the Document Library

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

Global Trade Item Number

SKUGTIN
SML1912-25MG04061832452463
SML1912-5MG04061832452470