ChemicalBook > CAS DataBase List > GSK461364

GSK461364

Product Name
GSK461364
CAS No.
929095-18-1
Chemical Name
GSK461364
Synonyms
CS-553;GSK4613;GSK461364;GSK-461364;GSK-461364A;GSK461364 USP/EP/BP;GSK461364(GSK-461364);GSK-461364; GSK-461364A;PLK1 inhibitor GS461364;PLK1 inhibitor GSK461364
CBNumber
CB62473747
Molecular Formula
C27H28F3N5O2S
Formula Weight
543.6
MOL File
929095-18-1.mol
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GSK461364 Property

Melting point:
>150°C (dec.)
Boiling point:
658.0±65.0 °C(Predicted)
Density 
1.39
storage temp. 
Hygroscopic, -20°C Freezer, Under inert atmosphere
solubility 
Chloroform (Slightly), DMSO (Slightly), Methanol (Slightly)
pka
15.16±0.50(Predicted)
form 
Solid
color 
Off-White to Light Beige
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical
Product number
18099
Product name
GSK461364
Purity
≥95%
Packaging
1mg
Price
$34
Updated
2024/03/01
Cayman Chemical
Product number
18099
Product name
GSK461364
Purity
≥95%
Packaging
5mg
Price
$117
Updated
2024/03/01
Cayman Chemical
Product number
18099
Product name
GSK461364
Purity
≥95%
Packaging
10mg
Price
$216
Updated
2024/03/01
Cayman Chemical
Product number
18099
Product name
GSK461364
Purity
≥95%
Packaging
25mg
Price
$493
Updated
2024/03/01
TRC
Product number
G797705
Product name
GSK461364
Packaging
2.5mg
Price
$50
Updated
2021/12/16
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GSK461364 Chemical Properties,Usage,Production

Uses

GSK 461364 is a dose-dependant inhibitor of proliferating cancer cell lines as well as an apoptotic agent at higher dosage levels.

Definition

ChEBI: 5-[6-[(4-methyl-1-piperazinyl)methyl]-1-benzimidazolyl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]-2-thiophenecarboxamide is a member of (trifluoromethyl)benzenes.

Biological Activity

gsk461364 is a potent and reversible atp competitive plk1 inhibitor. polo-like kinases (plk) are a family of serine threonine kinases that are critical regulators of dna damage response and cell cycle progression.

in vitro

gsk461364 showed at least 390-fold greater selectivity for plk1 than for plk2 and plk3 and 1,000-fold greater than for 48 other kinases. the drug showed antiproliferative activity against multiple (>120) tumor cell lines and potently inhibited the proliferation of greater than 83% and 91% of these cell lines [1].

in vivo

intraperitoneal administration of gsk461364 caused regression or tumor growth delay in different xenograft models. in vivo suppression of plk1 by using gsk461364 resulted in mitotic arrest with aberrant mitotic figures consisting of monopolar or collapsed mitotic spindles [1].

target

PLK1

References

[1] olmos d, barker d, sharma r, brunetto at, yap ta, taegtmeyer ab, barriuso j, medani h, degenhardt yy, allred aj, smith da, murray sc, lampkin ta, dar mm, wilson r, de bono js, blagden sp. phase i study of gsk461364, a specific and competitive polo-like kinase 1 inhibitor, in patients with advanced solid malignancies. clin cancer res. 2011 may 15;17(10):3420-30.

GSK461364 Preparation Products And Raw materials

Raw materials

Preparation Products

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GSK461364 Suppliers

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View Lastest Price from GSK461364 manufacturers

Career Henan Chemical Co
Product
GSK-461364 929095-18-1
Price
US $1.00/g
Min. Order
1g
Purity
99%
Supply Ability
1ton
Release date
2020-01-10

929095-18-1, GSK461364Related Search:


  • (R)-5-(6-((4-methylpiperazin-1-yl)methyl)-1H-benzo[d]imidazol-1-yl)-3-(1-(2-(trifluoromethyl)phenyl)ethoxy)thiophene-2-carboxamide
  • GSK-461364A
  • GSK461364(GSK-461364)
  • 5-[6-[(4-Methyl-1-piperazinyl)methyl]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]
  • 5-[6-[(4-Methyl-1-piperazinyl)methyl]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phen
  • GSK461364
  • GSK-461364
  • GSK4613
  • GSK461364, 98%, a potent Polo-like kinase 1 (PLK1) inhibitor
  • 5-[6-[(4-methyl-1-piperazinyl)methyl]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]-2-Thiophenecarboxamide
  • GSK-461364; GSK-461364A
  • PLK1 inhibitor GS461364
  • CS-553
  • 2-Thiophenecarboxamide, 5-[6-[(4-methyl-1-piperazinyl)methyl]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]-
  • GSK461364 USP/EP/BP
  • PLK1 inhibitor GSK461364
  • 5-[6-[(4-methylpiperazin-1-yl)methyl]benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
  • 929095-18-1
  • C27H28F3N5O2S
  • Inhibitors
  • APIs