929095-18-1 Usage
Description
GSK461364 is a chemical compound that acts as a dose-dependent inhibitor of proliferating cancer cell lines and an apoptotic agent at higher dosage levels. It has the potential to target and suppress the growth of cancer cells, making it a promising candidate for cancer treatment and research.
Uses
Used in Oncology:
GSK461364 is used as an anticancer agent for its ability to inhibit the proliferation of cancer cells in a dose-dependent manner. It targets various cancer cell lines and can induce apoptosis at higher dosage levels, offering a potential therapeutic approach for cancer treatment.
Used in Cancer Research:
GSK461364 is utilized as a research tool to study the mechanisms of cancer cell growth inhibition and apoptosis. Its dose-dependent effects on cancer cells provide valuable insights into the development of novel cancer therapies and the understanding of cancer biology.
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].
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.
Check Digit Verification of cas no
The CAS Registry Mumber 929095-18-1 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 9,2,9,0,9 and 5 respectively; the second part has 2 digits, 1 and 8 respectively.
Calculate Digit Verification of CAS Registry Number 929095-18:
(8*9)+(7*2)+(6*9)+(5*0)+(4*9)+(3*5)+(2*1)+(1*8)=201
201 % 10 = 1
So 929095-18-1 is a valid CAS Registry Number.
929095-18-1Relevant articles and documents
Regioselective synthesis of benzimidazole thiophene inhibitors of polo-like kinase 1
Hornberger, Keith R.,Badiang, Jennifer G.,Salovich, James M.,Kuntz, Kevin W.,Emmitte, Kyle A.,Cheung, Mui
scheme or table, p. 6348 - 6351 (2009/04/07)
A regioselective synthesis of novel 1-(2-thienyl)-benzimidazole inhibitors of polo-like kinase 1 is described. Amination of substituted 2-iodo or -bromo nitrobenzenes with a 2-aminothiophene derivative catalyzed by Pd2dba3 and XANTPH
BENZIMIDAZOLE THIOPHENE COMPOUNDS
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Page/Page column 59, (2010/11/26)
The present invention provides benzimidazole thiophene compounds pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.
