660868-91-7 Usage
Uses
Used in Oncology:
GW843682 is used as a PLK1 and PLK3 inhibitor for the treatment of various types of cancer. It has shown efficacy in inhibiting the growth of multiple cancer cell lines, including human uterine sarcoma cells, drug-resistant cells, and patient-derived leukemia cells. GW843682, 5-(5,6-Dimethoxy-1H-benzimidazol-1-yl)-3-[2-(trifluoromethyl)-benzyl]oxythiophene-2-carboxamide's ability to induce cell cycle arrest and apoptosis makes it a promising therapeutic agent for cancer treatment.
Used in Drug Resistance Research:
GW843682 is used as a tool in studying the mechanisms of drug resistance in cancer cells. Its ability to inhibit the growth of drug-resistant cancer cells, such as the P-glycoprotein-expressing MES-SA/Dx5 subline, provides insights into the development of strategies to overcome drug resistance in cancer treatment.
Used in Cancer Cell Line Screening:
GW843682 is used as a screening agent to evaluate the sensitivity of various cancer cell lines to PLK inhibition. Its potency and selectivity for PLK1 and PLK3 make it a valuable tool for identifying cancer cells that are dependent on these kinases for their growth and survival.
Used in Cancer Cell Cycle and Apoptosis Studies:
GW843682 is used as a research compound to investigate the role of PLK1 and PLK3 in the regulation of the cell cycle and apoptosis in cancer cells. Its ability to induce G2/M cell cycle arrest and apoptosis in cancer cells provides valuable information on the molecular mechanisms underlying the anti-cancer effects of PLK inhibition.
Biological Activity
Selective inhibitor of polo-like kinase 1 (PLK1) and polo-like kinase 3 (PLK3) (IC 50 values are 2.2 and 9.1 nM respectively). Displays > 100-fold selectivity over ~30 other kinases tested including cdk1 and cdk2. Inhibits proliferation of most tumor cells in vitro and is selective over normal diploid fibroblasts.
Check Digit Verification of cas no
The CAS Registry Mumber 660868-91-7 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 6,6,0,8,6 and 8 respectively; the second part has 2 digits, 9 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 660868-91:
(8*6)+(7*6)+(6*0)+(5*8)+(4*6)+(3*8)+(2*9)+(1*1)=197
197 % 10 = 7
So 660868-91-7 is a valid CAS Registry Number.
660868-91-7Relevant articles and documents
Discovery of thiophene inhibitors of polo-like kinase
Emmitte, Kyle A.,Andrews, C. Webb,Badiang, Jennifer G.,Davis-Ward, Ronda G.,Dickson, Hamilton D.,Drewry, David H.,Emerson, Holly K.,Epperly, Andrea H.,Hassler, Daniel F.,Knick, Victoria B.,Kuntz, Kevin W.,Lansing, Timothy J.,Linn, James A.,Mook Jr., Robert A.,Nailor, Kristen E.,Salovich, James M.,Spehar, Glenn M.,Cheung, Mui
scheme or table, p. 1018 - 1021 (2009/09/06)
The discovery and development of a series of thiophenes as potent and selective inhibitors of PLK is described. Identification and characterization of 2, a useful in vitro PLK inhibitor tool compound, is also presented.
THIOPHENE COMPOUNDS
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Page 124-125, (2008/06/13)
The present invention provides compounds of formula (I): (I) pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.
