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化驗
≥98% (HPLC)
形狀
solid
顏色
off-white
溶解度
DMSO: >10 mg/mL
起源
GlaxoSmithKline
儲存溫度
2-8°C
SMILES 字串
COc1cc2ncn(-c3cc(OCc4ccccc4C(F)(F)F)c(s3)C(N)=O)c2cc1OC
InChI
1S/C22H18F3N3O4S/c1-30-16-7-14-15(8-17(16)31-2)28(11-27-14)19-9-18(20(33-19)21(26)29)32-10-12-5-3-4-6-13(12)22(23,24)25/h3-9,11H,10H2,1-2H3,(H2,26,29)
InChI 密鑰
JSKUWFIZUALZLX-UHFFFAOYSA-N
應用
GW843682X has been used as a polo-like kinase-1 (PLK1) inhibitor:
- to study the influence of PLK1 inhibition on Wee1 (G2 check point kinase), cyclin-dependent protein kinase 1 (Cdc2)–Yp15, expression in melanoma cells
- to determine if PLK1 inhibition decreased the survival of hamartin and tuberin deficient cells
- to investigate if inhibitors of PLK1 and aurora kinases have a synergistic antimitotic impact in HeLa cells
生化／生理作用
GW843682X is an anti-cancer compound. It can improve the ability of vincristine to promote growth arrest and apoptosis in leukemia cells. GW843682X is capable of disturbing the formation of spindles and terminate mitoses in lung adenocarcinoma cells.
GW843682X is a polo-like kinase-1 (PLK1) and polo-like kinase-3 (PLK3) inhibitor with nanomolar activity. It shows potent inhibition of proliferation of a wide variety of tumor cell lines.
特點和優勢
This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
個人防護裝備
dust mask type N95 (US), Eyeshields, Gloves
Timothy J Lansing et al.
Molecular cancer therapeutics, 6(2), 450-459 (2007-02-03)
Polo-like kinase 1 (PLK1) plays key roles in the regulation of mitotic progression, including mitotic entry, spindle formation, chromosome segregation, and cytokinesis. PLK1 expression and activity are strongly linked to proliferating cells. Many studies have shown that PLK1 expression is
Julio Vera et al.
Cellular signalling, 27(5), 951-960 (2015-02-17)
In the present report, the role of ATR-Chk1-Wee1 and ATM-Chk2-p53-p21 pathways in stress-induced cell cycle control is analysed in melanoma cells. Treatment of p53 wild-type melanoma cells with the genotoxic agent doxorubicin induces G2-M arrest, inhibitory phosphorylation of cell cycle
T Ikezoe et al.
Leukemia, 23(9), 1564-1576 (2009-05-08)
Polo-like kinase1 (PLK1) belongs to the family of serine/threonine kinases and plays an important role in centrosome maturation, bipolar spindle formation, and cytokinesis during mitosis. We found in this study that PLK1 was aberrantly highly expressed in a variety of
Jingjing Li et al.
Oncotarget, 6(11), 9327-9340 (2015-04-15)
Mitosis is choreographed by a number of protein kinases including polo-like kinases and Aurora kinases. As these kinases are frequently dysregulated in cancers, small-molecule inhibitors have been developed for targeted anticancer therapies. Given that PLK1 and Aurora kinases possess both
Matthildi Valianou et al.
Cell cycle (Georgetown, Tex.), 14(3), 399-407 (2015-01-08)
The mechanistic target of rapamycin complex 1 (mTORC1) increases translation, cell size and angiogenesis, and inhibits autophagy. mTORC1 is negatively regulated by hamartin and tuberin, the protein products of the tumor suppressors TSC1 and TSC2 that are mutated in Tuberous
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