GSK-461364

Chemical Information
Product Name GSK-461364 CAS No. 929095-18-1
Molecular Weight 543.60 Molecular Formula C27H28F3N5O2S
MOQ 100g Brand Biolang

Product Description

GSK461364 is a potent Polo-like kinase 1 (PLK1) inhibitor with a Ki value of 2.2 nM.
GSK461364 inhibits cancer cell line proliferation from multiple origins with minimal toxicity in nondividing human cells. RNA silencing of WT p53 increases the antiproliferative activity of GSK461364. As many cancer therapies tend to be more effective in p53 WT patients, the higher sensitivity of p53-deficient tumors toward GSK461364 can potentially offer an opportunity to treat tumors that are refractory to other chemotherapies as well as early line therapy for these genotypes. GSK461364 is a thiophene amide that inhibits purified Plk1 enzyme in vitro with a Ki of 2 nM and has >100-fold selectivity for Plk1 compared with Plk2 and Plk3. GSK461364 is a potent inhibitor of cell proliferation causing 50% growth inhibition (GI50) below 100 nM in most of the cell lines tested with limited toxicity against human nonproliferating cells. Inhibition of cell cycle progression is concentration dependent with initial delay at G2 phase at high GSK461364 concentrations and arrest at M phase at lower concentrations. Currently, GSK461364 is in a dose-escalation first-time-in-human trial. Cell lines with mutations in the TP53 gene tended to be more sensitive to GSK461364, and that inhibiting the p53 response by RNA silencing confers increased sensitivity in some p53 wild-type (WT) cells. Furthermore, these more sensitive cell lines also have increased levels of chromosome instability, a characteristic associated with TP53 mutations. In preclinical testing, GSK461364 shows antiproliferative activity against multiple (>120) tumor cell lines and potently inhibits the proliferation of greater than 83% and 91% of these cell lines, with IC50 values lower than 50 and 100 nM, respectively.

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About Biolang

Shanghai Biolang Bio-Tech Co., Ltd., founded in 2004, located in Shanghai and Nanjing, R&D and logistics center located in Wuhan National Bioindustry Base,the production base in Luotian, Tongshan, Dongying, Pingxiang.Biolang is specialized manufacturer and supplier of New-Type pharmaceutical Raw Materials and Pharmaceutical Intermediates.