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现货供应GDC-0879

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产品名称: 现货供应GDC-0879
产品型号: C13706
产品展商: Chembest
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简单介绍

Chemical Name: 5-[1-(2-Hydroxy-ethyl)-3-pyridin-4-yl-1H-pyrazol-4-yl]-indan-1-one oxime 英文名:GDC-0879 分子式:C19H18N4O2 分子量:334.37 纯度:>99% CAS:905281-76-7


现货供应GDC-0879  的详细介绍
Chemical Name: 5-[1-(2-Hydroxy-ethyl)-3-pyridin-4-yl-1H-pyrazol-4-yl]-indan-1-one oxime
英文名:GDC-0879
分子式:C19H18N4O2
分子量:334.37
纯度:>99%
CAS:905281-76-7
Biological Activity:
Selective inhibitor of protein kinase, targeting B-Raf (V600E).GDC-0879 is a highly selective, novel potent, orally bioavailable B-Raf inhibitor in various in vitro and cell-based assays with an IC50 estimate of 0.13 nM against purified B-Raf V600E enzyme and a cellular pERK IC50 of 63 nM in the MALME-3M cell line.For this compound, subnanomolar enzyme potency translated into very effective reduction of cellular viability of BRAF-mutant Malme3M cells (EC50 values were 0.75 umol/L for GDC-0879).In GDC-0879-treated mice, both cell line- and patient-derived BRAFV600E tumors exhibited stronger and more sustained pharmacodynamic inhibition (>90% for 8 hours) and improved survival compared with mutant KRAS-expressing tumors.
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