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现货供应GDC-0879
产品型号：C13706
英文简称：
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产品详情
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.