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My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > MAPK > GDC-0879CAS：905281-76-7
Molecular Formula：C19H18N4O2
Molecular Weight：334.37
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
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| CAS | 905281-76-7 |
| Name | GDC-0879 |
| Molecular Formula | C19H18N4O2 |
| Molecular Weight | 334.37 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| SMILES | O/N=C1C(C=CC(C2=CN(CCO)N=C2C3=CC=NC=C3)=C4)=C4CC/1 |
| Target Point | Raf |
| Passage | MAPK |
| Background | GDC-0879 is a potent and selective B-Raf inhibitor. |
| Biological Activity | GDC-0879 是一种有效的选择性 B-Raf 抑制剂，IC50 为 0.13 nM[1-2]。 |
| IC50 | B-Raf:0.13nM(IC50)[1-2] |
| In Vitro | GDC-0879也抑制pERK，IC50为63 nM [1]。 GDC-0879代表了一种新的有效和选择性B-Raf抑制剂，正被评估为潜在的抗肿瘤剂。 GDC-0879在V600E B-Raf突变细胞系中显示出对Raf/MEK/ERK信号传导途径的有效抑制，其中低细胞pMEK1抑制IC50估计分别在A375黑素瘤和Colo205结肠癌细胞中为59和29nM [2]。 |
| In Vivo | 在小鼠MCT中口服施用15，25，50，100和200mg/kg后，GDC-0879的药代动力学参数估计如下：ka = 8.20h -1，ke = 0.59h -1，表观体积分布= 6.19 L/kg [2]。 |
| Cell Experiment | 使用A375和Colo205细胞测定GDC-0879对pMEK抑制的体外IC 50估计。简言之，将A375或Colo205细胞与一系列GDC-0879浓度(0.5nM至6.75μM)孵育25分钟。裂解细胞，裂解物在16，100g离心30分钟，测定总蛋白水平。酶联免疫吸附测定试剂盒用于测定96孔格式的pMEK1和总MEK1蛋白水平。一式两份地分析样品，每孔20μg蛋白质。使用用重组pMEK1或MEK1测定的标准曲线，将450nm处获得的光密度转换为每毫升(对于pMEK1)或毫微克/毫升(对于总MEK1)的单位。然后将pMEK1 /总MEK1比率计算为每纳克单位。使用GraphPad Prism 4.02版[2]通过非线性回归估计pMEK1抑制的IC50估计值。 |
| Animal Experiment | 小鼠[2]雌性无胸腺nu/nu小鼠(体重25-28g)口服剂量为15，25，50，100和200mg/kg GDC-0879。在给药后0.5，1，2，4，8和24小时通过心脏穿刺(末端收集)收集血液样品(~1mL)到含有K2EDTA抗凝血剂的管中。收集后立即将血液与K2EDTA混合并储存在冰上。在30分钟内，将血液样品在4℃下以约1000至1500g离心5分钟，并收获血浆。将血浆样品储存在-80°C直至分析[2]。 |
| Data Literature Source | [1]. Hansen JD，et al. Potent and selective pyrazole-based inhibitors of B-Raf kinase. Bioorg Med Chem Lett. 2008 Aug 15;18(16):4692-5. [2]. Wong H，et al. Pharmacodynamics of 2-[4-[(1E)-1-(hydroxyimino)-2，3-dihydro-1H-inden-5-yl]-3-(pyridine-4-yl)-1H-pyrazol-1-yl]ethan-1-ol (GDC-0879)，a potent and selective B-Raf kinase inhibitor: understanding relationships between systemic concentrations，phosphorylated mitogen-activated protein kinase kinase 1 inhibition，and efficacy. J Pharmacol Exp Ther. 2009 Apr;329(1):360-7. |
| Unit | Bottle |
| Specification | 2mg 5mg |
GDC-0879 是一种有效的选择性 B-Raf 抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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