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- 2025年12月05日
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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 英文名：
BAY 869766; RDEA119
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
923032-37-5
- 规格：
10 mM * 1 mL/5 mg/10 mg/50 mg/100 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥937.0 |
|---|---|---|---|
| 规格： | 5 mg | 产品价格： | ￥744.0 |
| 规格： | 10 mg | 产品价格： | ￥1116.0 |
| 规格： | 50 mg | 产品价格： | ￥2720.0 |
| 规格： | 100 mg | 产品价格： | ￥4836.0 |
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Refametinib
CAS No. : 923032-37-5
MCE 国际站：Refametinib
产品活性：Refametinib (BAY 869766; RDEA119) 是一种口服有效，非ATP竞争的，选择性 MEK1/MEK2 变构抑制剂，IC50 分别为 19 nM 和 47 nM。
研究领域：MAPK/ERK Pathway
作用靶点：MEK
In Vitro: Refametinib (BAY 869766; RDEA119) selectively binds directly to an allosteric pocket in the MEK1/2 enzymes. Refametinib potently inhibits MEK activity in enzyme inhibition assays in a non-ATP-competitive manner (MEK1 IC50=19 nM, MEK2 IC50=47 nM) determined through incorporation of radioactive phosphate from ATP into ERK as substrate. Refametinib potently inhibits MEK activity as measured by phosphorylation of ERK1/2 across several human cancer cell lines of different tissue origins and BRAF mutational status with EC50 values ranging from 2.5 to 15.8 nM. Refametinib inhibits anchorage-dependent growth of human cancer cell lines harboring the gain-of-function V600E BRAF mutant with GI50 values ranging from 67 to 89 nM. In contrast, Refametinib has significantly less growth-inhibitory potency against cell lines with wild-type BRAF (A431 cells) or MDA-MB-231 cells harboring a BRAF mutation G464V that shows minimal (<2-fold increase) enhancement of inherent kinase activity. Under anchorage-independent conditions, GI50 values for all cell lines tested are similar (40-84 nM). MDA-MB-231 and A431 cells are significantly more sensitive to Refametinib under anchorage-independent conditions.
In Vivo: Refametinib (BAY 869766; RDEA119) is an orally available, potent, non-ATP-competitive, highly selective inhibitor of MEK1/2, which is active in human tumor xenograft models and is well tolerated within the therapeutic exposure range in animals.
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文献和实验能力有关。因此，损伤显现的快慢，至少部分地与组织的增殖活力有关。增殖活跃的组织，如消化道粘膜、骨髓和皮肤表皮等损伤显现得早，而由缓慢增殖细胞组成的组织如中枢神经系统和周围神经系统、肾、真皮、软骨和骨显现损伤慢。这些组织的损伤主要与其中靶细胞的枯竭有关。 (三)放射线杀伤细胞的程度与剂量的大小有关，这种量效关系可用细胞存活曲线来表示。它的特点可用下列参数来描述：D。值是曲线直线部分，使细胞存活下降到．照射前37％所需的剂量，亦称为平均致死剂量；外推值n和准阈剂量D，是反映肩区大小的参数；初始斜率D：是指存活
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