质量水平
检测方案
≥95% (HPLC)
形式
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
white to off-white
溶解性
DMSO: 20 mg/mL
运输
ambient
储存温度
2-8°C
InChI
1S/C16H14F3IN2O4/c17-11-3-2-10(16(25)22-26-7-9(24)6-23)15(14(11)19)21-13-4-1-8(20)5-12(13)18/h1-5,9,21,23-24H,6-7H2,(H,22,25)/t9-/m1/s1
InChI key
SUDAHWBOROXANE-SECBINFHSA-N
一般描述
一种可渗透细胞的苯甲酰胺化合物，可作为非竞争性，高效，选择性MEK/MAPKK/MKK抑制剂，并有效阻断细胞Erk1/2磷酸化（在血清刺激后血清饥饿的HeLa中降低>90%，在C26中降低50%，分别使用25和0.33 nM抑制剂），而在无细胞激酶测定中，即使在浓度为高10 µM的情况下，对Erk1/2或一组66种其他激酶的活性也影响很小或没有影响。显示可在小鼠中口服使用，并在体内抑制表达BRAF（V600E）的SKMEL28细胞源性肿瘤的生长和Erk磷酸化。
一种可渗透细胞的苯甲酰胺化合物，可作为非竞争性，高效，选择性MEK/MAPKK/MKK抑制剂，并有效阻断细胞Erk1/2磷酸化（在血清刺激后血清饥饿的HeLa中降低>90%，在C26中降低50%，分别使用25和0.33 nM抑制剂），而在无细胞激酶测定中，即使在浓度为高10 µM的情况下，对Erk1/2或一组66种其他激酶的活性也影响很小或没有影响。显示可在小鼠中口服使用，并在体内抑制表达BRAF（V600E）的SKMEL28细胞源性肿瘤的生长和Erk磷酸化。也有InSolution 格式（目录号444968）。
包装
用惰性气体包装
警告
毒性：标准处理（A）
重悬
复溶后，等分并冷冻保存（-20°C）。贮备液在-20°C下可稳定保存至多3个月。
其他说明
Barrett, S.D., et al. 2008.Bioorg.Med. Chem. Lett.18, 6501.
Leyton, J., et al. 2008.Mol.Cancer Ther.7, 3112.
Silva, J., et al. 2008.PLoS Biol.6, 2237.
Ying, Q.L., et al. 2008.Nature453, 519.
Bain, J., et al. 2007.Biochem.J.408, 297.
Solit, D.B., et al. 2006.Nature439, 358.
Leyton, J., et al. 2008.Mol.Cancer Ther.7, 3112.
Silva, J., et al. 2008.PLoS Biol.6, 2237.
Ying, Q.L., et al. 2008.Nature453, 519.
Bain, J., et al. 2007.Biochem.J.408, 297.
Solit, D.B., et al. 2006.Nature439, 358.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
警示用语：
Danger
危险声明
危险分类
Acute Tox. 3 Oral - Aquatic Chronic 4 - STOT RE 2
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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