产品名称

英文名称：Selumetinib (AZD6244)

同义词

Selumetinib、606143-52-6、AZD6244、ARRY-142886、AZD 6244、5-[(4-BROMO-2-CHLOROPHENYL)AMINO]-4-FLUORO-N-(2-HYDROXYETHOXY)-1-METHYL-1H-BENZIMIDAZOLE-6-CARBOXAMIDE、AZD-6244、ARRY 142886、Selumetinib (AZD6244)、ARRY-886、AZD6244 (Selumetinib)、selumetinibum、UNII-6UH91I

产品性质

CAS编号：606143-52-6

分子式：C17H15BrClFN4O3

分子量：457.69

PubChem编号：10127622

英文别名：Selumetinib|606143-52-6|AZD6244|ARRY-142886|AZD 6244|5-[(4-BROMO-2-CHLOROPHENYL)AMINO]-4-FLUORO-N-(2-HYDROXYETHOXY)-1-METHYL-1H-BENZIMIDAZOLE-6-CARBOXAMIDE|AZD-6244|ARRY 142886|Selumetinib (AZD6244)|ARRY-886|AZD6244 (Selumetinib)|selumetinibum|UNII-6UH91I

规格或纯度：≥99%

英文名称：Selumetinib (AZD6244)

生化机理：Selumetinib is a non-ATP competitive inhibitor of MEK-1 (IC50 = 14 nM). This compound inactivates the phosphorylation of ERK1/2 (IC50 < 40 nM). Selumetinib has little effect on p38, c-Jun-NH2-kinase, or the MEK/ERK5 pathways.Potent, selective, non-ATP competitive MEK1/2 inhibitor (IC 50 MEK1 = 14 nM).\xa0Also inhibits\xa0ERK1/2 phosphorylation.

储存温度：-20°C储存

运输条件：超低温冰袋运输

备注：如果有可能，您尽量在使用的当天配置溶液，并在当天使用完它。但是，如果您需要预先配制储备溶液，我们建议您将溶液等份保存在-20°C的密封小瓶中。通常，它们最多可以使用一个月。在使用前和打开样品瓶之前，我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度，用法和处理的建议吗？请访问我们的常见问题（FAQ）页面以获取更多详细信息。

产品介绍：Selumetinib (AZD6244)是一种有效，高选择性的MEK1抑制剂，IC50为14 nM，也抑制ERK1/2磷酸化，IC50为10 nM，对p38α， MKK6， EGFR， ErbB2， ERK2， B-Raf等没有抑制作用。Phase 3。A MEK-1 non-ATP competitive inhibitor.Selumetinib (AZD6244) is a potent, highly selective MEK1 inhibitor with IC50 of 14 nM, also inhibits ERK1/2 phosphorylation with IC50 of 10 nM, no inhibition to p38α, MKK6, EGFR, ErbB2, ERK2, B-Raf, etc. Phase 3.A MEK-1 non-ATP competitive inhibitor.

ALogP：3.6

IUPAC Name：6-(4-bromo-2-chloroanilino)-7-fluoro-N-(2-hydroxyethoxy)-3-methylbenzimidazole-5-carboxamide

INCHI：InChI=1S/C17H15BrClFN4O3/c1-24-8-21-16-13(24)7-10(17(26)23-27-5-4-25)15(14(16)20)22-12-3-2-9(18)6-11(12)19/h2-3,6-8,22,25H,4-5H2,1H3,(H,23,26)

InChi Key：CYOHGALHFOKKQC-UHFFFAOYSA-N

Canonical SMILES：CN1C=NC2=C1C=C(C(=C2F)NC3=C(C=C(C=C3)Br)Cl)C(=O)NOCCO

Isomeric SMILES：CN1C=NC2=C1C=C(C(=C2F)NC3=C(C=C(C=C3)Br)Cl)C(=O)NOCCO

PubChem CID：10127622

Wikipedia：Selumetinib

DiscoveRx TREEspot：AZD-6244/ARRY-886|

ChEMBL Ligand：CHEMBL1614701

RCSB PDB Ligand：3EW

Reactome Reaction：R-HSA-9657606

溶解性：Soluble in DMSO (92 mg/ml at 25 °C), water (<1 mg/ml at 25 °C), and ethanol (<1 mg/ml at 25 °C).

象形图：

信号词：Danger

危险声明：H373 Causes damage to organs through prolonged or repeated exposureH411 Toxic to aquatic life with long lasting effectsH318 Causes serious eye damageH317 May cause an allergic skin reactionH361 Suspected of damaging fertility or the unborn child

预防措施声明：P261,P273,P280,P302+P352,P321,P405,P501,P260,P272,P333+P313,P362+P364,P391,P203,P264+P265,P305+P354+P338,P318,P317,P319

产品包装