Selumetinib
Cat. No.：YN350209
CAS No. ：606143-52-6
| 产品名称: | Selumetinib |
| CAS No.: | 606143-52-6 |
| Chemical Name: | 5-[(4-bromo-2-chlorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzimidazole-6-carboxamide |
| Synonyms: | 司美替尼; AZD6244; ARRY-142886 |
| 分子量: | 457.68 |
| 分子式: | C₁₇H₁₅BrClFN₄O₃ |
| SMILES: | O=C(C1=C(C(F)=C2N=CN(C2=C1)C)NC3=CC=C(C=C3Cl)Br)NOCCO |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | Selumetinib (AZD6244) 是一种高效选择性的，非 ATP 竞争性的MEK1/2抑制剂， 抑制 MEK1 的IC50为14 nM。Selumetinib (AZD6244) 抑制 MEK1/2 磷酸化水平。 |
| IC50和靶点: | [{name:"MEK:12 nM (IC50)"},{name: "MEK1:14 nM (IC50)'}, 'MEK2'] |
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Yeh, T.C., Marsh, V., Bernat, B.A., et al.Biological characterization of ARRY-142886 (AZD6244), a potent, highly selective mitogen-activated protein kinase kinase 1/2 inhibitorClin. Cancer Res.13(5),1576-1583(2007)
Davis, M.I., Hunt, J.P., Herrgard, S., et al.Comprehensive analysis of kinase inhibitor selectivityNat. Biotechnol.29(11),1046-1051(2011)
Huynh, H., Soo, K.C., Chow, P.K.H., et al.Targeted inhibition of the extracellular signal-regulated kinase kinase pathway with AZD6244 (ARRY-142886) in the treatment of hepatocellular carcinomaMol. Cancer Ther.6(1),138-146(2007)
Davies, B.R., Logie, A., McKay, J.S., et al.AZD6244 (ARRY-142886), a potent inhibitor of mitogen-activated protein kinase/extracellular signal-regulated kinase kinase 1/2 kinases: mechanism of action in vivo, pharmacokinetic/pharmacodynamic relationship, and potential for combination in preclinical modelsMol. Cancer Ther.6(8),2209-2219(2007)
Corcoran, R.B., Cheng, K.A., Hata, A.N., et al.Synthetic lethal interaction of combined BCL-XL and MEK inhibition promotes tumor regressions in KRAS mutant cancer modelsCancer Cell23(1),121-128(2013)
Robert, C., Dummer, R., Gutzmer, R., et al.Selumetinib plus dacarbazine versus placebo plus dacarbazine as first-line treatment for BRAF-mutant metastatic melanoma: A phase 2 double-blind randomised studyLancet Oncol.14(8),733-740(2013)
