MEK
The mitogen-activated protein kinases (MAPKs) mediate intracellular signals activated by a wide variety of extracellular stimuli. These serine/threonine kinase are activated by MEK 1/2, MEK3/6, MEK4/7 and MEK5, respectively. The RAS-RAF-MEK1/2 pathway is commonly activated by various extracellular stimuli, growth factors, hormones, cytokines and environmental stresses, leading to distinct intracellular responses via either a series of phosphorylation events and of protein-protein interactions involving RAS, RAF, ERK and MEK. The activation of the RAS-RAF-MEK-MAPK pathway culminates in the regulation of gene transcription promoting cancer cell proliferation, survival, migration and angiogenesis. Genes encoding RAS or BRAF, when mutated or amplified, activate MAPK signalling through MEK, making MEK an attractive target for anti-cancer drug development. Whereas MEK is not frequently found mutated in solid tumours, BRAF is mutated in about 20% of all cancers and in approximately 40 to 60% of melanomas; furthermore, KRAS or NRAS mutations have been found in about 55% of metastatic CRC (mCRC). Lower rate of BRAF mutations have been observed in lung cancer (2-4%) whereas KRAS mutations remain the most frequent alteration in lung cancer, with an average mutation rate of 20-30% in adenocarcinoma. MEK1/2 act as a transducer of the growth factor receptorRAS-RAF-MAPK signalling cascade and its role in cancer development and progression in selected human cancers, such as NSCLC and CRC.
References
1.Martinelli E, et al. Cancer Treat Rev. 2017;53:61–69.
References
1.Martinelli E, et al. Cancer Treat Rev. 2017;53:61–69.
MAPK/ERK Signaling
MEK
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Nedometinib
产品货号 : M37153
cas no: 2252314-46-6
Nedometinib 是一种针对 MEK1 的酪氨酸激酶抑制剂。Nedometinib具有抗肿瘤作用,可用于皮肤病、皮肤纤维神经瘤、神经纤维瘤病的研究。 -
MEK-IN-4
产品货号 : M34333
cas no: 297744-42-4
MEK-IN-4 是一种 MEK 抑制剂。MEK-IN-4 可用于炎症性疾病和癌症的研究。 -
MEK inhibitor
产品货号 : M33014
cas no: 334951-92-7
MEK inhibitor 是一种 MEK 抑制剂,具有抗肿瘤活性。 -
PD 198306
产品货号 : M27491
cas no: 212631-61-3
PD 198306 是一种选择性 MAPK/ERK 激酶 (MEK) 抑制剂,具有抗痛觉过敏作用。 PD 198306 可降低链脲佐菌素 (Streptozocin) 诱导的活性 ERK1 水平的增加。 -
PD184161
产品货号 : M27439
cas no: 212631-67-9
PD184161 是一种新型口服 MEK 抑制剂。