MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

E6201

CAS No. : 603987-35-5

MCE 站：E6201

产品活性：E6201 (ER-806201) 是一种 ATP 竞争性的 MEK1 和 FLT3 双重激酶抑制剂。E6201 抑制 MEK1 诱导的 ERK2 磷酸化，IC₅₀ 值为 5.2 nM，MKK4 诱导的 JNK 磷酸化，IC₅₀ 值为 91 nM，以及 MKK6 诱导的 p38 MAPK 磷酸化，IC₅₀ 值为 19 nM。具有抗肿瘤和抗银屑病功效。

研究领域：MAPK/ERK Pathway  |  Protein Tyrosine Kinase/RTK

作用靶点：MEK  |  FLT3

In Vitro: E6201 is an inhibitor of MEKK1 ａnd MEK families but not the MAPK family. E6201 inhibits MEKK1- induced phosphorylation of MEK1, MKK4, ａnd MKK6 with IC₅₀ values of 31, 522, ａnd 65 nM, respectively. E6201 has no effect on other MAPK family enzymes such as ERK2, JNKs, ａnd p38 MAPK at 10 μM.
E6201 inhibits LPS-induced TNF transcription with an IC₅₀ value of 50±14 nM, but does not suppress β-actin transcription at 3 μM ａnd only slightly at 10 μM.
E6201 inhibits the receptor tyrosine kinases VEGFR2, PDGFR, hepatocyte growth factor receptor, ａnd EGFR with IC₅₀ values of 350, 860, 1100, ａnd 5400 nM, respectively, as well as the nonreceptor tyrosine kinase Syk with an IC₅₀ value of 460 nM. E6201 does not inhibit ZAP-70 or IKK at 10 μM or PKC activity at 100 μM.
E6201 inhibits IL-2 production 48 h after stimulation with the T-cell mitogen PHA-P, with an IC₅₀ value of 18 nM.
E6201 inhibits the proliferation of EGF-stimulated human keratinocytes with an IC₅₀ value of 160 nM.
E6201 suppresses IL-8 production in human keratinocytes 24 h after stimulation with IL-1α or TNFα, with IC₅₀ values of 60 ａnd 30 nM, respectively.
E6201 inhibits TNFα, IL-1, IL-6, ａnd IL-8 production from human PBMCs with IC₅₀ values of 20, 16, 52, ａnd 53 nM, respectively.
E6201 (0.08-20.0 μM) significantly inhibited triple-negative breast cancer (TNBC) cell proliferation ａnd anchorage-independent colony formation in a dose-dependent manner.
E6201 (1 μM) inhibits expression of phospho-ERK ａnd induces G1 phase cell cycle arrest, ａnd apoptosis in TNBC.

In Vivo: E6201 (30 mg/kg; administered via tail vein injection three times per week) inhibits TNBC xenograft tumor growth. E6201 strongly inhibits pERK ａnd Ki-67 expression in xenograft tumor tissues.

相关产品：Sorafenib  |  Trametinib  |  PD98059  |  U0126-EtOH  |  Mirdametinib  |  Cabozantinib  |  Gilteritinib  |  Selumetinib  |  Binimetinib  |  Cobimetinib  |  Quizartinib  |  Fostamatinib  |  R406  |  Crenolanib  |  (E/Z)-Zotiraciclib  |  Pacritinib  |  Isorhamnetin  |  Ripretinib  |  AT9283  |  Lidocaine  |  CA-4948  |  Dovitinib  |  Ro 5126766  |  Sitravatinib  |  Rebastinib  |  BIX02189  |  CI-1040  |  KW-2449

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  染料试剂  |  PROTAC  |  同位素标记物

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Dye Reagents  |  PROTAC  |  Isotope-Labeled Compounds

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。