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- 2025年12月05日
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- 英文名：
ER-806201
- 库存：
货期：询盘
- 供应商：
MedChemExpress LLC
- CAS号：
603987-35-5
- 规格：
询盘
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E6201
CAS No. : 603987-35-5
MCE 国际站：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
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.
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