E6201  (Synonyms: ER-806201)

E6201 (ER-806201) is an ATP-competitive dual kinase inhibitor of MEK1 and FLT3. E6201 inhibits MEK1- induced ERK2 phosphorylation with an IC₅₀ value of 5.2 nM, MKK4-induced JNK phosphorylation with an IC₅₀ value of 91 nM, and MKK6-induced p38 MAPK phosphorylation with an IC₅₀ value of 19 nM. Anti-tumor and anti-psoriasis efficacy^[1][2].

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^[1].
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^[1].
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^[1].
E6201 inhibits IL-2 production 48 h after stimulation with the T-cell mitogen PHA-P, with an IC₅₀ value of 18 nM^[1].
E6201 inhibits the proliferation of EGF-stimulated human keratinocytes with an IC₅₀ value of 160 nM^[1].
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^[1].
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^[1].
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^[2].
E6201 (1 μM) inhibits expression of phospho-ERK and induces G1 phase cell cycle arrest, and apoptosis in TNBC^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

389.44

C₂₁H₂₇NO₆

603987-35-5

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Masaki Goto, et al. E6201 [(3S,4R,5Z,8S,9S,11E)-14-(ethylamino)-8, 9,16-trihydroxy-3,4-dimethyl-3,4,9,19-tetrahydro-1H-2-benzoxacyclotetradecine-1,7(8H)-dione], a novel kinase inhibitor of mitogen-activated protein kinase/extracellular signal-regulated ki  [Content Brief]

  [2]. Jangsoon Lee, et al. Anti-tumor and anti-metastasis efficacy of E6201, a MEK1 inhibitor, in preclinical models of triple-negative breast cancer. Breast Cancer Res Treat. 2019 Jun;175(2):339-351.  [Content Brief]