1. MAPK/ERK Pathway
    Protein Tyrosine Kinase/RTK
  2. MEK
    FLT3
  3. E6201

E6201 (Synonyms: ER-806201)

Cat. No.: HY-15496
Handling Instructions

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.

For research use only. We do not sell to patients.

E6201 Chemical Structure

E6201 Chemical Structure

CAS No. : 603987-35-5

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Description

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].

IC50 & Target

MEK1

5.2 nM (IC50)

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[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.

Cell Viability Assay[2]

Cell Line: Human TNBC cell lines BT20, HCC70, MDA-MB-231, HCC1806, HCC1937, SUM149 and SUM159
Concentration: 0.00, 0.08, 0.16, 0.31, 0.63, 1.25, 2.50, 5.00, 10.0, 20.0 μM
Incubation Time: 5 days
Result: Inhibited TNBC cell proliferation and anchorage-independent colony formation in a dose-dependent manner.

Western Blot Analysis[3]

Cell Line: Human TNBC cell lines BT20, HCC70, MDA-MB-231, HCC1806, HCC1937, SUM149 and SUM159
Concentration: 1 μM
Incubation Time: 0, 1, 24 hours
Result: pERK expression level showed a rapid (apparent by 1 hour) and sustained (still apparent at 24 hours) decrease in the tested TNBC cell lines following treatment.
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[2].

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

Animal Model: Female Nod.Scid gamma mice (age 4 to 6 weeks old) bearing MDA-MB-231-LM2 xenograft tumors[2]
Dosage: 30 mg/kg
Administration: Administered via tail vein injection three times per week for 17 days
Result: Compared with mice treated with vehicle control, the E6201-treated mice showed 60% tumor growth suppression.
Molecular Weight

389.44

Formula

C21H27NO6

CAS No.
SMILES

OC1=C2C(/C=C/C[[email protected]@H]([[email protected]@H](C(/C=C\[[email protected]]([[email protected]@H](OC2=O)C)C)=O)O)O)=CC(NCC)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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