E6201

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].

Product Specifications

CAS Number

[603987-35-5]

Product Name Alternative

ER-806201

UNSPSC

12352005

Target

FLT3; MEK

Type

Reference compound

Related Pathways

MAPK/ERK Pathway; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/e6201.html

Solubility

10 mM in DMSO

Smiles

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

Molecular Formula

C21H27NO6

Molecular Weight

389.44

References & Citations

[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 kinase kinase (MEK) -1 and MEK kinase-1: in vitro characterization of its anti-inflammatory and antihyperproliferative activities. J Pharmacol Exp Ther. 2009 Nov;331 (2) :485-95.|[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.