A potent inhibitor of MEK in (IC50 = 2.3 nM; Kd = 74 nM when activated with ATP) that suppresses phosphorylation of ERK in mouse colon 26 tumors (IC50 = 35 nM)

CI-1040 – 25 mg

Brand:
Cayman
CAS:
212631-79-3
Storage:
-20
UN-No:
De Minimis - 3077 / 9

The dual specific threonine/tyrosine kinase, map kinase kinase (MEK), is a key component of the RAS/RAF/MEK/ERK signaling pathway that is frequently activated in human tumors.{6694,16830} CI-1040 is a benzhydroxamate compound that potently inhibits MEK in an in vitro mitogen-activated protein kinase cascade assay with an IC50 value of 2.3 nM (Kd = 74 nM when activated with adenosine triphosphate).{16877,15629} It can suppress phosphorylation of ERK in mouse colon 26 tumors with an IC50 value of 35 nM and demonstrates in vivo activity with oral administration in a mouse tumor model.{16877} The second-generation MEK inhibitor PD 0325901 (Item No. 13034) is a structural derivative of CI-1040 that was developed for improved solubility.{16877}  

 

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SKU: 11580 - 25 mg Category:

Description

A potent inhibitor of MEK in (IC50 = 2.3 nM; Kd = 74 nM when activated with ATP) that suppresses phosphorylation of ERK in mouse colon 26 tumors (IC50 = 35 nM)

Formal name: 2-[(2-chloro-4-iodophenyl)amino]-N-(cyclopropylmethoxy)-3,4-difluoro-benzamide

Synonyms:  PD 184352

Molecular weight: 478.7

CAS: 212631-79-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|RAS/RAF/MEK/ERK/MAPK||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|ERK/MAPK Signaling

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