A dual ERK1 and ERK5 inhibitor (IC50s = 40.43 and 64.5 nM

ADTL-EI1712 – 10 mg

Brand:
Cayman
CAS:
2414916-45-1
Storage:
-20
UN-No:
Non-Hazardous - /

ADTL-EI1712 is a dual inhibitor of ERK1 and ERK5 (IC50s = 40.43 and 64.5 nM, respectively).{59056} It reduces ERK1 and ERK5 activity by 93.5% and 89.4%, respectively, but also inhibits ERK2 activity by 92.7%, in a panel of 100 kinases at 1 µM. ADTL-EI1712 inhibits proliferation of HL-60 and MKN74, but not HeLa, cancer cells (IC50s = 1.26, 2.55, and >50 µM, respectively). It reduces tumor growth and intratumor phosphorylation of ERK1/2 and ERK5 in an MKN74 mouse xenograft model when administered at a dose of 50 mg/kg per day.  

 

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SKU: 30602 - 10 mg Category:

Description

A dual ERK1 and ERK5 inhibitor (IC50s = 40.43 and 64.5 nM, respectively); reduces ERK1 and ERK5 activity by 93.5% and 89.4%, respectively, but also inhibits ERK2 activity by 92.7%, in a panel of 100 kinases at 1 µM; inhibits proliferation of HL-60 and MKN74 cancer cells (IC50s = 1.26 and 2.55 µM, respectively); reduces tumor growth and intratumor phosphorylation of ERK1/2 and ERK5 in an MKN74 mouse xenograft model at 50 mg/kg per day

Formal name: 2-[(2-chlorobenzoyl)amino]-6-[[(2-chlorophenyl)amino]thioxomethyl]-4,5,6,7-tetrahydro-thieno[2,3-c]pyridine-3-carboxamide

Synonyms: 

Molecular weight: 505.4

CAS: 2414916-45-1

Purity: ≥98%

Formulation: A crystalline solid

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