A dual ERK1 and ERK5 inhibitor
货号:ajcx21626
CAS:2414916-45-1
分子式:C22H18Cl2N4O2S2
分子量：505.4
溶解度:DMF: 1 mg/ml,DMSO: 1 mg/ml,DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml
纯度：98%
存储：Store at -20°C
库存：现货

Background:

ADTL-EI1712 is a dual inhibitor of ERK1 and ERK5 (IC₅₀s = 40.43 and 64.5 nM, respectively).¹It 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.

1.Wang, G., Zhao, Y., Liu, Y., et al.Discovery of a novel dual-target inhibitor of ERK1 and ERK5 that induces regulated cell death to overcome compensatory mechanism in specific tumor typesJ. Med. Chem.63(8)3976-3995(2020)