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Product Description
– 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.
Web ID
– T38377
Storage Temperature
– -20℃
Shipping
– Blue Ice
Molecular Formula
– C22H18Cl2N4O2S2
References
– 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)
CAS Number
– 2414916-45-1
Molecular Weight
– C22H18Cl2N4O2S2
SMILES
– C(N)(=O)C=1C2=C(SC1NC(=O)C3=C(Cl)C=CC=C3)CN(C(NC4=C(Cl)C=CC=C4)=S)CC2
Pathway
– Others
Product type
– Small Compound
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