ADTL-EI1712

ADTL-EI1712 is a dual inhibitor of ERK1 and ERK5 (IC50s = 40.43 and 64.5 nM, respectively). 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.Formal Name: 2-[(2-chlorobenzoyl)amino]-6-[[(2-chlorophenyl)amino]thioxomethyl]-4,5,6,7-tetrahydro-thieno[2,3-c]pyridine-3-carboxamide. CAS Number: 2414916-45-1. Molecular Formula: C22H18Cl2N4O2S2. Formula Weight: 505.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 1 mg/ml, DMSO: 1 mg/ml, DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml. SMILES: O=C(C1=C(NC(C2=CC=CC=C2Cl)=O)SC3=C1CCN(C(NC4=CC=CC=C4Cl)=S)C3)N. InChi Code: InChI=1S/C22H18Cl2N4O2S2/c23-14-6-2-1-5-12(14)20(30)27-21-18(19(25)29)13-9-10-28(11-17(13)32-21)22(31)26-16-8-4-3-7-15(16)24/h1-8H,9-11H2,(H2,25,29)(H,26,31)(H,27,30). InChi Key: LVSFMPVPLIMFMY-UHFFFAOYSA-N.