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MW 581.5 Da, Purity >98%. p53-MDM2 binding inhibitor (IC₅₀ = 13 μM). Less potent enantiomer of (-)-Nutlin-3 (Asc-4428 ). Shows antiproliferative effects (IC₅₀ values are 2.2 and 1.3 μM for human skin and murine fibroblasts respectively). Shows antitumor effects in vivo. Orally active.
MW 341.8 Da, Purity >99%. Cell-permeable IGF1R inhibitor (IC₅₀ = 12 μM for IGF-stimulated autophosphorylation). Shows antiproliferative effects against MCF-7 breast cancer cells. Induces renal hypertrophy in vivo. .
MW 365.8 Da, Purity >99%. Potent, selective 5-HT (serotonin) uptake inhibitor. Inhibits human and rat 5-HT transporters (Ki values are 0.065 and 0.05 nM, respectively). Antidepressant and anxiolytic in vivo.