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Biological Activity:
Oral HDM2 inhibitor (or antagonist), which showed potent activity against multiple myeloma (MM) cells in vitro and ex vivo; potential agent to restore p53 function and to potentially impact other HDM2 dependent pathways.
Note: Its directly water soluble form, JNJ26854165 dihydrochloride (Axon 1586), is also available.
References: online
T. Stühmer et al. A first-in-class HDM2-inhibitor (JNJ-26854165) in phase I development shows potent activity against multiple myeloma (MM) cells in vitro and ex vivo. J Clin Oncol 26: 2008 (May 20 suppl; abstr 14694)
K Kojima et al. The Novel Tryptamine Derivative JNJ-26854165 Induces Wild-Type p53- and E2F1-Mediated Apoptosis in Acute Myeloid and Lymphoid Leukemias. Mol. Cancer Ther. 2010, 9(9), 2545–2557. [online]
Chemical Name: N-[2-(1H-Indol-3-yl)-ethyl]-N'-pyridin-4-yl-benzene-1,3-diamine
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