ABT-263-d8

ABT-263-d₈ is intended for use as an internal standard for the quantification of ABT-263 by GC- or LC-MS. ABT-263 is an inhibitor of the Bcl-2 family proteins Bcl-2, Bcl-xL, and Bcl-W (K_is = <1, <0.5, and <1 nM, respectively).¹ It is selective for Bcl-2, Bcl-xL, and Bcl-W over Mcl-1 and A1 (K_is = 550 and 354 nM, respectively). ABT-263 is cytotoxic in a panel of small cell lung cancer (SCLC), leukemia, and lymphoma cell lines with a mean EC₅₀ value of 1 µM. It induces apoptosis in influenza A-infected retinal pigment epithelial cells (EC₅₀ = 0.08 µM).² ABT-263 (100 mg/kg) induces tumor regression in NCI H146 SCLC and RS4;11 acute lymphocytic leukemia (ALL) mouse xenograft models.^1,3

1.Tse, C., Shoemaker, A.R., Adickes, J., et al.ABT-263: A potent and orally bioavailable Bcl-2 family inhibitorCancer Res.68(9)3421-3428(2008) 2.Bulanova, D., Ianevski, A., Bugai, A., et al.Antiviral properties of chemical inhibitors of cellular anti-apoptotic Bcl-2 proteinsViruses9(10)E271(2017) 3.Shoemaker, A.R., Mitten, M.J., Adickes, S., et al.Activity of the Bcl-2 family inhibitor ABT-263 in a panel of small cell lung cancer xenograft modelsClin. Cancer Res.14(11)3268-3277(2008)