AT-101 acetic acid

• CAT Number: I005214
• CAS Number: 866541-93-7
• Molecular Formula: C30H30O8.C2H4O2
• Molecular Weight: 578.61
• Purity: ≥95%
• Target: Bcl-2; Bcl-xl; Mcl-1
• Solubility: DMSO; Methanol: ≤ 7.75 mg/mL
• Storage: 3 years -20C powder
• IC50: 0.32/0.48/0.18 uM for Bcl-2/Bcl-xL/Mcl-1

AT-101 acetic acid (CAT: I005214) is the R-(-) enantiomer of gossypol acetic acid. It exhibits binding affinity to Bcl-2, Bcl-xL, and Mcl-1 with Ki values of 0.32 μM, 0.48 μM, and 0.18 μM, respectively. AT-101 is an orally bioavailable BH3 mimetic that interacts with the hydrophobic surface binding groove BH3 of anti-apoptotic proteins, inhibiting their heterodimerization with pro-apoptotic members of the Bcl-2 family. By doing so, it can impede tumor cell proliferation and induce apoptosis. In vitro, studies have shown that AT-101 activates caspase-9 and induces apoptosis in various cancer cell lines, including drug-resistant and multiple myeloma cells. In vivo, AT-101 delays the onset of androgen-independent growth in VCaP prostate cancer xenografts.

Reference

[1]. Loberg RD, McGregor N, Ying C et al. In vivo evaluation of AT-101 (R-(-)-gossypol acetic acid) in androgen-independent growth of VCaP prostate cancer cells in combination with surgical castration. Neoplasia. 2007 Dec;9(12):1030-7.
[2]. Kline MP, Rajkumar SV, Timm MM et al. R-(-)-gossypol (AT-101) activates programmed cell death in multiple myeloma cells. Exp Hematol. 2008 May;36(5):568-76.
[3]. Balakrishnan K, Burger JA, Wierda WG, Gandhi V. AT-101 induces apoptosis in CLL B cells and overcomes stromal cell-mediated Mcl-1 induction and drug resistance. Blood. 2009 Jan 1;113(1):149-53.
[4]. Moretti L, Li B, Kim KW et al. AT-101, a pan-Bcl-2 inhibitor, leads to radiosensitization of non-small cell lung cancer. J Thorac Oncol. 2010 May;5(5):680-7.
[5]. McGregor N, Patel L, Craig M et al. AT-101 (R-(-)-gossypol acetic acid) enhances the effectiveness of androgen deprivation therapy in the VCaP prostate cancer model. J Cell Biochem. 2010 Aug 1;110(5):1187-94.