AT-101_90141-22-3_DataSheet_MedChemExpress

Product Name:CAS No.: Cat. No.:MWt:Formula:Purity :

AT-10190141-22-3HY-15464518.55C30H30O8>98%

Solubility:DMSO >80 mg/ml Ethanol >80 mg/ml

Mechanisms:

Pathways:Apoptosis; Target:Bcl-2 Family

Biological Activity:

AT101, the R-(-) enantiomer of Gossypol acetic acid, binds with Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.32 μM,0.48 μM and 0.18 μM.

IC50 Value: 0.32/0.48/0.18 uM for Bcl-2/Bcl-xL/Mcl-1 Target: Bcl-2; Bcl-xl; Mcl-1

AT-101 is orally bioavailable solvate of R-(-)-enantiomer of gossypol with potential antineoplastic activity. As aBH3 mimetic, AT-101 binds to the hydrophobic surface binding groove BH3 of the anti-apoptotic proteins Bcl-2 and Bcl-xL, blocking their heterodimerization with pro-apoptotic members of the Bcl-2 family of proteinssuch as Bad, Bid, and Bim; this may result in the inhibition of tumor cell proliferation and the induction oftumor cell apoptosis. AT-101 induces apoptosis in vitro through activation of caspase-9; cytotoxic to multiplemyeloma and drug-resistant cell lines. AT-101 delays onset of androgen-independent growth of VCaPprostate cancer xenog...References:

[1]. Loberg RD, McGregor N, Ying C et al. In vivo evaluation of AT-101 (R-(-)-gossypol acetic acid) inandrogen-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 inmultiple 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 andovercomes 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 celllung cancer. J Thorac Oncol. 2010 May;5(5):680-7. [5]. R-(-)-gossypol acetic acid

[6]. McGregor N, Patel L, Craig M et al. AT-101 (R-(-)-gossypol acetic ac...

Caution: Not fully tested. For research purposes only

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