(+)-Apogossypol

Additional information:
(+)-Apogossypol is a pan-BCL-2 antagonist. (+)-Apogossypol binds to Mcl-1, Bcl-2 and Bcl-xL with EC50s of 2.6, 2.8 and 3.69 µM, respectively.|Product information|CAS Number: 66389-74-0|Molecular Weight: 462.53|Formula: C28H30O6|Synonym:|NSC736630|Apogossypol|Chemical Name: 3,3′-dimethyl-5,5′-bis(propan-2-yl)-[2,2′-binaphthalene]-1,1′,6,6′,7,7′-hexol|Smiles: CC1=CC2=C(C(C)C)C(O)=C(O)C=C2C(O)=C1C1=C(O)C2=CC(O)=C(O)C(C(C)C)=C2C=C1C|InChiKey: PBJKWGWHZVXBGU-UHFFFAOYSA-N|InChi: InChI=1S/C28H30O6/c1-11(2)21-15-7-13(5)23(25(31)17(15)9-19(29)27(21)33)24-14(6)8-16-18(26(24)32)10-20(30)28(34)22(16)12(3)4/h7-12,29-34H,1-6H3|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: ≥16.2mg/mL in DMSO with gentle warming|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥360 days if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|In agreement with NMR binding and fluorescence polarization assays (FPAs) data, (+)-Apogossypol displays potent binding affinity to Bcl-xL with Kd values of 1.7 µM.To investigate the inhibitory effects of (+)-Apogossypol and Gossypol on LNCaP cell survival, the MTT assay is performed.{{Crizotinib} site|{Crizotinib} ROS Kinase|{Crizotinib} Purity & Documentation|{Crizotinib} References|{Crizotinib} custom synthesis|{Crizotinib} Cancer} The results demonstrate that (+)-Apogossypol inhibits the proliferation of LNCaP cells in a time- and dose-dependent manner, in a similar way with Gossypol.PMID:35670838 The concentration for 50% inhibition (IC50) on LNCaP cells within ~72 h is 9.57 μM, while the IC50 of Gossypol on LNCaP cells is 10.35 μM.|In Vivo:|Due to its modified structure, (+)-Apogossypol is expected to exhibit lower toxicity while maintaining the significant anti-growth and anti-tumor activities in vitro, similar to those of Gossypol. The anti-cancer effect of (+)-Apogossypol is evaluated in mice bearing subcutaneous LNCaP cell xenografts. The tumor growth is monitored and measured by a caliper and balance. The survival rate of the mice is notably improved by (+)-Apogossypol. Of note, the tumor sizes are also markedly decreased by (+)-Apogossypol treatment (PReferences:| Zhan W, et al. Inhibitory activity of apogossypol in human prostate cancer in vitro and in vivo. Mol Med Rep. 2015 Jun;11(6):4142-8.Wei J, et al. Apogossypol derivatives as antagonists of antiapoptotic Bcl-2 family proteins. Mol Cancer Ther. 2009 Apr;8(4):904-13. Products are for research use only. Not for human use.|