[CAS NO. 66389-74-0] (+)-Apogossypol
PRODUCTS SPECIFICATIONS [66389-74-0]
DESCRIPTION [66389-74-0]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 462.54 |
| Molecular Formula | C28H32O6 |
| SMILES | OC1=C2C=C(O)C(O)=C(C(C)C)C2=CC(C)=[C@@]1[C@@]3=C(C)C=C4C(C(C)C)=C(O)C(O)=CC4=C3O |
Summary
IC50 & Target
|
Mcl-1 2.6 μM (EC 50 ) |
Bcl-2 2.8 μM (EC 50 ) |
Bcl-xL 3.69 μM (EC 50 ) |
In Vitro
In agreement with NMR binding and fluorescence polarization assays (FPAs) data, (+)-Apogossypol displays potent binding affinity to Bcl-xL with K d values of 1.7 µM [1] .To investigate the inhibitory effects of (+)-Apogossypol and Gossypol on LNCaP cell survival, the MTT assay is performed. The results demonstrate that (+)-Apogossypol inhibits the proliferation of LNCaP cells in a time- and dose-dependent manner, in a similar way with Gossypol. The concentration for 50% inhibition (IC 50 ) on LNCaP cells within ~72 h is 9.57 μM, while the IC 50 of Gossypol on LNCaP cells is 10.35 μM [2] .
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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 (P<0.01) [2] .
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
References