All AbMole products are for research use only, cannot be used for human consumption.
ABT-737 is a potent and selective inhibitor of B-cell lymphoma-2 (BCL-2) family proteins. The ABT-737 single-agent LC90 values ranged from 100 nM for COG-LL-319 and RS4; 11 cells to low micromolar concentrations for the other five ALL cell lines. ABT-737 efficiently induces apoptosis and suppresses growth of hepatoma cells in combination with sorafenib. Moreover, we observed that the enhancement of ABT-737-mediated apoptosis by NCTD was associated with activation of mitochondrial apoptosis signaling pathway, which involved cytosolic release of cytochrome c, cleavage of caspase-9 and caspase-3. Finally, knockdown of Mcl-1 substantially potentiated ABT-737-mediated apoptotic cell death, confirming the potency of Mcl-1 repression by NCTD in enhancing ABT-737-induced apoptosis. These results therefore suggest that combination treatment with NCTD can overcome ABT-737 resistance and enhance ABT-737 therapeutic efficacy in treating human HCC.
 |
Source | Cancer Res (2014). Figure 4. ABT-737 |
| Method | Western blot | |
| Cell Lines | SCLC cell lines | |
| Concentrations | 100 nmol/L | |
| Incubation Time | 24 or 72 h | |
| Results | We did observe that the proapoptotic proteins BAX and BAK were increased in both PDXs treated with rapamycin alone or in combination with ABT-737. |
 |
Source | Cancer Res (2014). Figure 3. ABT-737 |
| Method | i.e. | |
| Cell Lines | SCLC PDX models | |
| Concentrations | 100 mg/kg | |
| Incubation Time | 14 d | |
| Results | Correlating these findings with transcriptional profiling data, we observed decreased levels of six HIF-1α–regulated genes in LX47 after treatment with ABT-737, this effect was less pronounced in LX33, but nonetheless, observed for most genes. |
| Cell Experiment | |
|---|---|
| Cell lines | CLL cells and platelets |
| Preparation method | Apoptosis analysis Peripheral blood mononuclear cells were purified using Histopaque and cultured in RPMI 1640 medium supplemented with 10% fetal calf serum and 2 mmol/l L-glutamine at2*106 cells/ml. Cells were exposed to different concentrations of ABT-737, ABT-263, or ABT-199 for 4 h before analysis of apoptosis by externalisation of phosphatidylserine (PS) and binding of AnnexinV/fluorescein isothiocyanate (FITC). Platelets isolated from healthy volunteers were cultured in Hepes-buffered saline and exposed to different concentrations of ABT-737, ABT-263, or ABT-199 for 4 h before analysis of apoptosis in the CD41-positive population by externalisation of PS and binding of AnnexinV/FITC. |
| Concentrations | 0~3µM |
| Incubation time | 4 h |
| Animal Experiment | |
|---|---|
| Animal models | C57BL/6 mice were injected (i.v.) with 3x106 T1 lymphoma cells |
| Formulation | formulated in 60% phosal 50PG (standardized phosphatidylcholine concentrate with at least 50% PC and propylene glycol |
| Dosages | 100 mg/kg |
| Administration | oral gavage |
| Molecular Weight | 813.43 |
| Formula | C42H45ClN6O5S2 |
| CAS Number | 852808-04-9 |
| Solubility (25°C) | DMSO 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Bcl-2 Products |
|---|
| ABT-263
ABT-263 (Navitoclax) is a potent, orally bioavailable inhibitor of the antiapoptotic Bcl-2 family members Bcl-2, Bcl-x (L), and Bcl-w. |
| AT-101
AT-101 (R-(-)-gossypol acetic acid) is a pan small molecule inhibitor of Bcl-2, Bcl-xL, and Mcl-1. |
| ABT-199
ABT-199 (Venetoclax) is a highly potent, orally bioavailable and BCL-2 inhibitor. ABT-199 is the first inhibitor targeting Bcl-2 and PPI. |
| TW-37
TW-37 is a novel nonpeptide inhibitor to recombinant Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.29 μM, 1.11 μM and 0.26 μM, respectively. |
| Apogossypolone
Apogossypolone (ApoG2) is a pan Bcl-2 inhibitor for Bcl-2, Bcl-XL and Mcl-1 with Ki of 35 nM, 660 nM and 25 nM, respectively. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2026 AbMole BioScience. All Rights Reserved.
