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A-1331852 is an orally available BCL-XL selective inhibitor with a Ki of less than 10 pM.
In vitro: A-1331852 selectively disrupts BCL-XL–BIM complexes and induces the hallmarks of apoptosis in BCL-XL–dependent Molt-4 cells with IC50s in the low nanomolar range but does not affect MEF cells lacking BAK or BAX. In CellTiter-Glo cell viability assay, A-1331852 inhibits NCI-H847, NCI-H1417, SET-2, HEL, OCI-M2 with EC50 values of 3, 7, 80, 120 and 100 nM.
In vivo: A-1331852 demonstrates antitumor efficacy in the Molt-4 xenograft model, inducing tumor regressions as a single agent. Additionally, A-1331852 combines with venetoclax to recapitulate the efficacy of navitoclax in the NCI-H1963.FP5 xenograft model of SCLC. A-1331852 significantly inhibits tumor growth in seven subcutaneous xenograft models of solid tumors, including breast cancer, NSCLC, and ovarian cancer.
| Cell Experiment | |
|---|---|
| Cell lines | bone marrow cells |
| Preparation method | 5 × 104 bone marrow cells were cultured for 4 or 24 h with or without the BCL-XL inhibitor A-1331852 in a 96-well plate in 100 μl of medium. Plates were allowed to equilibrate at room temperature prior to adding 100 μl Caspase-9 Glo reagent |
| Concentrations | 1 μM |
| Incubation time | 4 or 24 h |
| Animal Experiment | |
|---|---|
| Animal models | SCID-bg mice |
| Formulation | |
| Dosages | 25 mg/kg |
| Administration | orally |
| Molecular Weight | 658.81 |
| Formula | C38H38N6O3S |
| CAS Number | 1430844-80-6 |
| Solubility (25°C) | DMSO 50 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. |
| ABT-737
ABT-737 is a potent and selective inhibitor of B-cell lymphoma-2 (BCL-2) family proteins, in small cell lung cancer. |
| 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. |
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