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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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
| Molecular Weight | 658.81 |
| Formula | C38H38N6O3S |
| CAS Number | 1430844-80-6 |
| Purity | >98% |
| Solubility | 12 mg/mL in DMSO |
| Storage | at -20°C |
Targeting senescent cholangiocytes and activated fibroblasts with B-cell lymphoma-extra large inhibitors ameliorates fibrosis in multidrug resistance 2 gene knockout (Mdr2-/- ) mice.
Moncsek A, et al. Hepatology. 2018 Jan;67(1):247-259. PMID: 28802066.
The BH3-only proteins BIM and PUMA are not critical for the reticulocyte apoptosis caused by loss of the pro-survival protein BCL-XL.
Delbridge AR, et al. Cell Death Dis. 2017 Jul 6;8(7):e2914. PMID: 28682312.
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