1448525-91-4
1448525-91-4 structure
- Name: S55746 hydrochloride (BLC201 (hydrochloride))
- Chemical Name: S55746 hydrochloride
- CAS Number: 1448525-91-4
- Molecular Formula: C43H43ClN4O6
- Molecular Weight: 747.28
- Catalog: Signaling Pathways Apoptosis Bcl-2 Family
- Create Date: 2019-02-08 15:12:44
- Modify Date: 2024-01-11 10:38:54
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S55746 hydrochloride is a potent, orally active and selective BCL-2 inhibitor, with Kis and Kds of 1.3 nM, 520 nM and 3.9 nM, 186 nM for BCL-2 and BCL-XL, respectively. S55746 hydrochloride has antitumor activity.
| Name | S55746 hydrochloride |
|---|
| Description | S55746 hydrochloride is a potent, orally active and selective BCL-2 inhibitor, with Kis and Kds of 1.3 nM, 520 nM and 3.9 nM, 186 nM for BCL-2 and BCL-XL, respectively. S55746 hydrochloride has antitumor activity. |
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| Related Catalog | |
| Target |
Bcl-2:1.3 nM (Ki) Bcl-xL:520 nM (Ki) Bcl-2:3.9 nM (Kd) Bcl-xL:186 nM (Kd) |
| In Vitro | S55746 hydrochloride is a potent, orally active and selective BCL-2 inhibitor, with Kis and Kds of 1.3 nM, 520 nM and 3.9 nM, 186 nM for BCL-2 and BCL-XL, respectively. S55746 selectively induces cell death. S55746 potently causes RS4;11 cell killing with an IC50 of 71.6 nM after 72 h of treatment, but shows a much weaker activity in H146 (IC50 1.7 μM), a BCL-XL-dependent cell line. S55746 also selectively induces apoptosis through BCL-2 inhibition in a BAX/BAK-dependent manner. S55746 (3 nM) induces cell death in CLL cells[1]. |
| In Vivo | S55746 is a highly efficacious and well-tolerated orally active BCL-2 inhibitor. S55746 (25 and 100 mg/kg, p.o.) inhibits xenograft growth in RS4;11 and Toledo models[1]. |
| Cell Assay | Cells are seeded into 96-well plates and treated at 8 points with 1:2 serial dilution of S55746. Cell viability is assessed and assayed for viability using CellTiter-Glo reagent. Plates are read using luminescence plate reader. Results are normalized to the viability of cells without S55746 (control wells). The IC50 values are calculated using nonlinear regression algorithms in XCell software[1]. |
| Animal Admin | Mice[1] For each experiment, female SCID/beige mice are implanted subcutaneously with 3 × 106 Toledo or RS4;11 (1 × 106 cells for efficacy studies and 1 × 107 cells for pharmacodynamics studies) suspended in 1:1 mixture of cold DPBS and Matrigel in a total volume of 100 μL. Body weights are recorded and tumors are measured with digital calipers twice to three times a week. Tumor volume is calculated using the formula: length × width2/2. Percent changes in body weights is calculated as (BWcurrent - BWinitial)/(BWinitial) × 100. Data is presented as percent body weight change from the day of treatment initiation. When tumors reach approximately 200 mm3 for efficacy studies or 300 mm3 for pharmacodynamic studies, mice are randomized. S55746 is formulated in PEG300/EtOH/water (40/10/50). ABT-199 is formulated in PEG300/EtOH/Phosal (30/10/60). Mice are treated via oral gavage at 10 mL/kg with the doses and schedules described in the figure[1]. |
| References |
| Molecular Formula | C43H43ClN4O6 |
|---|---|
| Molecular Weight | 747.28 |
| Storage condition | 2-8℃ |