All AbMole products are for research use only, cannot be used for human consumption.
In vitro: The pro-survival protein myeloid cell leukemia 1 (MCL1) is over expressed in many cancers. S63845 is a small molecule that specifically binds with high affinity to the BH3-binding groove of MCL1. S63845 potently kills MCL1-dependent cancer cells, including multiple myeloma, leukaemia and lymphoma cells, by activating the BAX/BAK-dependent mitochondrial apoptotic pathway. The activity of S63845 is next evaluated in a panel of eight AML cell lines: all lines are sensitive to S63845 (IC50=4-233 nM). In vivo: S63845 shows potent anti-tumour activity with an acceptable safety margin as a single agent in several cancers. Intravenously injected (i.v.) S63845 exerts dose-dependent anti-tumour activity in human multiple myeloma (H929 and AMO1) xenografts in immunocompromised mice, with maximal tumour growth inhibition of 114% in the AMO1 model and 103% in the H929 model. At 25 mg/kg, S63845 induces complete regression in 7 out of 8 of the mice at 100 days after treatment in the AMO1 model.
Cancers (Basel). 2021 May 12;13(10):2310.
Unmasking BCL-2 Addiction in Synovial Sarcoma by Overcoming Low NOXA
S63845 purchased from AbMole
Mol Carcinog. 2020 Nov;59(11):1256-1268.
Mcl-1 targeting strategies unlock the proapoptotic potential of TRAIL in melanoma cells
S63845 purchased from AbMole
 |
Source | MOL CARCINOGEN 2020. Figure 5. S63845 (Abmole Bioscience, USA) |
| Method | Cell culture | |
| Cell Lines | Origin of human melanoma cell lines | |
| Concentrations | 5 µM | |
| Incubation Time | 24 hours | |
| Results | When applied alone, S63845 resulted in 15% apoptosis induction and reduction of viable cells to 60%. The proapoptotic Bcl-2 proteins Bax and Bak were strongly activated by S63845 (44%). |
| Molecular Weight | 829.26 |
| Formula | C39H37ClF4N6O6S |
| CAS Number | 1799633-27-4 |
| Solubility (25°C) | 10mM in DMSO |
| Storage | powder, at 4°C, protect from light, dry |
| Related Bcl-2 Products |
|---|
| ABBV-467
ABBV-467 is a selective MCL-1 inhibitor (Ki: <0.01 nM). |
| WEHI-539
WEHI-539 is a selective inhibitor of Bcl-XL with an IC50 of 1.1 nM. |
| (Rac)-Lisaftoclax
(Rac)-Lisaftoclax ((Rac)-APG-2575) is a Bcl-2 inhibitor that can be uesd for hematologic malignancy research. |
| BcI-2/BcI-xI ligand 1
BcI-2/BcI-xI ligand 1 is a BcI-2/BcI-xI ligand, and can be used for synthesis of PROTAC BcI-2/BcI-xI Degrader-1. |
| AZD-5991 (S-enantiomer)
AZD-5991 S-enantiomer is the less active enantiomer of AZD-5991. |
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 2010-2024 AbMole BioScience. All Rights Reserved.
