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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
| 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 |
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Products are for research use only. Not for human use. We do not sell to patients.
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