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S63845

Cat. No. M5273

All AbMole products are for research use only, cannot be used for human consumption.

S63845 Structure
Synonym:

S-63845, S 63845

Size Price Availability
2mg USD 180 Out of stock
5mg USD 360 Out of stock
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Quality Control & Documentation
Biological Activity

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.

Product Citations
Customer Product Validations & Biological Datas
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%).
Chemical Information
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
References

[1] Letai A, et al. Cancer Cell. S63845, an MCL-1 Selective BH3 Mimetic: Another Arrow in Our Quiver.

[2] Kotschy A, et al. Nature. The MCL1 inhibitor S63845 is tolerable and effective in diverse cancer models.

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Keywords: S63845, S-63845, S 63845 supplier, Bcl-2, inhibitors, activators

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