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S63845

Cat. No. M5273
S63845 Structure
Synonym:

S-63845, S 63845

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2mg USD 162  USD180 Out of stock
5mg USD 324  USD360 Out of stock
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Quality Control
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%).
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 829.26
Formula C39H37ClF4N6O6S
CAS Number 1799633-27-4
Purity 99.63%
Solubility 10mM in DMSO
Storage powder, at 4°C, protect from light, dry
References

S63845, an MCL-1 Selective BH3 Mimetic: Another Arrow in Our Quiver.
Letai A, et al. Cancer Cell. 2016 Dec 12;30(6):834-835. PMID: 27960083.

The MCL1 inhibitor S63845 is tolerable and effective in diverse cancer models.
Kotschy A, et al. Nature. 2016 Oct 27;538(7626):477-482. PMID: 27760111.

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  Catalog
Abmole Inhibitor Catalog 2017




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

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