Home Apoptosis Bcl-2 inhibitor S63845 For research use only.

S63845

S63845 is a new, selective MCL-1 inhibitor with the Kd value of 0.19 nM and has no discernible binding to the other BCL-2 members, BCL-2 or BCL-XL.

S63845 Chemical Structure

S63845 Chemical Structure

CAS No. 1799633-27-4

Purity & Quality Control

S63845 Related Products

Signaling Pathway

Bcl-2 Signaling Pathways

Bcl-2 Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human T-ALL cell lines Cell viability assay 72 h Cell lines are sensitive to S63845 treatment as shown by 50% growth inhibitory (IC50) values in a submicromolar range. 30008477
Click to View More Cell Line Experimental Data

Biological Activity

Description S63845 is a new, selective MCL-1 inhibitor with the Kd value of 0.19 nM and has no discernible binding to the other BCL-2 members, BCL-2 or BCL-XL.
Targets
human MCL-1 [1]
0.19 nM(Kd)
In vitro
In vitro S63845 induces death of cancer cell lines with known reliance on MCL-1, displaying classical hallmarks of apoptosis that are dependent on caspases and BAX/BAK-mediated mitochondrial outer membrane permeabilisation. It has a 6 fold higher affinity for human MCL-1 over mouse MCL-1[1]. S63845 is effective against haematological cancer-derived cell lines in vitro and in vivo and also AML samples, but does not readily kill normal human haematopoietic progenitor cells[2].
Cell Research Cell lines HeLa cells
Concentrations 0.1, 0.3, 1, 3 μM
Incubation Time 4 h
Method

HeLa cells transduced with Flag–BCL-XL, Flag–BCL-2 or Flag–MCL1 expression constructs are treated for 4 h with increasing concentrations of S63845, before immunopreciptation using anti-FLAG antibody. Immunoprecipitates and total inputs are analysed by immunoblotting for the FLAG-tagged proteins as well as the associated BAK and BAX proteins.
Experimental Result Images Methods Biomarkers Images PMID
Immunofluorescence HSP70 31341643
Growth inhibition assay Cell viability 30008477
In Vivo
In vivo In vivo, S63845 shows potent anti-tumour activity with an acceptable safety margin as a single agent in several cancers. S63845 is well tolerated by the mice with no significant weight loss observed. Some of solid tumour models shows sensitivity to S63845 monotherapy, while many others are only killed when treated with a combination of S63845 and inhibitors of oncogenic kinases[2].
Animal Research Animal Models C57BL/6 mice
Dosages 25 mg/kg
Administration i.v.

Chemical Information & Solubility

Molecular Weight 829.26 Formula

C39H37ClF4N6O6S
CAS No. 1799633-27-4 SDF Download S63845 SDF
Smiles CC1=C(C=CC(=C1Cl)OCCN2CCN(CC2)C)C3=C(SC4=NC=NC(=C34)OC(CC5=CC=CC=C5OCC6=CC=NN6CC(F)(F)F)C(=O)O)C7=CC=C(O7)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (120.58 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 38 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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