S63845 | 99.73%(HPLC) | In Stock

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

CAS: 1799633-27-4

Selleck's S63845 has been cited by 95 publications

Purity & Quality Control

Batch: Purity: 99.73%

99.73

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Signaling Pathway

Bcl-2 Signaling Pathway

Choose Selective Bcl-2 Inhibitors

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.

References
[1] Jason A. Powell, et al. Journal of Xiangya Medicine. 2017. [2] Kotschy A, et al. Nature. 2016, 538(7626):477-482.

References

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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

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
Batch:

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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.

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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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