S63845

Catalog No.S8383

For research use only.

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 No. 1799633-27-4

Selleck's S63845 has been cited by 55 publications

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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

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 Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human T-ALL cell lines MXTD[YxtKH[rYXLpcIl1gSCjc4PhfS=> M1Sy[|cz6oDLaB?= MUHD[YxtKGyrbnXzJIFz\SC|ZX7zbZRqfmVidH:gV|Y{QDR3IITy[YF1dWWwdDDhd{B{cG:5bjDifUA2OCViZ4Lve5RpKGmwaHnibZRwenliKFnDOVAqKH[jbIXld{BqdiCjIIP1Zo1q[3KxbX;sZZIhemGwZ3Wu MmP3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByMEi0O|coRjNyMEC4OFc4RC:jPh?=
Assay
Methods Test Index PMID
Immunofluorescence HSP70 31341643
Growth inhibition assay Cell viability 30008477
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].

Protocol (from reference)

Cell Research:

[2]

  • 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.

Animal Research:

[2]

  • Animal Models: C57BL/6 mice
  • Dosages: 25 mg/kg
  • Administration: i.v.

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(120.58 mM)
Water Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 829.26
Formula

C39H37ClF4N6O6S

CAS No. 1799633-27-4
Storage 3 years -20°C powder
2 years -80°C in solvent
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

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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.

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

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Molarity Calculator

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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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