Home Apoptosis Bcl-2 inhibitor A-1155463

A-1155463

Catalog No.S7800

For research use only.

A-1155463, a highly potent and selective BCL-XL inhibitor, shows picomolar binding affinity to BCL-XL, and >1000-fold weaker binding to BCL-2 and related proteins BCL-W(Ki=19 nM) and MCL-1(Ki>440 nM).

A-1155463 Chemical Structure

CAS No. 1235034-55-5

Selleck's A-1155463 has been cited by 26 publications

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Biological Activity

Description A-1155463, a highly potent and selective BCL-XL inhibitor, shows picomolar binding affinity to BCL-XL, and >1000-fold weaker binding to BCL-2 and related proteins BCL-W(Ki=19 nM) and MCL-1(Ki>440 nM).
Targets
BCL-XL [1]
(Cell-free assay)
<0.01 nM(Ki)
In vitro

A-1155463 disrupts BCL-XL-BIM but not BCL-2-BIM complexes in cells. A-1155463 kills BCL-XL-dependent Molt-4 cells (EC50=70 nM) but has no measurable cytotoxicity against BCL-2-dependent RS4;11 cells (EC50>5 mM). A-1155463 induces the hallmarks of apoptosis, as evidenced by the release of cytochrome c from mitochondria, caspase activation, and the accumulation of caspase-dependent sub-G0-G1 DNA content in BCL-XL-dependent H146 cells[2].
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NCI-H146 cells NULHcYJoS3m2b4TvfIlkcXS7IHHzd4F6 MVW0PEBpenN? M3LRRmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KEKFTD3YUE1l\XCnbnTlcpQhcHWvYX6gUmNKNUhzNE[gZ4VtdHNiaX6gdJJme2WwY3Wgc4YhOTBnIHj1cYFvKHOncoXtJIlv[3WkYYTl[EBnd3JiNEigbJJ{KGK7IFPlcIwhfGm2ZYLHcI8hemWjZ3XueEBj[XOnZDDhd5NigSxiRVO1NF0xNjB4NTFOwG0> NILqSG49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUOxN|MyPyd-MkWzNVM{OTd:L3G+
MOLT4 M37LUmN6fG:2b4jpZ4l1gSCjc4PhfS=> NWqx[2h[S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSmOuLWjMJIRmeGWwZHHueEBOV0yWNDDj[YxteyCkeTDj[YxtKGKjc3XkJIF{e2G7LDDFR|UxRTBwMEhOwG0> NYTLW|JwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[5PFg{ODZpPkK2PVg5OzB4PD;hQi=>
Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Growth inhibition assay EC50 26134786
In vivo Following a single 5 mg/kg IP dose of A-1155463 in nontumor bearing SCID-Beige mice, platelet counts fall dramatically as measured at 6 h postdose and then rebound to normal levels within 72 h. Daily Dosing at 5 mg/kg IP to SCID-Beige mice that had been inoculated with BCL-XL-dependent H146 tumor cells for 14 days causes a statistically significant inhibition of tumor growth (maximum tumor growth inhibition = 44%), which is alleviated upon cessation of dosing[1].

Protocol (from reference)

Cell Research:[3]
  • Cell lines: Colorectal cell lines (ATCC)
  • Concentrations: 0-10 μM
  • Incubation Time: 72 h
  • Method: Cells are treated with increasing concentration of A-1155463. Cells are assayed for viability after 72 h using the CellTiter-Glo luminescent cell viability assay according to the manufacturer’s protocol. Results are normalized to cells without treatment. EC50 is calculated using the GraphPad Prism software.
Animal Research:[1]
  • Animal Models: SCID-Beige Mice
  • Dosages: 5 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

 DMSO 80 mg/mL
(119.44 mM)
Water Insoluble
Ethanol Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.

 6mg/mL

Chemical Information

Molecular Weight 669.79
Formula

C35H32FN5O4S2
CAS No. 1235034-55-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN(C)CC#CC1=CC(=C(C=C1)OCCCC2=C(N=C(S2)N3CCC4=C(C3)C(=CC=C4)C(=O)NC5=NC6=CC=CC=C6S5)C(=O)O)F

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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.

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