A-1155463

Catalog No.S7800

A-1155463 Chemical Structure

Molecular Weight(MW): 669.79

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).

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Cited by 2 Publications

1 Customer Review

  • Tumor growth rate (TGR) of tumors orthotopically implanted in rats on day 3, 7 and 10 compared to day 0. Rats were treated with doxorubicin, A-1155463 or a combination. Treatment with A-1155463 resulted in a significant decrease in TGR compared to control mice.

    Oncogenesis, 2018, 7(9):74. A-1155463 purchased from Selleck.

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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 M2jPd2N6fG:2b4jpZ4l1gSCjc4PhfS=> MYm0PEBpenN? MUfDfZRwfG:6aXPpeJkh[WejaX7zeEBDS0xvWFyt[IVx\W6mZX70JIh2dWGwIF7DTU1JOTR4IHPlcIx{KGmwIIDy[ZNmdmOnIH;mJFExLSCqdX3hckB{\XK3bTDpcoN2[mG2ZXSg[o9zKDR6IHjyd{BjgSCFZXzsJJRqfGW{R3zvJJJm[WenboSgZoF{\WRiYYPzZZktKEWFNUC9NE4xPjVizszN NUPtTIpxOjV|MUOzNVc>

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Growth inhibition assay
EC50; 

PubMed: 26134786     


Colorectal cell lines were treated with increasing concentrations of A-1155463. Cells were assayed for viability after 72 h. Results were normalized to cells without treatment. Each cell line was treated with A-1155463 in at least 3 different experiments and the average EC50 is presented. BCL2L1 copy number gain >3 is indicated with + or -. Mutation status of APC and β-catenin is also indicated with + or -. 

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

Cell Research:[3]
+ Expand
  • 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.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: SCID-Beige Mice
  • Formulation: 5% DMSO, 10% EtOH, 20% Cremaphor ELP, and 65% D5W
  • Dosages: 5 mg/kg
  • Administration: i.p.
    (Only for Reference)

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 669.79
Formula

C35H32FN5O4S2
CAS No. 1235034-55-5
Storage powder
in solvent
Synonyms N/A

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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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Bcl-2 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID