A-1155463

For research use only. Not for use in humans.

Catalog No.S7800

7 publications

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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Selleck's A-1155463 has been cited by 7 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 NV\SOJNDS3m2b4TvfIlkcXS7IHHzd4F6 NVSzUFFpPDhiaILz MXLDfZRwfG:6aXPpeJkh[WejaX7zeEBDS0xvWFyt[IVx\W6mZX70JIh2dWGwIF7DTU1JOTR4IHPlcIx{KGmwIIDy[ZNmdmOnIH;mJFExLSCqdX3hckB{\XK3bTDpcoN2[mG2ZXSg[o9zKDR6IHjyd{BjgSCFZXzsJJRqfGW{R3zvJJJm[WenboSgZoF{\WRiYYPzZZktKEWFNUC9NE4xPjVizszN MXmyOVMyOzNzNx?=

... 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]
- Collapse
  • 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]
- Collapse
  • 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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Bcl-2 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID