Home Apoptosis Bcl-2 inhibitor A-1155463 Dihydrochloride For research use only.

A-1155463 Dihydrochloride

A-1155463 Dihydrochloride, 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 Dihydrochloride Chemical Structure

A-1155463 Dihydrochloride Chemical Structure

CAS No. 1235034-55-5(free base)

Purity & Quality Control

A-1155463 Dihydrochloride Related Products

Signaling Pathway

Bcl-2 Signaling Pathways

Bcl-2 Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NCI-H146 cells Cytotoxicity assay 48 hrs Cytotoxicity against BCL-XL-dependent human NCI-H146 cells in presence of 10% human serum incubated for 48 hrs by Cell titerGlo reagent based assay, EC50=0.065 μM 25313317
MOLT4 Cytotoxicity assay Cytotoxicity against human Bcl-XL dependant MOLT4 cells by cell based assay, EC50=0.07μM 26988306
Click to View More Cell Line Experimental Data

Biological Activity

Description A-1155463 Dihydrochloride, 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
In vitro

A-1155463 Dihydrochloride 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 Research 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.
Experimental Result Images Methods Biomarkers Images PMID
Growth inhibition assay EC50 26134786
In Vivo
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].
Animal Research Animal Models SCID-Beige Mice
Dosages 5 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 742.71 Formula

C35H34Cl2FN5O4S2
CAS No. 1235034-55-5(free base) SDF Download A-1155463 Dihydrochloride SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (134.64 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, 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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