Home Apoptosis Bcl-2 inhibitor A-1331852 For research use only.

A-1331852

A-1331852 is a potent and selectiveBCL-XL inhibitor with Ki value less than 0.01 nM for BCL-XL and 6 nM, 4 nM, 142 nM for Bcl-2, Bcl-W, MCL-1 respectively. It may be useful in the treatment of cancer, immune and autoimmune diseases.

A-1331852 Chemical Structure

A-1331852 Chemical Structure

CAS: 1430844-80-6

Selleck's A-1331852 has been cited by 49 publications

Purity & Quality Control

Batch: Purity: 99.94%
99.94

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEL cells  Apoptosis assay 48 h induce apoptosis synergistically with ruxolitinib in HEL cells 29928488
H1299 cells Apoptosis assay 100 nM a combination of A-1210477 and A-1331852 resulted in a marked induction of apoptosis 28079887
CLL Apoptosis assay 4 h insensitive to A-1331852, IC50=1.1 μM 26954718
MOLT-4 Apoptosis assay 4 h sensitive to A-1331852, IC50~6.7 nM 26954718
H929 Apoptosis assay 4 h insensitive to A-1331852 26954718
H1299 Apoptosis assay 4 h insensitive to A-1331852 26954718
K562 Apoptosis assay 24 h extremely potent in inducing apoptosis at low nanomolar concentrations 26987906
KCL22 Apoptosis assay 24 h extremely potent in inducing apoptosis at low nanomolar concentrations 26987906
MOLT4 Cytotoxicity assay Cytotoxicity against human Bcl-XL dependant MOLT4 cells by cell based assay, EC50 = 0.006 μM. 26988306
Click to View More Cell Line Experimental Data

Biological Activity

Description A-1331852 is a potent and selectiveBCL-XL inhibitor with Ki value less than 0.01 nM for BCL-XL and 6 nM, 4 nM, 142 nM for Bcl-2, Bcl-W, MCL-1 respectively. It may be useful in the treatment of cancer, immune and autoimmune diseases.
Targets
Bcl-xL [1]
(Cell-free assay)
<0.01 nM(Ki)
In vitro
In vitro A-1331852 exhibits remarkable potency both as a single agent and in combination with TKIs in killing primary CD34+ CML cell. Also, It has remarkable potency in inducing apoptosis in these cells at low nanomolar concentrations as early as 1 h post-treatment[2].
Cell Research Cell lines K562 cells
Concentrations 100 nM
Incubation Time 0-2 h
Method Immunoprecipitation of BCL-XL is carried out in K562 cells, exposed to A-1331852 (100 nM) for 0-2 h, and the eluted complexes are immunoblotted for the indicated proteins. The input cell lysates and the immunodepleted supernatant (labeled as Flow-through) are immunoblotted to check the efficiency of the immunoprecipitation.
Experimental Result Images Methods Biomarkers Images PMID
Western blot BIM / Bad / Bcl-XL 26987906
Growth inhibition assay Cell viability 28273655
In Vivo
In vivo A-1331852 demonstrates antitumor efficacy in the Molt-4 xenograft model, inducing tumor regressions as a single agent[1].
Animal Research Animal Models SCID and SCID-bg mice
Dosages 25 mg/kg
Administration Oral administration

Chemical lnformation & Solubility

Molecular Weight 658.81 Formula

C38H38N6O3S
CAS No. 1430844-80-6 SDF Download A-1331852 SDF
Smiles CC1=C(C=NN1CC23CC4CC(C2)CC(C4)C3)C5=C(N=C(C=C5)N6CCC7=C(C6)C(=CC=C7)C(=O)NC8=NC9=CC=CC=C9S8)C(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (151.78 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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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