Home Apoptosis Bcl-2 inhibitor A-1210477 For research use only.

A-1210477

A-1210477 is a potent and selective MCL-1 inhibitor with Ki and IC50 of 0.454 nM and 26.2 nM, respectively, >100-fold selectivity over other Bcl-2 family members.

A-1210477 Chemical Structure

A-1210477 Chemical Structure

CAS No. 1668553-26-1

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A-1210477 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
human H23 cells Cytotoxicity assay 24 hrs Cytotoxicity against human H23 cells incubated for 24 hrs by CCK8 assay 31389699
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Biological Activity

Description A-1210477 is a potent and selective MCL-1 inhibitor with Ki and IC50 of 0.454 nM and 26.2 nM, respectively, >100-fold selectivity over other Bcl-2 family members.
Targets
MCL-1 [1]
(Cell-free assay)
26.2 nM
In vitro
In vitro In H929 cells, A-1210477 binds to MCL-1 with high affinity and induces MCL-1 protein elevation. In H929, H2110, and H23 cells, A-1210477 induce the hallmarks of apoptosis, and inhibits MCL-1-dependent cell viability. A-1210477 also synergizes with navitoclax to kill a variety of cancer cell lines. [1] In SKBR3 cells, A-1210477 inhibits MCL-1–BIM interaction and induces classical features of apoptosis. [2] In addition, A-1210477 sensitizes non-Hodgkin's lymphoma cell lines to venetoclax (ABT-199). [3]
Kinase Assay Binding affinity assays
TR-FRET-binding affinity assays are performed for BCL-2, BCL-XL, and MCL-1 in 4.52 mM monobasic potassium phosphate, 15.48 mM dibasic potassium phosphate, 1 mM sodium EDTA, 0.05% Pluronic F-68 detergent, 50 mM sodium chloride, and 1 mM DTT (pH 7.5). For MCL-1 assays, GST-tagged MCL-1 (1 nM) is mixed with 100 nM f-Bak, 1 nM Tb-labeled anti-GST antibody, and compound at room temperature (RT) for 60 min. Fluorescence is measured on an Envision plate reader using a 340/35 nm excitation filter and 520/525 (f-Bak) and 495/510 nm (Tb-labeled anti-GST antibody) emission filters.
Cell Research Cell lines H929, H2110, and H23 cells
Concentrations ~30 μM
Incubation Time 48 h or 72 h
Method Adherent cell lines are seeded at 50 000 cells per well in 96-well plates and treated for 48 h with compounds diluted in half-log steps starting at 30 μM and ending at 0.001 μM. Multiple myeloma cell lines were seeded at 15 000–20 000 cells per well and treated similarly. Effects on proliferation and viability were determined using CellTiter-Glo reagent according to the manufacturer’s instructions. IC50 values are determined by non-linear regression analysis of the concentration response data.
Experimental Result Images Methods Biomarkers Images PMID
Western blot Mcl-1 PARP / MEK / Cyt c/ Tom20 pERK / ERK / p-MCL1 / Caspase-3 30796196

Chemical Information & Solubility

Molecular Weight 850.04 Formula

C46H55N7O7S
CAS No. 1668553-26-1 SDF Download A-1210477 SDF
Smiles CC1=NN(C(=C1C2=CC=CC3=C2N(C(=C3CCCOC4=CC=CC5=CC=CC=C54)C(=O)O)CCN6CCOCC6)COC7=CC=C(C=C7)N8CCN(CC8)S(=O)(=O)N(C)C)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 3 mg/mL ( (3.52 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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