A-1210477

Catalog No.S7790

A-1210477 Chemical Structure

Molecular Weight(MW): 850.04

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.

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2 Customer Reviews

  • (d) MVA protects against cell death in HeLa induced by the Mcl-1 inhibitor A-1210477. HeLa cells were infected with MVA (MOI=10) for 18 h and afterwards treated with the Mcl-1 inhibitor A-1210477 (10 μM) for 4 h. Apoptosis induction was measured as the percentage of cells positive for active caspase-3 by flow cytometry. Data are representative of three independent experiments (**P=0.007; two-tailed paired t-test).

    Cell Death Dis, 2016, 7(8):e2340. . A-1210477 purchased from Selleck.

    C. FACs analysis of KCNR after 72-hour treatment with 10 nmol/L ABT199 alone or in combination with 10 μmol/L A-1210477. Data represent the mean percentages of cells in sub-G1 ± SD of three replicate experiments. D. in vitro effects on BIM displacement from BCL-2 and MCL-1 after 24-hour treatment of KCNR with 10 nmol/L of ABT199 or 10μmol/L of A-1210477 and a combination of both compounds. BIM displacement was established by detecting BIM/BCL-2 and BIM/MCL-1 complex levels by anti-BCL-2 and anti-MCL-1 immunoprecipitation, followed by Western blotting for BIM. BCL-2 and MCL-1 levels served as loading control.

    Oncotarget, 2016, 7(19):27946-58. A-1210477 purchased from Selleck.

Purity & Quality Control

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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 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]

Protocol

Kinase Assay:[1]
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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:[1]
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  • 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.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 3 mg/mL warmed (3.52 mM)
Water Insoluble
Ethanol Insoluble

* 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 850.04
Formula

C46H55N7O7S

CAS No. 1668553-26-1
Storage powder
Synonyms N/A

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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

Tel: +1-832-582-8158 Ext:3

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Bcl-2 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID