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.
Cited by 18 Publications
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U251 glioblastoma (F) or MeWo melanoma (G) cells were treated with selective BH-3 mimetics, GTPP or the combination of both for 24 h (U251) or 48 h (MeWo). Thereafter, cells were stained with annexin V and propidium iodide and analyzed by flow cytometry. Shown are representative flow plots.
Cancer Research, 2017, doi:10.1158/0008-5472. A-1210477 purchased from Selleck.
Cells were treated for 48 h of control (DMSO), 5 μM A-1210477, 3.3 μM ABT-263 or the combination of 5 μM A-1210477 plus 3.3 μM ABT-263, and then subjected to Immunoblot with an antibody recognizing full length and cleaved PARP. The combination treatment increased the cleaved: full-length PARP ratio in all lines. Molecular weight markers are in kDa.
Cell Death Dis, 2018, 9(9):907. A-1210477 purchased from Selleck.
(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.
CRC (RKO, HT29) and melanoma (A375) cell lines were treated with A-1210477 alone or combined with cobimetinib for 48 at the indicated doses. ERK activation, BIM isoform expression, and cleavage of PARP and CASPASE3 were analyzed by immunoblotting.
Mol Cancer Ther, 2016, 15(12):3015-3027. 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.
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Choose Selective Bcl-2 Inhibitors
|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.|
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.  In SKBR3 cells, A-1210477 inhibits MCL-1–BIM interaction and induces classical features of apoptosis.  In addition, A-1210477 sensitizes non-Hodgkin's lymphoma cell lines to venetoclax (ABT-199). 
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.
|In vitro||DMSO||3 mg/mL warmed (3.52 mM)|
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