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A-1210477

Catalog No. T2632 CAS 1668553-26-1

A-1210477 is an effective and specific MCL-1 and Bcl-2 inhibitor (Ki/IC50: 0.454/26.2 nM).

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A-1210477, CAS 1668553-26-1

Pack Size	Availability	Price/USD
2 mg	In stock	$ 34.00
5 mg	In stock	$ 55.00
10 mg	In stock	$ 97.00
25 mg	In stock	$ 163.00
50 mg	In stock	$ 288.00
100 mg	In stock	$ 448.00
500 mg	In stock	$ 987.00

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Purity: 99.76%

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Description	A-1210477 is an effective and specific MCL-1 and Bcl-2 inhibitor (Ki/IC50: 0.454/26.2 nM).
Targets&IC50	MCL1:26.2 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]
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	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)

Molecular Weight	850.04
Formula	C46H55N7O7S
CAS No.	1668553-26-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: Insoluble

H2O: 10 mM

References and Literature

1. Leverson JD, et al. Cell Death Dis. 2015, 6:e1590. doi: 10.1038/cddis.2014.561. 2. Xiao Y, et al. Mol Cancer Ther. 2015, 14(8), 1837-1847. 3. Phillips DC, et al. Blood Cancer J. 2015, 5:e368. doi: 10.1038/bcj.2015.88.

Citations

1. Zhu P J, Yu Z Z, Lv Y F, et al. Discovery of 3, 5-Dimethyl-4-Sulfonyl-1 H-Pyrrole-Based Myeloid Cell Leukemia 1 Inhibitors with High Affinity, Selectivity, and Oral Bioavailability. Journal of Medicinal Chemistry. 2021, 64(15): 11330-11353.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Active Compound Library Highly Selective Inhibitor Library PPI Inhibitor Library Anti-COVID-19 Compound Library Bioactive Compounds Library Max Target-Focused Phenotypic Screening Library Bioactive Compound Library Anti-Cancer Compound Library Anti-Aging Compound Library

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Keywords

A-1210477 1668553-26-1 Apoptosis BCL inhibit Inhibitor A 1210477 Bcl-2 Family A1210477 inhibitor

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