A-1210477

Hersteller MedChem Express
Kategorie
Typ Inhibitors
Specific against other
Menge 5mg
ArtNr HY-12468-5mg
eClass 6.1 30220300
eClass 9.0 32160605
Lieferbar
CAS No.
1668553-26-1
Purity
>98%
MW
8500366
Formula
C46H55N7O7S
Solubility
DMSO: ? 4.8 mg/mL
Biological Description
A-1210477 is a potent and selective inhibitor of MCL-1, and weakly binds to BCL-2 and BCL-XL, with Ki of 0.45 nM, 132 nM and >660 nM, respectively.
IC50 & Target: Ki: 0.45 nM (MCL-1), 132 nM (BCL-2), >660 nM (BCL-XL)[1]
In Vitro: A-1210477 (10?uM) reduces the amount of BIM co-immunoprecipitated with MCL-1 antibody, and triggers MCL-1 elevation in a variety of cancer cell lines, including the breast cancer cell line HCC-1806. A-1210477 inhibits MCL-1-NOXA interactions with an IC50 of approximately 1?uM, while having no effect on BCL-2-BIM or BCL-XL-BCL-XS interactions. The NSCLC cell lines H2110 and H23 are sensitive to A-1210477 with cell viability IC50<10?uM, confirming that A-1210477 can kill MCL-1-dependent cell lines[1]. A-1210477 induces extensive concentration-dependent apoptosis in H929 cells following a brief (4?h) exposure. A-1210477 interacts with MCL-1 with Kd of appr 740?nM. A-1210477 (10?uM) induces extensive mitochondrial fragmentation in a DRP-1-dependent manner[2]. A-1210477 upregulates MCL-1 expression in BRAF-mutant CRC cells and in the melanoma cell line A375 in a dose-dependent manner. A-1210477 releases BAK from MCL-1 and cobimetinib induces BIM that is required for BAX activation[3]. A-1210477 (0, 5, 10 and 15?uM) has minimal effect on cell viability but substantially sensitizes resistant BCL2High NHL cell lines to navitoclax[4].
Publications
Open Biol. 2016 Aug; 6(8). pii: 160134.
Menge: 5mg
Lieferbar: In stock
Listenpreis: 120,71 €
Rabatt: -10,0%
Preis: 108,64 €
Sie sparen: 12,07 €
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