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Home > Bcl-2 Protein Inhibitors/Degraders > MCL-1 Selective Inhibitors > A-1210477

A-1210477

A-1210477 is a proteolytically stable, cell-permeable and high affinity BH3 mimetics of anti-apoptotic protein MCL-1, binding to the target potently and selectively with a Ki value of 0.45 nM, highly selective against closely related proteins of BCL-2 (Ki = 132 nM, >290-fold selectivity) and BCL-XL (Ki > 660 nM, >1400-fold selectivity). A-1210477 is the first-in-class small molecule MCL-1 inhibitor with sufficient potency to disrupt the tight-binding MCL-1-BIM complex in living cells, achieving the hallmarks of intrinsic apoptosis, and demonstrating clear-on-target cancer cell killing capability either as a single agent or in combination with ABT-263 (Navitoclax).

Catalog NO:	CT-A121
Synonym:	A1210477
CAS NO:	1668553-26-1
Mol. Formula:	C₄₆H₅₅N₇O₇S ∙ 0.5xHCl
MW:	868.3

** A snow-white recrystallized crystalline powder (see attached picture), clean (>99.5% by HPLC) + impeccable 1H-NMR, + a perfect Quantitative Elemental Analysis. BULK STOCK!!!. Ship within 1 day.

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NO	Size	Price	In Stock	Quantity
1	10 mg	$100.00	YES
2	50 mg	$225.00	YES
3	100 mg	$395.00	YES

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Solubility : Soluble in DMSO

Storage : Store at 0°C (short term), -20°C (long term), desiccated

Purity : >99% (HPLC at 214 and 254 nm)

Original QC Data : HPLC-MS, ¹HNMR, and Quantitative Elemental Analysis

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Current Lot, Certificate of Analysis
A-1210477, lot 01, Appearance (color).pdf

JD Leverson, et al, Potent and selective small-molecule MCL-1inhibitors demonstrate on-target cancer cell killing activity as single agents and in combination with ABT-263(navitoclax), Cell Death & Disease (2015) 6, e1590; doi: 10.1038/cddis.2014.561

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