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A-1210477

Chemical Structure : A-1210477

CAS No.: 1668553-26-1

A-1210477 (A1210477)

Catalog No.: PC-43048Not For Human Use, Lab Use Only.

A-1210477 is a potent, selective Mcl-1 inhibitor that bind to Mcl-1 (Ki=0.45 nM) to disrupt MCL-1-BIM complexes, shows much weaker against Bcl-2 (Ki=132 nM) and Bcl-XL (Ki>660 nM).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

A-1210477 is a potent, selective Mcl-1 inhibitor that bind to Mcl-1 (Ki=0.45 nM) to disrupt MCL-1-BIM complexes, shows much weaker against Bcl-2 (Ki=132 nM) and Bcl-XL (Ki>660 nM).
A-1210477 induces the hallmarks of intrinsic apoptosis and demonstrates single agent killing of multiple myeloma and non-small cell lung cancer cell lines.
A-1210477 synergizes with the BCL-2/BCL-XL inhibitor navitoclax to kill a variety of cancer cell lines.
A-1210477 also enhances cobimetinib-induced apoptosis in vitro.

Physicochemical Properties

M.Wt 850.0366
Formula C46H55N7O7S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: < 4.8 mg/mL

Chemical Name/SMILES

1H-Indole-2-carboxylic acid, 7-[5-[[4-[4-[(dimethylamino)sulfonyl]-1-piperazinyl]phenoxy]methyl]-1,3-dimethyl-1H-pyrazol-4-yl]-1-[2-(4-morpholinyl)ethyl]-3-[3-(1-naphthalenyloxy)propyl]-

References

1. Leverson JD, et al. Cell Death Dis. 2015 Jan 15;6:e1590.

2. Xiao Y, et al. Mol Cancer Ther. 2015 Aug;14(8):1837-47.

3. Phillips DC, et al. Blood Cancer J. 2015 Nov 13;5:e368.

4. Karpel-Massler G, et al. Cancer Res. 2017 Jul 1;77(13):3513-3526.

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