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Brigatinib

Chemical Structure : Brigatinib

CAS No.: 1197953-54-0

Brigatinib (AP-26113;AP26113)

Catalog No.: PC-43260Not For Human Use, Lab Use Only.

Brigatinib (AP-26113, AP26113) is a potent, selective, second generation ALK inhibitor with IC50 of 0.62 nM, exhibits about fivefold greater potency in vitro compared with crizotinib.

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

Biological Activity

Brigatinib (AP-26113, AP26113) is a potent, selective, second generation ALK inhibitor with IC50 of 0.62 nM, exhibits about fivefold greater potency in vitro compared with crizotinib.
Brigatinib (AP-26113, AP26113) shows high activity against both sensitive and resistant H3122 cells, decreasing cell growth, suppressing ALK phosphorylation, and inducing apoptosis.
Brigatinib (AP-26113, AP26113) is also active in Ba/F3 cells expressing either native or mutant EML4-ALK with IC50 of 10 and 24 nM, respectively.
Brigatinib (AP-26113, AP26113) demonstrates promising activity in crizotinib resistant.

Physicochemical Properties

M.Wt 584.0924
Formula C29H39ClN7O2P
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

10 mM in Ethanol

Chemical Name/SMILES

2,4-Pyrimidinediamine, 5-chloro-N4-[2-(dimethylphosphinyl)phenyl]-N2-[2-methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]-

References

1. Katayama R, et al. Proc Natl Acad Sci U S A. 2011 May 3;108(18):7535-40.

2. Ceccon M, et al. Mol Cancer Res. 2013 Feb;11(2):122-32.

3. Ceccon M, et al. Mol Cancer Res. 2015 Apr;13(4):775-83.

4. Fontana D, et al. Cancer Med. 2015 Jul;4(7):953-65.

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