Iruplinalkib (WX-0593) | ALK inhibitor

Chemical Structure : Iruplinalkib

CAS No.: 1854943-32-0

Iruplinalkib (WX-0593, WX0593)

Catalog No.: PC-73422Not For Human Use, Lab Use Only.

Iruplinalkib (WX-0593) is a potent ALK inhibitor, inhibits the activity of both wild type (IC50=5.38 nM) and resistant mutants of ALK (ALKL1196M IC50=9.26 nM) in vitro, and overcomes crizotinib-resistant mutations.

Packing	Price	Stock
5 mg	$138	In stock
10 mg	$228	In stock
25 mg	$398	In stock
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Biological Activity

Iruplinalkib (WX-0593) is a potent ALK inhibitor, inhibits the activity of both wild type (IC50=5.38 nM) and resistant mutants of ALK (ALKL1196M IC50=9.26 nM) in vitro, and overcomes crizotinib-resistant mutations.
WX-0593 displayed potent enzymatic activities for ALKWT, ALKL 1196M, ALK C1156Y and EGFR L858R/T790M with IC50 of 5.38, 9.26, 9.28, and 16.74 nM respectively.
WX-0593 also showed expected anti-proliferative activity in six cell lines, Karpas-299, Ba/F3, Ba/F3 (EML4-ALK-WT), Ba/F3 (EML4-ALK-L1196M), Ba/F3 (EML4-ALK-C1156Y), and NCI-H1975, with IC50 of 4.5, 2208, 4, 9.5, 9, and 508 nM, respectively.
WX-0593 could fully inhibit p-ALK, p-ERK,p-STAT5 at 11.1 nM and p-AKT at 100 nM in NCI-H3122 cells.
WX-0593 can inhibit the activity of both wide type and crizotinib resistant ALK and showed strong antitumor activity in in vitro and in vivo preclinical models.

Physicochemical Properties

M.Wt	569.087
Formula	C29H38ClN6O2P
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 DMSO
Chemical Name/SMILES	(2-((5-chloro-2-((2-methoxy-4-(9-methyl-3,9-diazaspiro[5.5]undecan-3-yl)phenyl)amino)pyrimidin-4-yl)amino)phenyl)dimethylphosphine oxide

References

1. Liu X, et al. Bioorg Med Chem Lett. 2022 Apr 11;66:128730.

2. Shi Y, et al. Signal Transduct Target Ther. 2022 Jan 28;7(1):25.

3. Liu Xile, et al. Cancer Research 78(13 Supplement):4794-4794.

Iruplinalkib (WX-0593, WX0593)

Biological Activity

Physicochemical Properties

References

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