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Chemical Structure : Iruplinalkib
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.
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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.
| M.Wt | 569.087 | |
| Formula | C29H38ClN6O2P | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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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.
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