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Chemical Structure : GNS-1481
Catalog No.: PC-60919Not For Human Use, Lab Use Only.
A novel potent, irreversible, T790M mutant-selective inhibitor of mutant EGFR with IC50 of 6.2, 3.4 and 4.2 nM for L858R-T790M, T790M and Del19-T790M, respectively.
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GNS-1481 is a potent, irreversible, T790M mutant-selective inhibitor of mutant EGFR with IC50 of 6.2, 3.4 and 4.2 nM for L858R-T790M, T790M and Del19-T790M, respectively.
GNS-1481 displays >5-fold selectivity over wild type EGFR (IC50=26.5 nM) and L858R mutant (IC50=25.8 nM).
GNS-1481 demonstrates effectivity in multiple mouse xenograft models of human lung adenocarcinoma (T790M-positive or -negative), exhibiting less activity against wild-type EGFR than existing approved EGFR kinase inhibitors (including osimertinib).
GNS-1481 also shows superior potency against intracranial metastasis of EGFR-mutant lung adenocarcinoma.
| M.Wt | 518.622 | |
| Formula | C27H34N8O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Rho JK, et al. Cancer Res. 2017 Mar 1;77(5):1200-1211.
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