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Chemical Structure : ER121
Catalog No.: PC-20174Not For Human Use, Lab Use Only.
ER121 (ER-121) is a potent, dual kinase inhibitor targeting both mutant EGFR and activated erbB2 with IC50 of 0.08/0.15 nM (EGFR C797S/EGFR WT, ATP=10 uM).
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ER121 (ER-121) is a potent, dual kinase inhibitor targeting both mutant EGFR and activated erbB2 with IC50 of 0.08/0.15 nM (EGFR C797S/EGFR WT, ATP=10 uM).
ER121 exhibits kinase inhibitory action in vitro for EGFR mutants with the T790 M and C797S mutations with IC50 value is in the sub-nM or nM region (10 uM ATP).
ER121 inhibits EGFR mutants more effectively than AZD9291.
ER121 (5 mg/kg and 15 mg/kg, oral) inhibited tumor growth in mice exhibiting C797S mutant tumors.
ER121 (5 mg/kg and 15 mg/kg, oral or i.p.) exhibits anti-tumor activity against Herceptin resistant breast tumors.
| M.Wt | 487.96 | |
| Formula | C24H27ClFN5O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Goel PN, et al. Biochem Biophys Res Commun. 2023 Apr 9;651:39-46.
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