ER121 | EGFR inhibitor | Probechem Biochemicals

Chemical Structure : ER121

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ER121 (ER-121)

货号: 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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25 mg		Get quote
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100 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	487.96
分子式	C24H27ClFN5O3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(E)-N-(4-((3-chloro-4-fluorophenyl)amino)-7-ethoxyquinazolin-6-yl)-4-((3-hydroxypropyl)(methyl)amino)but-2-enamide

参考文献

1. Goel PN, et al. Biochem Biophys Res Commun. 2023 Apr 9;651:39-46.

ER121 (ER-121)

生物&药学活性

物理化学性质&存储条件

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ER121 (ER-121)

生物&药学活性

物理化学性质&存储条件

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