Enozertinib (ORIC-114) | EGFR inhibitor | Probechem Biochemicals

Chemical Structure : Enozertinib

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Enozertinib (ORIC-114, ORIC114)

货号: PC-24132Not For Human Use, Lab Use Only.

Enozertinib (ORIC-114) is a potent, brain penetrant, orally bioavailable, irreversible inhibitor of exon 20 insertions in EGFR and HER2.

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生物&药学活性

Enozertinib (ORIC-114) is a potent, brain penetrant, orally bioavailable, irreversible inhibitor of exon 20 insertions in EGFR and HER2.

ORIC-114 is highly selective for the EGFR family of receptors, with excellent kinome selectivity compared to other reported exon 20 inhibitors, reducing the risk of off-target kinase liabilities.

ORIC-114 administration (3 mg/kg, once daily oral) induced robust tumor regressions with greater than 100% tumor growth inhibition in the absence of significant body weight loss in an EGFR exon 20 insertion H773_V774insNPH NSCLC PDX model.

物理化学性质&存储条件

分子量	660.77
分子式	C35H42F2N8O3
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	2-Propenamide, N-[2-[4-(4-cyclopropyl-1-piperazinyl)-1-piperidinyl]-5-[[6-[(3R)-3-(3,5-difluorophenyl)-2-isoxazolidinyl]-4-pyrimidinyl]amino]-4-methoxyphenyl]-

参考文献

1. Patent WO2020190119 A1.
2. Jason E. Long, et al. Cancer Res (2022) 82 (12_Supplement): 3335.

Enozertinib (ORIC-114, ORIC114)

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Enozertinib (ORIC-114, ORIC114)

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