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Rezivertinib

Chemical Structure : Rezivertinib

CAS No.: 1835667-12-3

Rezivertinib (BPI-7711)

Catalog No.: PC-38343Not For Human Use, Lab Use Only.

Rezivertinib (BPI-7711) is a novel third-generation EGFR tyrosine kinase inhibitor selective for EGFR-sensitizing and T790M mutations, shows potential against T790M-mediated drug resistance.

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Biological Activity

Rezivertinib (BPI-7711) is a novel third-generation EGFR tyrosine kinase inhibitor selective for EGFR-sensitizing and T790M mutations, shows potential against T790M-mediated drug resistance.
Rezivertinib (BPI-7711) specifically and covalently binds to and inhibits selective EGFR mutations, with particularly high selectivity against the T790M mutation, prevents EGFR mutant-mediated signaling and leads to cell death in EGFR mutant-expressing tumor cells.
Rezivertinib (BPI-7711) shows minimal activity against wild-type EGFR (wt EGFR), and does not cause dose-limiting toxicities that occur during the use of non-selective EGFR inhibitors, which also inhibit wt EGFR.

Physicochemical Properties

M.Wt 486.576
Formula C27H30N6O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-[2-[2-(dimethylamino)ethoxy]-4-methoxy-5-[[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino]phenyl]prop-2-enamide

References

1. Yuankai Shi, et al. J Thorac Oncol. 2022 Feb 15;S1556-0864(22)00084-3.

2. Nagasaka M, et al. J Thorac Oncol. 2021 May;16(5):740-763.

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