Mutated EGFR-IN-3

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Mutated EGFR-IN-3 

Mutated EGFR-IN-3，化合物 3，是 EGFR(L858R/T790M) 和 EGFR(L858R/T790M/C797S) 突变体的有效，具有 ATP 竞争性和高选择性的变构二苯并二氮杂酮抑制剂，抑制 EGFR(L858R/T790M) 和 EGFR(L858R/T790M/C797S) 的 IC50 值分别为 12 nM 和 13 nM。

Mutated EGFR-IN-3

Mutated EGFR-IN-3 Chemical Structure

CAS No. : 2375107-27-8

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生物活性

Mutated EGFR-IN-3 (compound 3) is a potent, ATP-competitive and highly selective allosteric dibenzodiazepinone inhibitor of the EGFR(L858R/T790M) and EGFR(L858R/T790M/C797S) mutants with IC50 values of 12 nM and 13 nM, respectively[1].

IC50 & Target[1]

EGFRL858R/T790M

12 nM (IC50)

EGFRC797S

13 nM (IC50)

体外研究
(In Vitro)

Mutated EGFR-IN-3 inhibits EGFR through an allosteric mechanism, biochemical IC50 values at varying ATP concentrations: 10 µM, 10.0 µM, 100.0 µM, 1000.0 µM are 15 nM, 8.3nM,11.0 nM and 8.3 nM, respectively for L858R/T790M cells[1].
Mutated EGFR-IN-3 exhibits antiproliferative activities of a panel of EGFR allosteric inhibitors are 7.0 µM, 3.3 µM, 3.8 µM, 4.0 µM and 4.5 µM for parental, WT, L858R, L858R/T790M and L858R/T790M/C797S, respectively in the absence of Cetuximab in Ba/F3 cells[1].
Mutated EGFR-IN-3 exhibits antiproliferative activities of a panel of EGFR allosteric inhibitors are 3.2 µM, 2.7 µM, 0.36 µM and 0.20 µM for WT,L858R, L858R/T790M and L858R/T790M/C797S, respectively in the presence of Cetuximab in Ba/F3 cells[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

508.59

Formula

C31H29FN4O2
CAS 号

2375107-27-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. De Clercq DJH，et al. Discovery and Optimization of Dibenzodiazepinones as Allosteric Mutant-Selective EGFR Inhibitors.ACS Med Chem Lett. 2019 Oct 22;10(11):1549-1553.

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