Sunvozertinib (Synonyms: DZD9008) |
| カタログ番号GC63521 |
Sunvozertinib (DZD9008) は強力な ErbB (EGFR、Her2、特に変異型) および BTK 阻害剤です。 Sunvozertinib は、EGFR エクソン 20 NPH 挿入、EGFR エクソン 20 ASV 挿入、EGFR L858R および T790M 変異、Her2 Exon20 YVMA、および EGFR WT A431 に対して、それぞれ 20.4、20.4、1.1、7.5、および 80.4 nM の IC50 を示します (特許 WO2019149164A1、例52)。
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Cas No.: 2370013-12-8
Sample solution is provided at 25 µL, 10mM.
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Sunvozertinib is a potent ErbBs (EGFR, Her2, especially mutant forms) and BTK inhibitor. Sunvozertinib shows IC50s of 20.4, 20.4, 1.1, 7.5, and 80.4 nM for EGFR exon 20 NPH insertion, EGFR exon 20 ASV insertion, EGFR L858R and T790M mutations, and Her2 Exon20 YVMA, and EGFR WT A431, respectively (patent WO2019149164A1, example 52)[1].
Sunvozertinib shows GI50s of 60.4, 83.2, 3.3, 101.3, and 47.1 nM for EGFR exon NPH insertion, EGFR exon 20 ASV insertion, EGFR L858R and T790M mutations, and Her2 Exon20 YVMA, and EGFR WT A431, respectively. Sunvozertinib shows GI50s of 3.2, 5.8, 51.3, and 1983.5 nM for BTK WT OCI-LY-10, BTK WT TMD-8, BTK WT Ri-1, and non-BCR activated DB, respectively[1].Sunvozertinib inhibits p-BTK with IC50 of 1.6 nM[1].
[1]. Zhengtao LI, et al. Erbb/btk inhibitors. WO2019149164A1.
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