Sunvozertinib (Synonyms: DZD9008) |
| رقم الكتالوجGC63521 |
Sunvozertinib (DZD9008) هو أحد مثبطات ErbBs (EGFR ، Her2 ، وخاصة الأشكال الطافرة) ومثبط BTKيعرض Sunvozertinib IC50s من 20.4 و 20.4 و 1.1 و 7.5 و 80.4 نانومتر لإدخال EGFR exon 20 NPH وإدخال EGFR exon 20 ASV وطفرات EGFR L858R و T790M و Her2 Exon20 YVMA و EGFR WT A431 ، على التوالي (براءة اختراع WO2019149164A1 ، على التوالي) 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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