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Sunvozertinib Sale

(Synonyms: DZD9008) 目录号 : GC63521

Sunvozertinib 是一种有效的 ErbBs (EGFR、Her2,尤其是突变型) 和 BTK 抑制剂。Sunvozertinib 显示 EGFR 外显子 20 NPH 插入、EGFR 外显子 20 ASV 插入、EGFR L858R 和 T790M 突变以及 Her2 外显子 20 YVMA 和 EGFR WT A431 的 IC50 分别为 20.4、20.4、1.1、7.5 和 80.4 nM (详细信息请参考专利 WO2019149164A1, example 52)。

Sunvozertinib Chemical Structure

Cas No.:2370013-12-8

规格 价格 库存 购买数量
5 mg
¥1,620.00
现货
10 mg
¥2,610.00
现货
25 mg
¥5,220.00
现货

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产品描述

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.

Chemical Properties

Cas No. 2370013-12-8 SDF
别名 DZD9008
分子式 C29H35ClFN7O3 分子量 584.08
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1 mg 5 mg 10 mg
1 mM 1.7121 mL 8.5605 mL 17.1209 mL
5 mM 0.3424 mL 1.7121 mL 3.4242 mL
10 mM 0.1712 mL 0.856 mL 1.7121 mL
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Research Update

Sunvozertinib, a Selective EGFR Inhibitor for Previously Treated Non-Small Cell Lung Cancer with EGFR Exon 20 Insertion Mutations

Cancer Discov 2022 Jul 6;12(7):1676-1689.PMID:35404393DOI:PMC9262839

Epidermal growth factor receptor exon 20 insertion mutations (EGFRexon20ins) are detected in approximately 2% of patients with non-small cell lung cancer (NSCLC). Due to a lack of effective therapy, the prognosis of these patients is typically poor. Sunvozertinib (DZD9008) was designed as an oral, potent, irreversible, and selective EGFR tyrosine kinase inhibitor, showing activity against EGFRexon20ins and other mutations. In both cell lines and xenograft models, Sunvozertinib shows potent antitumor activity. In the two ongoing phase I clinical studies, Sunvozertinib was tolerated up to 400 mg once daily. The most common drug-related adverse events included diarrhea and skin rash. Antitumor efficacy was observed at the doses of 100 mg and above in patients with EGFRexon20ins NSCLC across different subtypes, with prior amivantamab treatment as well as with baseline brain metastasis. The median duration of response has not been reached. Significance: We report the discovery and early clinical development of Sunvozertinib, a potential treatment option for the unmet medical need of EGFRexon20ins NSCLC. This article is highlighted in the In This Issue feature, p. 1599.