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Sunvozertinib

SKU: orb1685916

描述

Sunvozertinib (DZD9008) is a selective small molecule inhibitor targeting EGFR and Her2 mutations, including various exon 20 insertions and the L858R/T790M double mutation. It has demonstrated potent activity in preclinical in vitro and in vivo models of non-small cell lung cancer (NSCLC), supporting its investigation for targeted cancer therapy.

研究领域

Cardiovascular Research, Signal Transduction

图片与验证

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关键属性

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CAS 号2370013-12-8
MW584.08
纯度99.71% (May vary between batches)
分子式C29H35ClFN7O3
SMILESCOc1cc(N2CC[C@H](C2)N(C)C)c(NC(=O)C=C)cc1Nc1nccc(Nc2cc(Cl)c(F)cc2C(C)(C)O)n1
靶点EGFR,BTK
溶解性10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (8.56 mM);DMSO:247.5 mg/mL (423.74 mM)

生物活性

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靶点 IC50
HER2 exon20 YVMA:7.5 nM|EGFR (L858R/T790M):1.1 nM|EGFR (exon 20 insertion):20.4 nM
体内
METHODS: Blood samples from the LU3075 PDX mouse model were collected at 0.5, 1, 2, 4, 8, and 24 hours after administration of sunvozertinib (DZD9008) (12.5, 25, and 50 mg/kg, orally, twice daily) on day 28 for LC/MS-MS analysis. RESULTS Oral sunvozertinib (DZD9008) showed profound anti-tumor efficacy in a dose-dependent manner.
体外
METHODS: To test the cellular activity of Sunvozertinib (DZD9008) , 14 different EGFRexon20ins were engineered into the Ba/F3 cell line. RESULTS In these cell lines, Sunvozertinib (DZD9008) showed potent pEGFR downregulation activity with IC50 ranging from 6 to 40 nM; in other cell lines expressing EGFR sensitive mutations, T790M resistance mutations, and rare mutations, Sunvozertinib (DZD9008) downregulated pEGFR more effectively with IC50 ranging from 1.1 to 12 nM; in the A431 cell line overexpressing wild-type EGFR, Sunvozertinib (DZD9008) was less potent in downregulating pEGFR with an IC50 of 58 nM.

储存与操作

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储存-20°C
有效期12 months from date of receipt.
免责声明For research use only

别名

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EGFR, DZD 9008, DZD9008, DZD-9008, BTK, Sunvozertinib

相似产品

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  • Sunvozertinib [orb3032913]

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  • (S)-Sunvozertinib [orb1298200]

    99.69% (May vary between batches)

    2370013-49-1

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    50 mg, 100 mg, 1 mg, 5 mg, 10 mg, 25 mg, 1 ml x 10 mM (in DMSO)
质量保证

质量保证

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our 条款与条件和选购指南.

关键属性

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暂无计算属性。

实验方案信息

可选规格

请在下方选择规格

1 mg
¥ 910.00
5 mg
¥ 1,300.00
10 mg
¥ 1,690.00
25 mg
¥ 2,340.00
1 ml x 10 mM (in DMSO)
¥ 2,730.00
50 mg
¥ 3,510.00
100 mg
¥ 5,720.00
500 mg
¥ 19,500.00
发货Usually dispatched within 5-10 working days
批量询价