1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Metabolic Enzyme/Protease
  2. EGFR Anaplastic lymphoma kinase (ALK) Cytochrome P450
  3. DA-0157

DA-0157 是一种口服有效的 EGFRALK 抑制剂,可以克服非小细胞肺癌(NSCLC)中 EGFR 和 ALK 的耐药突变。DA-0157 可抑制 Ba/F3-EGFR Del19/T790M/C797S (IC50 = 6.9 nM)、Ba/F3-EGFR WT (IC50 = 0.83 μM)、Ba/F3-EML4-ALK-L1196M (IC50 = 5.5 nM) 和 Ba/F3-EML4-ALK (IC50 = 7.4 nM) 的增殖。 DA-0157 抑制 CYP2D6IC50 为 5.26 μM。DA-0157 在小鼠模型中表现出抗肿瘤活性。

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DA-0157

DA-0157 Chemical Structure

CAS No. : 2756978-82-0

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

DA-0157 is the orally active inhibitor for EGFR and ALK that overcomes drug-resistant mutations of EGFR C797S and ALK in NSCLC) cells. DA-0157 inhibits the proliferation of Ba/F3-EGFR Del19/T790M/C797S (IC50 = 6.9 nM), Ba/F3-EGFR WT (IC50 = 0.83 μM), Ba/F3-EML4-ALK-L1196M (IC50 = 5.5 nM), and Ba/F3-EML4-ALK (IC50 = 7.4 nM). DA-0157 inhibits CYP2D6 with IC50 of 5.26 μM. DA-0157 exhibits antitumor efficacy in mouse models[1].

分子量

656.60

Formula

C31H43BrN7O2P

CAS 号
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.

纯度 & 产品资料
参考文献
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  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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DA-0157
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HY-170928
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