1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  2. EGFR
  3. Neptinib

Neptinib (NEP010) 是一种具有口服活性的 Afatinib (HY-10261) 衍生物,通过改善药代动力学具有比 Afatinib (HY-10261) 更强的抗肿瘤活性。Neptinib 对不同 EGFR 突变的小鼠非小细胞肺癌移植模型有显著的抑制肿瘤生长的作用。Neptinib 对 EGFR 激酶家族具有一定的抑制作用,对 EGFRwt, EGFRL858R/T790M, EGFRL858REGFRT790MIC50 值分别为 0.24 nM、7.25 nM、0.46 nM 和 1.79 nM。

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Neptinib Chemical Structure

Neptinib Chemical Structure

CAS No. : 2085843-51-0

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Neptinib (NEP010) is an orally active derivative of Afatinib (HY-10261) that has stronger antitumor activity than Afatinib (HY-10261) by improving pharmacokinetics. Neptinib has a significant inhibitory effect on tumor growth in mouse non-small cell lung cancer models with different EGFR mutations. Neptinib has a certain inhibitory effect on the EGFR kinase family, with IC50 values ??of 0.24 nM, 7.25 nM, 0.46 nM and 1.79 nM for EGFRwt, EGFRL858R/T790M, EGFRL858R and EGFRT790M, respectively[1].

IC50 & Target[1]

EGFR (WT)

0.24 nM (IC50)

EGFRL858R/T790M

7.25 nM (IC50)

EGFRL858R

0.46 nM (IC50)

EGFRT790M

1.79 nM (IC50)

分子量

443.90

Formula

C22H23ClFN5O2

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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产品名称:
Neptinib
目录号:
HY-164503
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