1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR
  2. EGFR mTOR
  3. BIEGi-1

BIEGi-1 是一种 EGFR 抑制剂。BIEGi-1 在细胞中有效破坏 EGFR-Rheb 相互作用。BIEGi-1 在 EGFR 突变细胞中显著抑制 EGFR 激酶活性 (降低 p-Y1068-EGFR) 以及 mTORC1 活化 (降低 p-T389-S6K1)。BIEGi-1 对 EGFR 突变的 PC9 和 HCC827 细胞表现出强效的抗增殖作用,IC50 值分别为 17 nM 和 20 nM。BIEGi-1 可用于研究携带 EGFR 突变的癌症,如非小细胞肺癌 (NSCLC)。

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BIEGi-1

BIEGi-1 Chemical Structure

CAS No. : 1429497-30-2

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BIEGi-1 is an EGFR inhibitor. BIEGi-1 effectively disrupts the EGFR-Rheb interaction in cells. BIEGi-1 robustly inhibits EGFR kinase activity (reduces p-Y1068-EGFR) as well as mTORC1 activation (reduces p-T389-S6K1) in EGFR-mutant cells. BIEGi-1 shows strong antiproliferative effects on EGFR-mutant PC9 and HCC827 cells with IC50 values of 17 nM and 20 nM, respectively. BIEGi-1 can be used for the study of cancers harboring EGFR mutations, such as non-small cell lung cancer (NSCLC)[1].

IC50 & Target[1]

mTORC1

 

体外研究
(In Vitro)

BIEGi-1 (25 nM, 12 h) 在 PC9 细胞 (EGFR 突变) 中有效破坏 EGFR 与 Rheb 之间的相互作用[1]
BIEGi-1 (25 nM, 12 h) 在 EGFR 突变的 PC9 和 HCC827 细胞中强效抑制 EGFR 激酶活性 (降低 p-Y1068-EGFR) 以及 mTORC1 激活 (降低 p-T389-S6K1)[1]
BIEGi-1 (0.01-10000 nM, 72 h) 对 PC9 和 HCC827 细胞表现出强效的抗增殖作用,IC50 分别为 17 nM 和 20 nM[1]
BIEGi-1 (200 nM, 24 h) 在血清饥饿的 HEK-293T 细胞中,抑制由溶酶体定位的 LAMP2-V5-EGFR-TKD (野生型和激酶失活型) 诱导的 mTORC1 激活[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: EGFR-mutant PC9 and HCC827 cells
Concentration: 25 nM
Incubation Time: 12 h
Result: Reduced p-Y1068-EGFR and p-T389-S6K1 in EGFR-mutant PC9 and HCC827 cells.
分子量

615.72

Formula

C36H37N7O3

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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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:
BIEGi-1
目录号:
HY-17654
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