1. Cell Cycle/DNA Damage Protein Tyrosine Kinase/RTK JAK/STAT Signaling Apoptosis
  2. Topoisomerase EGFR CDK Apoptosis
  3. EGFR-IN-45

EGFR-IN-45 是一种有效的表皮生长因子受体 (EGFR) 泛抑制剂,对 EGFRCDK2IC50 分别为 0.4 µM 和 1.6 µM。EGFR-IN-45 也抑制拓扑异构酶 Topo ITopo II。EGFR-IN-45 能将癌细胞抑制在 G1 前期,诱导细胞凋亡 (apoptosis)。

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EGFR-IN-45 Chemical Structure

EGFR-IN-45 Chemical Structure

CAS No. : 2765560-03-8

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EGFR-IN-45 is a potent epidermal growth factor receptor (EGFR) pan inhibitor, with IC50s of 0.4 µM and 1.6 µM for EGFR and CDK2, respectively. EGFR-IN-45 also inhibit Topo I and Topo II. EGFR-IN-45 arrests cancer cells in the pre-G1 phase and induces apoptosis[1].

IC50 & Target[1]

CDK2

1.6 μM (IC50)

EGFR

0.4 μM (IC50)

体外研究
(In Vitro)

EGFR-IN-45 (compound 30b) (0-10 μM; 48 hours) exhibits the high anticancer activity against Panc-1, MCF-7, HT-29 and A-549[1].
EGFR-IN-45 (20 and 100 μM; hours) can inhibit Topo I and Topo II in a dose-dependent manner[1].
EGFR-IN-45 (0-8 μM; 24 hours) has a high percentage of cell accumulation in the pre-G1 phase in MCF-7[1].
EGFR-IN-45 (0-8 μM; 24 hours) induces high amounts of apoptosis, with a necrosis percent of 2.99[1].

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

Cell Proliferation Assay

Cell Line: Panc-1, MCF-7, HT-29 and A-549[1]
Concentration: 0-10 μM
Incubation Time: 48 hours
Result: Exhibited the high anticancer activity with IC50s of 0.9±0.20, 0.8±0.5, 1.3±0.3, 1.2±0.2 μM in Panc-1, MCF-7, HT-29 and A-549, respectively.

Cell Cycle Analysis

Cell Line: MCF-7[1]
Concentration: 0, 2, 4, 6 and 8 μM
Incubation Time: 24 hours
Result: Showed a high percentage of cell accumulation (36.02%) in the pre-G1 phase in MCF-7.

Apoptosis Analysis

Cell Line: MCF-7[1]
Concentration: 0, 2, 4, 6 and 8 μM
Incubation Time: 24 hours
Result: Induced high amounts of apoptosis, with a necrosis percent of 2.99.
分子量

473.53

Formula

C28H23N7O

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
  • 摩尔计算器

  • 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:
EGFR-IN-45
目录号:
HY-145867
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