EGFR-IN-45

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

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 EGFR 和 CDK2 的 IC50 分别为 0.4 µM 和 1.6 µM。EGFR-IN-45 也抑制拓扑异构酶 Topo I 和 Topo II。EGFR-IN-45 能将癌细胞抑制在 G1 前期，诱导细胞凋亡 (apoptosis)。

EGFR-IN-45

EGFR-IN-45 Chemical Structure

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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].

上海金畔生物科技有限公司 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
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.
参考文献

  • [1]. Mekheimer RA, Allam SMR, Al-Sheikh MA, et al. Discovery of new pyrimido[5,4-c]quinolines as potential antiproliferative agents with multitarget actions: Rapid synthesis, docking, and ADME studies. Bioorg Chem. 2022;121:105693.

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