2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Cell Cycle/DNA Damage Apoptosis
  3. EGFR CDK Apoptosis Caspase Bcl-2 Family
  4. EGFR/CDK2-IN-5

EGFR/CDK2-IN-5 是一种强效的 EGFR 和 CDK2 双重抑制剂，其 IC50 值分别为 17.30 nM 和 212.10 nM。EGFR/CDK2-IN-5 还能抑制 EGFRT790M，IC50 值为 123.8 nM。EGFR/CDK2-IN-5 具有显著的抗癌活性。EGFR/CDK2-IN-5 可诱导 G1 期和 S 期细胞周期阻滞和细胞凋亡 (apoptosis)，并伴有 caspase-3/9 和 Bax 水平升高以及 Bcl-2 水平降低。EGFR/CDK2-IN-5 可用于肺癌、乳腺癌和白血病等癌症的研究。

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EGFR/CDK2-IN-5

EGFR/CDK2-IN-5 Chemical Structure

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EGFR/CDK2-IN-5 相关抗体

Top Publications Citing Use of Products

查看 EGFR 亚型特异性产品:

查看所有亚型
EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

查看 CDK 亚型特异性产品:

查看所有亚型
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

查看 Caspase 亚型特异性产品:

查看所有亚型
Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

查看 Bcl-2 Family 亚型特异性产品:

查看所有亚型
Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EGFR/CDK2-IN-5 is a potent dual EGFR and CDK2 inhibitor with IC50s of 17.30 and 212.10 nM, respectively. EGFR/CDK2-IN-5 also inhibits EGFRT790M with an IC50 of 123.8 nM. EGFR/CDK2-IN-5 exhibits potent anticancer activity. EGFR/CDK2-IN-5 induces G1 and S cell cycle arrest and apoptosis, accompanied by increased levels of caspase-3/9 and Bax, as well as decreased Bcl-2 levels. EGFR/CDK2-IN-5 can be used for the research of cancers, such as lung cancer, breast cancer, and leukemia[1].

IC50 & Target[1]

CDK2

212.10 nM (IC50)

EGFR

17.30 nM (IC50)

EGFRT790M

123.8 nM (IC50)

Caspase-9

 

Caspase-3

 

Bcl-2

 

Bax

 

体外研究
(In Vitro)

EGFR/CDK2-IN-5 (compound 7c) (48 小时) 在多种癌细胞中表现出广谱活性，对 HCT-116 和 LOX-IMVI 细胞的活性强，IC50 值分别为 11.3 和 20.03 μM，而对正常细胞 WI-38 和 Vero 细胞的细胞毒性较低 (IC50 > 50 μM)[1]。
EGFR/CDK2-IN-5 (11.3-20.03 μM，24 小时) 在 HCT-116 中引起 G1 期阻滞，在 LOX-IMVI 中引起 S 期阻滞，并诱导两种细胞发生凋亡[1]。
EGFR/CDK2-IN-5 (5.65 μM，24 小时) 在 HCT-116 细胞中降低了 EGFR、pEGFR、pCDK2 和 CDK2 蛋白的表达[1]。
EGFR/CDK2-IN-5 (11.3 μM，48 h) 可增加 HCT-116 细胞中 caspase-3/9 和 Bax 的基因表达水平以及 BAX/Bcl-2 比率，同时降低 Bcl-2 的基因表达水平[1]。

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

EGFR/CDK2-IN-5 相关抗体:

Cell Cycle Analysis[1]

Cell Line: HCT-116, LOX-IMVI
Concentration: 11.3 μM (HCT-116), 20.03 μM (LOX-IMVI)
Incubation Time: 24 h
Result: Caused G1 phase arrest in HCT-116 and S phase arrest in LOX-IMVI.

Western Blot Analysis[1]

Cell Line: HCT-116
Concentration: 5.65 μM
Incubation Time: 24 h
Result: Reduced the expression of EGFR, pEGFR, CDK2, and pCDK2 in HCT-116 cells.

Apoptosis Analysis[1]

Cell Line: HCT-116, LOX-IMVI
Concentration: 11.3 μM (HCT-116), 20.03 μM (LOX-IMVI)
Incubation Time: 24 h
Result: Induced apoptosis in n HCT-116 and LOX-IMVI cells.

RT-PCR[1]

Cell Line: HCT-116
Concentration: 11.3 μM
Incubation Time: 48 h
Result: Increased the mRNA levels of Bax, caspase-3, and caspase-9.
Increased BAX/Bcl-2 ratio.
Decreased Bcl-2 mRNA levels.
分子量

508.61

Formula

C31H32N4O3
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

EGFR/CDK2-IN-5 相关分类

  • 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.

Keywords:

EGFR/CDK2-IN-5EGFRCDKApoptosisCaspaseBcl-2 FamilyEpidermal growth factor receptorErbB-1HER1Cyclin dependent kinaseCell cycleCytotoxicityCDK2Inhibitorinhibitorinhibit

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