2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK MAPK/ERK Pathway Apoptosis
  3. EGFR Raf Apoptosis
  4. EGFR/BRAFV600E-IN-4

EGFR/BRAFV600E-IN-4 (Compound 10f) 是一种双重EGFR/BRAFV600E 抑制剂, IC50 值分别为 61 nM、43 nM。EGFR/BRAFV600E-IN-4 可阻止细胞周期，在早期和晚期诱导细胞凋亡 (apoptosis)，并在体外抑制癌细胞生长，具有广谱抗癌活性。

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EGFR/BRAFV600E-IN-4 Chemical Structure

EGFR/BRAFV600E-IN-4 Chemical Structure

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EGFR/BRAFV600E-IN-4 相关抗体

Top Publications Citing Use of Products

查看 EGFR 亚型特异性产品:

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

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BRaf c-Raf Raf

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EGFR/BRAFV600E-IN-4 (Compound 10f) is a dual EGFR and BRAFV600E inhibitor with IC50 values of 61 nM and 43 nM, respectively. EGFR/BRAFV600E-IN-4 arrests cell cycle, induces apoptosis in both early and late stages and inhibits cancer cells growth in vitro, and has a broad anticancer activity[1].

IC50 & Target[1]

BRafV600E

43 nM (IC50)

EGFR

61 nM (IC50)

体外研究
(In Vitro)

EGFR/BRAFV600E-IN-4 (0.01-100 μM) 具有广谱抗增殖活性，GI50 值范围为 1.66 至 > 100 μM。EGFR/BRAFV600E-IN-4 (0.01-100 μM) (1.56-100 nM, 48 小时) 可抑制 A-549、Panc-1、HT-29、MCF-7 细胞生长，IC50 值范围为 24 nM 至 27 nM，但对 MCF-10A 细胞相对安全，细胞存活率为 91%。 EGFR/BRAFV600E-IN-4 (24 nM, 24 小时) 将细胞停滞在 G0/G1 期并阻止从 G1 期向 S 和 G2/M 期的转变，在早期和晚期诱导细胞凋亡。

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

EGFR/BRAFV600E-IN-4 相关抗体:

Cell Proliferation Assay[1]

Cell Line: A-549, Panc-1, HT-29, MCF-7
Concentration: 1.56, 3.125, 6.25, 12.5, 25, 50, 100 nM
Incubation Time: 48 h
Result: Displayed significant anti-proliferative activity on A-549, Panc-1, HT-29, MCF-7with IC50 values of 24 nM, 25 nM, 25 nM, 27 nM, respectively.

Cell Cycle Analysis[1]

Cell Line: A-549
Concentration: 24 nM
Incubation Time: 24 h
Result: Revealed an increase in the percentage of accumulation of cells in the G0-G1 phase by 64.18 %.
The percentages of cell accumulation in the S and G2/M phases decreased from 31.44 % and 13.27 % in untreated cells to 24.05 % and 11.77 %, respectively.

Apoptosis Analysis[1]

Cell Line: A-549
Concentration: 24 nM
Incubation Time: 24 h
Result: Increased cells that entered both early and late apoptosis by 19.44 % and 11.13 %, respectively, while cells that got necrosis were only 3.3 %, indicating anti-proliferative activity.
分子量

384.45

Formula

C22H16N4OS
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/BRAFV600E-IN-4 相关分类

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  • 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/BRAFV600E-IN-4EGFRRafApoptosisEpidermal growth factor receptorErbB-1HER1Raf kinasesBRAFV600EapoptosisHT-29Panc-1MCF-7A-549anti-cancercell cycleInhibitorinhibitorinhibit

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