2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. EGFR-IN-208

EGFR-IN-208 是一种变构突变型 EGFRL858R/T790M、EGFRL858R/T790M/C797S 抑制剂，IC50 分别为 3.06 和 1.08 μM。EGFR-IN-208 可结合 EGFR 变构位点并抑制 EGFR 磷酸化。EGFR-IN-208 可诱导细胞凋亡 (apoptosis)，并在癌细胞中表现出抗增殖作用。EGFR-IN-208 可用于非小细胞肺癌的相关研究。

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EGFR-IN-208

EGFR-IN-208 Chemical Structure

CAS No. : 3087298-90-3

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EGFR-IN-208 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

  • 生物活性

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  • 参考文献

生物活性

EGFR-IN-208 is an allosteric mutant EGFRL858R/T790M and EGFRL858R/T790M/C797S inhibitor, with IC50 values of 3.06 μM and 1.08 μM, respectively. EGFR-IN-208 binds to the allosteric site of EGFR and inhibits EGFR phosphorylation. EGFR-IN-208 induces apoptosis and exhibits antiproliferative effects in cancer cells. EGFR-IN-208 can be used in research related to non-small cell lung cancer[1].

IC50 & Target[1]

EGFRL858R/T790M

1.08 μM (IC50)

EGFRL858R/T790M/C797S

3.06 μM (IC50)

体外研究
(In Vitro)

EGFR-IN-208 (Compound 2b) 可强效抑制 A549 (EGFRWT)、H3255 (EGFRL858R)、PC-9 (EGFRDel19)、H1975 (EGFRL858R/T790M) 及 Ba/F3 (EGFRL858R/T790M/C797S) 细胞的增殖，其 IC50 值范围为 1.08 μM 至 4.33 μM，对 Ba/F3 细胞的抑制活性最强[1]。
EGFR-IN-208 (0.1-3 μM) 可在 H1975 细胞和 Ba/F3-EGFRL858R/T790M/C797S 细胞中以浓度依赖的方式抑制 EGFR 磷酸化，且不改变总 EGFR 蛋白水平[1]。
EGFR-IN-208 (0.5-5 μM); 48 h) 可在 48 小时内以剂量依赖方式诱导 H1975 细胞和 Ba/F3-EGFRL858R/T790M/C797S 细胞发生凋亡，在测试浓度范围内的凋亡率为 12.98%至 51.8%[1]。

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

EGFR-IN-208 相关抗体:

Apoptosis Analysis[1]

Cell Line: H1975 (EGFRL858R/T790M), Ba/F3-EGFRL858R/T790M/C797S
Concentration: 1, 3 and 5 μM (H1975 cells); 0.5, 1 and 1.5 μM (Ba/F3-EGFRL858R/T790M/C797S cells)
Incubation Time: 48 h
Result: Induced dose-dependent apoptosis in both cell lines.
Increased apoptotic rates of H1975 cells to 12.98%, 22.64%, and 36.8% at 1, 3, and 5 μM respectively, with statistically significant increases relative to DMSO control.
Increased apoptotic rates of Ba/F3-EGFRL858R/T790M/C797S cells to 20.41%, 40.1%, and 51.8% at 0.5, 1.0, and 1.5 μM respectively, with statistically significant increases relative to DMSO control.
分子量

519.61

Formula

C32H30FN5O
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

EGFR-IN-208 相关分类

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Keywords:

EGFR-IN-2083087298-90-3EGFREpidermal growth factor receptorErbB-1HER1H1975 cellsmutant EGFRH3255 cellsEGFR allosteric sitesEGFR phosphorylationA549 cellsnon-small cell lung cancerEGFR (L858R/T790ML858R/T790M/C797S)PC-9 cellscell apoptosisInhibitorinhibitorinhibit

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