2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. EGFR-IN-49

EGFR-IN-49 是一种有效的选择性 EGFR 抑制剂，对 EGFRT790M 和 EGFRT790M/L858R 的IC50 值分别为 65.0 nM 和 13.6 nM。EGFR-IN-49 以剂量依赖性方式诱导细胞晚期凋亡 (apoptosis)。

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EGFR-IN-49 Chemical Structure

EGFR-IN-49 Chemical Structure

CAS No. : 2459932-81-9

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EGFR-IN-49 相关抗体

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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EGFR-IN-49 is a potent and selective EGFR inhibitor with IC50s of 65.0 nM and 13.6 nM for EGFRT790M and EGFRT790M/L858R, respectively. EGFR-IN-49 induces late apoptosis in a dose-dependent manner[1].

IC50 & Target[1]

EGFRT790M

65.0 nM (IC50)

EGFRL858R/T790M

13.6 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A-431 IC50
3.79 μM
Compound: 13a
Antiproliferative activity against human A-431 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against human A-431 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
[PMID: 32679450]
A549 IC50
4.34 μM
Compound: 13a
Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
[PMID: 32679450]
HeLa IC50
6.39 μM
Compound: 13a
Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
[PMID: 32679450]
L02 IC50
> 50 μM
Compound: 13a
Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
[PMID: 32679450]
MCF7 IC50
18.99 μM
Compound: 13a
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
[PMID: 32679450]
NCI-H1975 IC50
699.2 nM
Compound: 13a
Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as inhibition of cell viability measured after 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as inhibition of cell viability measured after 72 hrs by MTT assay
[PMID: 32679450]
体外研究
(In Vitro)

EGFR-IN-49 (compound 13a) (1, 10 µM) shows inhibition activity for H1975 cells with an IC50 of 699.2 nM[1].
EGFR-IN-49 (1 µM) shows an strong inhibitory activity to EGFRT790M, EGFRT790M/L858R, EGFRWT with IC50s of 65.0, 13.6, >1000 nM, respectively[1].
EGFR-IN-49 (0.2, 4, 8 µM; 48 h) induces cell apoptosis in a dose-dependent manner in A431 cells[1].

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

EGFR-IN-49 相关抗体:

Cell Proliferation Assay[1]

Cell Line: A549, A431, Hela, MCF7, LO2 cells
Concentration: 0-50 µM
Incubation Time:
Result: Showed excellent anti-proliferative activities with IC50s of 4.34, 3.79, 6.39, 18.99, >50 µM for A549, A431, Hela, MCF7, LO2 cells, respectively.

Apoptosis Analysis[1]

Cell Line: A431 cells
Concentration: 0.2, 4, 8 µM
Incubation Time: 48 h
Result: Induced cell apoptosis in a low concentration (0.33 µM) and exhibited higher percent of 16.41% % in the stage of late apoptotic at concentration of 4 µM.
分子量

413.45

Formula

C22H15N5O2S
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-49 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

EGFR-IN-492459932-81-9EGFREpidermal growth factor receptorErbB-1HER1SelectiveapoptosisA431 cellsEGFRT790MEGFRT790M/L858Rdose-dependent manneranti-proliferationlow cytotoxicInhibitorinhibitorinhibit

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