2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. EGFR-IN-73

EGFR-IN-73 (Compound 3f) 是最常见的 EGFR 突变 EGFR Del19 的有效抑制剂，IC50 为 119 nM。

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EGFR-IN-73 Chemical Structure

EGFR-IN-73 Chemical Structure

CAS No. : 2857033-34-0

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EGFR-IN-73 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-73 (Compound 3f) is a potent inhibitor for the most common EGFR mutation EGFR Del19 with an IC50 of 119 nM[1].

IC50 & Target[1]

EGFRdel19

119 nM (IC50)

EGFRL858R

820 nM (IC50)

EGFRWT

>10 μM (IC50)

EGFRL858R/T790M

>10 μM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
BaF3 IC50
147.9 nM
Compound: 3f
Antiproliferative activity against mouse BaF3 cells expressing De119/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
Antiproliferative activity against mouse BaF3 cells expressing De119/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
[PMID: 36384036]
BaF3 IC50
197.5 nM
Compound: 3f
Antiproliferative activity against mouse BaF3 cells expressing Del19 assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
Antiproliferative activity against mouse BaF3 cells expressing Del19 assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
[PMID: 36384036]
BaF3 IC50
385.6 nM
Compound: 3f
Antiproliferative activity against mouse BaF3 cells expressing L858R assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
Antiproliferative activity against mouse BaF3 cells expressing L858R assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
[PMID: 36384036]
BaF3 IC50
749.6 nM
Compound: 3f
Antiproliferative activity against mouse BaF3 cells expressing L858R/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
Antiproliferative activity against mouse BaF3 cells expressing L858R/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
[PMID: 36384036]
体外研究
(In Vitro)

EGFR-IN-73 (Compound 3f) (0.01 nM-10 μM; 72 h) is weakly active on the EGFR WT and a potent binder of the EGFR mutants EGFR d746-750 (Del19), EGFR d747-752/P753S, EGFR L858R, or EGFR d752-759 in addition to weaker interaction detected for other oncogenic mutants (FLT3 D835Y and FLT3 ITD D835V)[1].
EGFR-IN-73 shows excellent chemical stability under acid conditions with more than 95% after 3 h and also good stability at pH 7.4 above 80%[1].

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

EGFR-IN-73 相关抗体:

Cell Proliferation Assay[1]

Cell Line: Ba/F3 cell, EGFR WT, L858R, L858R/C797S, L858R/T790M, L858R/T790M/C797S, Del19, Del19/C797S, Del19/T790M, Del19/T790M/C797S, and Ex20 insertion mutants
Concentration: 0.01 nM-10 μM
Incubation Time: 72 h
Result: Did not inhibit EGFR WT growth, whereas inhibited both L858R and L858R/C979S mutants in the sub-micromolar range, with IC50 values of 385.6 and 749.6 nM, respectively. Was even more potent in cells transduced with the Del19 and Del19/C797S mutations than on the other mutants in this series, with IC50 values of 197.5 and 147.9 nM, respectively.

Western Blot Analysis[1]

Cell Line: Ba/F3 cells expressing various EGFR mutants
Concentration: 10, 100 and 1000 nM
Incubation Time: 8 h
Result: Showed significant activity at L858R and excellent activity at the Del19 and Del19/C797S mutant EGFR. Did not affect T790M and WT EGFR.
分子量

405.81

Formula

C19H17ClFN3O4
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-73 相关分类

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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-IN-732857033-34-0EGFREpidermal growth factor receptorErbB-1HER1Del19L858RBa/F3Inhibitorinhibitorinhibit

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