2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. EGFR/C797S-IN-1

EGFR/C797S-IN-1 是一种有效的 EGFR-C797S 抑制剂，IC50 值为 0.128 µM。EGFR/C797S-IN-1 显示出抗增殖活性和抗肿瘤活性。EGFR/C797S-IN-1 以剂量依赖的方式抑制 P-EGFR 蛋白的表达。

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EGFR/C797S-IN-1 Chemical Structure

EGFR/C797S-IN-1 Chemical Structure

CAS No. : 2378188-21-5

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EGFR/C797S-IN-1 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

  • 纯度 & 产品资料

  • 参考文献

生物活性

EGFR/C797S-IN-1 is a potent EGFR-C797S inhibitor with an IC50 value of 0.128 µM. EGFR/C797S-IN-1 shows anti-proliferative activity and anti-tumor activity. EGFR/C797S-IN-1 inhibits the expression of p-EGFR in a dose-dependent manner[1].

IC50 & Target[1]

EGFRL858R/T790M/C797S

0.128 μM (IC50)

体外研究
(In Vitro)

EGFR/C797S-IN-1 (compound 14d) (0-10 µM; 72 h) 显示抗增殖活性，对BaF3-EGFRL858R/T790M/C797S, BaF3-EGFR19del/T790M/C797S 的 IC50 值分别为 0.75、0.09 µM [1]。
EGFR/C797S-IN-1 (1-10000 nM; 24 h) 以剂量依赖性降低 p-EGFR、p-AKT、p-ERK 蛋白的表达[1]。

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

EGFR/C797S-IN-1 相关抗体:

Cell Proliferation Assay[1]

Cell Line: BaF3 cells with EGFRL858R/T790M/C797S and EGFR19del/T790M/C797S Mutations
Concentration: 0-10 µM
Incubation Time: 72 h
Result: Showed anti-proliferative activitie with IC50s of 0.75, 0.09 µM for BaF3-EGFRL858R/T790M/C797S, BaF3-EGFR19del/T790M/C797S, respectively.

Western Blot Analysis[1]

Cell Line: BaF3-EGFRL858R/T790M/C797S, BaF3-EGFR19del/T790M/C797S cells
Concentration: 1, 10, 100, 1000, 10000 nM
Incubation Time: 24 h
Result: Decreased the expression of p-EGFR, p-AKT. p-ERK protein in a dose dependent manner.
体内研究
(In Vivo)

EGFR/C797S-IN-1 (10、30 mg/kg；每日一次，持续 14 天) 呈剂量依赖性显著降低小鼠体内的肿瘤生长[1]。

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

Animal Model: SD male rats[1]
Dosage: 1 mg/kg for i.v.; 10 mg/kg for p.o.
Administration: i.v. or p.o.
Result: Displayed good biochemical activity and promising cellular activity.
Animal Model: BALB/c nude mice (BaF3-EGFR19del/T790M/C797S xenograft model)[1]
Dosage: 10, 30 mg/kg
Administration: I.p.; daily for 14 days
Result: Displayed an obvious suppressive effect of tumor growth, with the TGI at 51.36% and 67.95% at the dosage of 10 mg/kg and 30 mg/kg, respectively.
分子量

470.56

Formula

C28H30N4O3
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/C797S-IN-1 相关分类

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  • 稀释计算器

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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/C797S-IN-12378188-21-5EGFREpidermal growth factor receptorErbB-1HER1anti-proliferative activityanti-tumorBaF3 cellsp-EGFRp-AKTp-ERKInhibitorinhibitorinhibit

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