2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR
  3. EGFR Akt Anaplastic lymphoma kinase (ALK)
  4. EGFR-IN-176

EGFR-IN-176 是一种口服活性且 ATP 竞争性的 EGFR 突变体抑制剂 (特别是 C797S 介导的 EGFR 三重突变体)。EGFR-IN-176 对三重突变细胞的生长具有高度选择性抑制作用，包括 Ba/F3 EGFR19del/T790M/C797S (IC50 = 0.001 nM) 和 Ba/F3 EGFRL858R/T790M/C797S (IC50 = 0.04 nM)。EGFR-IN-176 能够有效抑制 Ba/F3 和 PC-9 细胞 (分别表达 EGFR19del/T790M/C797S 或 EGFRL858R/T790M/C797S 突变) 中 AKT 信号通路的活化，且该抑制作用呈现剂量依赖性。EGFR-IN-176 选择性抑制携带 EGFR 三重突变的细胞系中的 EGFR 信号传导，对表达野生型 EGFR 的 A431 细胞无抑制作用。EGFR-IN-176 可有效抑制 ALK 的酶活性 (IC50 < 0.5 nM)。EGFR-IN-176 在小鼠实验中有效抑制肿瘤生长，并显示出良好的抗非小细胞肺癌作用。

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EGFR-IN-176

EGFR-IN-176 Chemical Structure

CAS No. : 2754394-10-8

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EGFR-IN-176 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EGFR-IN-176 is an orally active and ATP-competitive EGFR mutant inhibitor (particularly C797S-mediated EGFR triple mutant). EGFR-IN-176 demonstrates highly selective inhibition of the growth of triple-mutant cells including Ba/F3 EGFR19del/T790M/C797S (IC50 = 0.001 nM) and Ba/F3 EGFRL858R/T790M/C797S (IC50 = 0.04 nM). EGFR-IN-176 effectively inhibits subsequent AKT signaling in Ba/F3 and PC-9 cells expressing EGFR19del/T790M/C797S or EGFRL858R/T790M/C797S. EGFR-IN-176 selectively inhibits EGFR signaling in cell lines harboring EGFR triple mutation and shows no inhibitory effect against A431 cells that express wild-type EGFR. EGFR-IN-176 can effectively inhibit the enzymatic activity of ALK (IC50 < 0.5 nM). EGFR-IN-176 effectively inhibits tumor growth in mouse experiments and shows good anti-nonsmall cell lung cancer (NSCLC) [1].

体外研究
(In Vitro)

EGFR-IN-176 (Compound 31r，0.0045 nM-10,000 nM，48 小时) 在体外对携带 EGFR 三重突变的细胞表现出极强的选择性生长抑制活性，包括 Ba/F3 EGFR19del/T790M/C797S (IC50 = 0.001 nM) 和 Ba/F3 EGFRL858R/T790M/C797S (IC50 = 0.04 nM) ，对野生型 EGFR 细胞 A431 (IC50 > 10,000 nM) 具有较低的细胞毒性[1]。 EGFR-IN-176 (500 nM，7 天) 可在短期内抑制 PC-9 EGFR19del/T790M/C797S 和 PC-9 EGFRL858R/T790M/C797S 的增殖，并在长期内使癌细胞失去自我更新和克隆生长能力[1]。 EGFR-IN-176 (250 nM，0-24 小时) 可有效抑制 PC-9 EGFR19del/T790M/C797S 和 PC-9 EGFRL858R/T790M/C797S 的迁移能力[1]。 EGFR-IN-176 (500 nM，48 小时) 可诱导 PC-9 EGFR19del/T790M/C797S 和 PC-9 EGFRL858R/T790M/C797S 细胞凋亡[1]。

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

EGFR-IN-176 相关抗体:

Cell Viability Assay[1]

Cell Line: Ba/F3 EGFR19del/T790M/C797S and Ba/F3 EGFRL858R/T790M/C797S
Concentration: 0.0045 nM ~ 10,000 nM
Incubation Time: 48 h
Result: Exhibited higher activity, with IC50 values of 0.001 nM (Ba/F3 EGFR19del/T790M/C797S) and 0.04 nM (Ba/F3 EGFRL858R/T790M/C797S)

Cell Migration Assay [1]

Cell Line: PC-9 EGFR19del/T790M/C797S and PC-9 EGFRL858R/T790M/C797S
Concentration: 250 nM
Incubation Time: 24 h
Result: Significantly slowed down the healing rate of scratches.

Apoptosis Analysis[1]

Cell Line: PC-9 EGFR19del/T790M/C797S and PC-9 EGFRL858R/T790M/C797S
Concentration: 500 nM
Incubation Time: 48 h
Result: significantly increased the proportion of early and late apoptotic cells
体内研究
(In Vivo)

EGFR-IN-176 (40-80 mg/kg，灌胃，每天一次，持续 21 天) 能以剂量依赖性方式显著抑制肿瘤生长，甚至可观察到 PC-9 荷瘤小鼠的肿瘤消退[1]。

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

Animal Model: Subcutaneously inoculate the right forelimb of 6-8-week-old BALB/c-nu mice with a 0.2 mL suspension of PC-9 EGFR19del/T790M/C797S cells at a concentration of 2.5×10^7 cells/mL until the tumor volume reaches 100-200 cubic millimeters.
Dosage: 40 mg/kg, 60 mg/kg, 80 mg/kg
Administration: Oral gavage, once daily for 21 days
Result: Showed a dose-dependent tumor growth inhibitory effect, the tumor growth inhibition rates (TGI) were 80.2% (40 mg/kg), 92.3% (60 mg/kg), and 105.7% (80 mg/kg), respectively.
Observed tumor regression in the high-dose group (80 mg/kg), the tumor volume decreased to below the initial volume.
Exhibited favorable in vivo tolerability, with no mortality or significant body weight loss observed.
Significantly inhibited EGFR phosphorylation and the activation of downstream signaling pathways.
分子量

699.87

Formula

C35H45N11O3S
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-176 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-IN-1762754394-10-8EGFRAktAnaplastic lymphoma kinase (ALK)Epidermal growth factor receptorErbB-1HER1PKBProtein kinase BAnaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246CancerAKTATPBa/F3ALKInhibitorinhibitorinhibit

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