2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Apoptosis MAPK/ERK Pathway Stem Cell/Wnt PI3K/Akt/mTOR
  3. EGFR Apoptosis p38 MAPK ERK Akt STAT
  4. EGFR-IN-173

EGFR-IN-173 是一种具有口服活性的泛突变 EGFR 酪氨酸激酶抑制剂，靶向 EGFR 19del、L858R/T790M 和 C797S 三重突变，可有效抑制 EGFR19del/T790M/C797S 突变体，IC50 为 1.19 nM，其对突变型 EGFR 的选择性较野生型高出 100 倍以上 (野生型 IC50 = 19.362 μM)。EGFR-IN-173 显著抑制细胞迁移，诱导非小细胞肺癌 (NSCLC) 细胞凋亡 (apoptosis)，抑制 EGFR 磷酸化并抑制下游通路 (MAPK/ERK、AKT、STAT3)。EGFR-IN-173 在 NSCLC 和 Ba/F3 异种移植模型中表现出抗肿瘤作用。EGFR-IN-173 可用于 NSCLC 研究。

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EGFR-IN-173

EGFR-IN-173 Chemical Structure

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EGFR-IN-173 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-173 is an orally active, pan-mutant EGFR tyrosine kinase inhibitor that targets EGFR 19del, L858R/T790M and C797S triple-mutations, potently inhibiting EGFR19del/T790M/C797S with an IC50 of 1.19 nM while showing over 100-fold selectivity for mutant over wild-type EGFR (IC50 = 19.362 μM against WT). EGFR-IN-173 significantly inhibits cell migration, induces apoptosis in non-small cell lung cancer (NSCLC) cells. EGFR-IN-173 inhibits EGFR phosphorylation and suppresses the downstream pathways (MAPK/ERK, AKT, STAT3). EGFR-IN-173 exhibits antitumor efficacy in NSCLC and Ba/F3 xenograft models. EGFR-IN-173 can be used for NSCLC research[1].

体外研究
(In Vitro)

EGFR-IN-173 (compound D10) (0.001-20 μM，72 小时) 对多种 EGFR 突变体表现出广泛而强大的抗增殖活性，在 HCC827 细胞 (EGFR19del) 中的 IC50 值为 0.69 nM，在 H1975 细胞 (EGFRL858R/T790M) 中为 0.242 μM，在 Ba/F3-EGFR19del/T790M/C797S 细胞中为 0.192 μM，在 Ba/F3-EGFRL858R/T790M/C797S 中为 1.303 μM，并对突变 EGFR 表现出超过 100 倍的选择性 (野生型 IC50 = 19.362 μM)[1]。
EGFR-IN-173 占据 EGFR 的活性位点，并与 Lys728 和 Ser797 形成重要的氢键[1]。
EGFR-IN-173 (10-100 nM，14天) 剂量依赖性地抑制非小细胞肺癌 HCC827 细胞的集落形成，从而抑制其长期增殖能力[1]。
EGFR-IN-173 (10-100 nM，0-48小时) 以浓度依赖性方式有效抑制非小细胞肺癌 H1975 细胞的迁移[1]。
EGFR-IN-173 (20-200 nM，48小时) 在 HCC827 细胞中诱导 G0/G1 期阻滞，且呈剂量依赖性[1]。
EGFR-IN-173 (1-2000 nM，48 小时) 通过触发标志性形态学事件 (包括染色质凝聚、核碎裂和凋亡小体的形成)，以浓度依赖性方式诱导早期和晚期细胞凋亡[1]。
EGFR-IN-173 (0.01-1 μM，48 小时) 能剂量依赖性地抑制 EGFR 磷酸化并抑制下游通路 (MAPK/ERK、AKT、STAT3)，最终触发细胞凋亡和 ERK1/2 等信号蛋白的降解[1]。

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

EGFR-IN-173 相关抗体:

Western Blot Analysis[1]

Cell Line: HCC827 cells and H1975-OR cells
Concentration: 0.01, 0.1 and 1 μM
Incubation Time: 48 h
Result: Exhibited superior dose-responsive inhibition of EGFR autophosphorylation at Tyr1068, a key molecular switch for downstream pathway activation.
Suppressed ERK1/2 phosphorylation (T202/Y204, T185/Y187) at 0.1 μM with 35.6 % inhibition, demonstrating potent blockade of the MAPK signaling axis.
Almost completely abrogated EGFR activation at 1 μM, whereas BLU-945 (HY-144680) showed weak inhibition at an equivalent concentration in HCC827 cells.
Significantly reduced ERK1/2 protein level at 100 nM.
Reduced p-Stat3 (Tyr705), p-Akt (Ser473), and p-Mek1/2 (Ser217/221) levels.
Increased cleaved caspase-3 at 100 nM, suggesting that the concurrent downregulation of ERK1/2 resulted from apoptosis-induced protein degradation.
Suppressed EGFR phosphorylation in H1975-OR cells at 100 nM.

Cell Migration Assay [1]

Cell Line: H1975 cells
Concentration: 10 and 100 nM
Incubation Time: 0, 24 and 48 h
Result: Significantly decreased wound closure compared to the negative control, indicating a dose-dependent inhibition of cell migration.
Resulted in a significantly larger wound area than the control over time.

Cell Cycle Analysis[1]

Cell Line: HCC827 cells
Concentration: 20 and 200 nM
Incubation Time: 48 h
Result: Dose-dependently accumulated cells in the G0/G1 phase, increasing the population from 74.40% at 20 nM to 94.58% at 200 nM.
Induced G0/G1 phase cell cycle arrest (94.58 %) comparable to Osimertinib (HY-15772) (94.92 %) at 200 nM.

Apoptosis Analysis[1]

Cell Line: HCC827 and H1975 cells
Concentration: 20, 200, and 2000 nM (H1975 cells, DAPI Staining); 20, 200, and 2000 nM (HCC827 cells, AO/EB Staining); 1, 10, and 100 nM (HCC827 cells, Hoechst 33342/PI Staining); 10, 100, and 1000 nM (HCC827 cells, Flow Cytometry)
Incubation Time: 48 h
Result: Induced dose-dependent nuclear condensation and fragmentation, with more pronounced effects than Osimertinib at equivalent concentrations.
Triggered nuclear condensation in HCC827 cells at 20 nM.
Induced a progressive rise in late-stage apoptosis in a concentration-dependent manner.
Exhibited concentration-dependent chromatin condensation and subsequent nuclear fragmentation, both hallmarks of apoptosis.
Induced the formation of apoptotic bodies.
Resulted in 6.36 %, 19.9 % and 31.6 % early apoptosis at 10, 100 and 1000 nM.

Cell Proliferation Assay[1]

Cell Line: HCC827 cells
Concentration: 10, 50 and 100 nM
Incubation Time: 14 days
Result: Dose-dependently suppressed colony formation, exhibiting 32.8 % inhibition at 10 nM compared to the control.
Showed 58.3 % inhibition at 50 nM and nearly complete suppression at 100 nM.
体内研究
(In Vivo)

EGFR-IN-173 (25 和 50 mg/kg，口服给药，每日一次，持续 12 天) 在 HCC827 异种移植瘤小鼠模型中表现出显著的抑制肿瘤生长作用[1]。
EGFR-IN-173 ( 50 mg/kg，口服给药，每日一次，持续 17 天) 在 Ba/F3-EGFR19del/T790M/C797S 异种移植瘤小鼠模型中对 EGFR19del/T790M/C797S 三重突变表现出一定的抑制作用[1]。

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

Animal Model: Female BALB/c nude mice, (6-8 weeks) subcutaneously injected with Ba/F3-EGFR19del/ T790M/C797S cells[1]
Dosage: 50 mg/kg
Administration: P.O., daily for 17 days
Result: Significantly reduced tumor volume and weight compared to the vehicle control group.
Reduced tumor cell density and increased intertumoral fibrosis.
Exhibited no significant body weight loss during the dosing period.
Animal Model: Male BALB/c nude mice (6-8 weeks) subcutaneously injected with HCC827 cells[1]
Dosage: 25 and 50 mg/kg
Administration: P.O., daily for 12 days
Result: Significantly suppressed tumor growth and reduced excised tumor weight at both low and high doses, demonstrating its potent efficacy and favorable dose tolerance.
Exhibited no significant body weight loss or clinically observable adverse effects at the dose of 50 mg/kg, supporting a favorable safety profile with minimal systemic toxicity.
分子量

583.06

Formula

C28H36ClN8O2P
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-173 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

EGFR-IN-173EGFRApoptosisp38 MAPKERKAktSTATEpidermal growth factor receptorErbB-1HER1Extracellular signal regulated kinasesPKBProtein kinase BEGFR19del/T790M/C797S mutantcell migrationapoptosisNSCLCMAPK/ERKAKTSTAT3Ba/F3 xenograft modelsNSCLC xenograft modelsInhibitorinhibitorinhibit

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