2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Apoptosis PI3K/Akt/mTOR Cell Cycle/DNA Damage
  3. EGFR Apoptosis Akt PERK
  4. EGFR-IN-175

EGFR-IN-175 是一种口服有效且有选择性的的 EGFRL858R/T790M/C797S 抑制剂，其 IC50 值为 18.94 nM。EGFR-IN-175 能够诱导细胞凋亡 (apoptosis) 并导致 G1 期阻滞。EGFR-IN-175 可下调 p-EGFR、p-AKT 和 p-ERK 的表达。EGFR-IN-175 可用于癌症研究，如肺癌研究。

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EGFR-IN-175

EGFR-IN-175 Chemical Structure

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EGFR-IN-175 相关抗体

Top Publications Citing Use of Products

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

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Akt Akt1 Akt2 Akt3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EGFR-IN-175 is an orally active and selective EGFRL858R/T790M/C797S inhibitor with an IC50 of 18.94 nM. EGFR-IN-175 can induce cell apoptosis and cause G1 phase arrest. EGFR-IN-175 can downregulate p-EGFR, p-AKT, and p-ERK expression. EGFR-IN-175 can be used for the research of cancer, such as lung cancer[1].

IC50 & Target[1]

EGFRWT

125.9 nM (IC50)

EGFRLR/TM

76.88 nM (IC50)

EGFRLR/TM/CS

18.94 nM (IC50)

体外研究
(In Vitro)

EGFR-IN-175 (Compound M49) 可抑制 BaF3-EGFRL858R/T790M/C797S、A431 和 H1975 细胞的增殖，其 IC50 值分别为 0.77、5.11 和 5.94 μM[1]。 EGFR-IN-175 (0.1-2.5 μM) 以剂量依赖性方式下调 BaF3-TM 细胞中 p-EGFR、p-AKT 和 p-ERK 的磷酸化水平[1]。 EGFR-IN-175 (0.1-2.5 μM, 48 h) 可诱导 BaF3-TM 细胞凋亡和 G1 期阻滞[1]。

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

EGFR-IN-175 相关抗体:

Apoptosis Analysis[1]

Cell Line: BaF3-TM cells
Concentration: 0.1, 1 and 2.5 μM
Incubation Time: 48 h
Result: Increased apoptosis rate, reaching 69.68% at 2.5 μM.
Upregulated protein expression of Cleaved-PARP and Cleaved-Caspase-3.
体内研究
(In Vivo)

EGFR-IN-175 (Compound M49) (腹腔注射 30 mg/kg，口服 30-60 mg/kg，每日一次，持续 14 天) 可抑制 BaF3-EGFRL858R/T790M/C797S 异种移植 BALB/c 裸鼠的肿瘤生长[1]。

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

Animal Model: BaF3-EGFRL858R/T790M/C797S xenograft BALB/c nude mice models[1]
Dosage: 30 mg/kg for i.p., 30 and 60 mg/kg for p.o
Administration: Once a day for 14 days
Result: Reduced tumor volume.
Reduced Ki67 and increased TUNEL-positive cells in tumors.
Downregulated p-EGFR.
Had no significant body weight loss and no toxicity to major organs.
分子量

702.85

Formula

C33H38N10O4S2
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-175 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-175EGFRApoptosisAktPERKEpidermal growth factor receptorErbB-1HER1PKBProtein kinase BProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinasep-EGFRp-AKTand p-ERKBaF3-TMLung cancerInhibitorinhibitorinhibit

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