2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Immunology/Inflammation
  3. EGFR PD-1/PD-L1
  4. EP26

EP26 是一种有效的和具有口服活性的 EGFR 和 PD-L1 抑制剂，IC50 值分别为 48.6 nM 和 1.77 µM。EP26 降低了 p-EGFR 的蛋白表达。EP26 诱导细胞周期停滞在 G0/G1 期。EP26 具有研究胶质母细胞瘤的潜力。

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EP26 Chemical Structure

EP26 Chemical Structure

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

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Customer Review

EP26 相关抗体

Top Publications Citing Use of Products

查看 EGFR 亚型特异性产品:

查看所有亚型
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

EP26 is a potent and orally active EGFR and PD-L1 inhibitor with IC50 values of 48.6 nM, 1.77 µM, respectively. EP26 decreased the protein expression of p-EGFR. EP26 induces cell cycle arrest at G0/G1 phase. EP26 has the potential for the research of glioblastoma[1].

IC50 & Target[1]

EGFR

48.6 nM (IC50)

PD-L1

1.77 μM (IC50)

体外研究
(In Vitro)

EP26 (0-4 µM; 48 h) 以剂量依赖性方式降低 p-EGFR 的蛋白表达[1]。
EP26 (0.5, 1, 2µM; 48 h) 诱导细胞周期停滞在 G0/G1 期[1]。
EP26 以剂量依赖性方式与人 PD-L1 和鼠 PD-L1 结合，KD 值分别为 0.58、0.52 µM[1]。

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

EP26 相关抗体:

Cell Proliferation Assay[1]

Cell Line: U87MG, U251, U87MG-vIII, GL261 cells
Concentration: 0-20 µM
Incubation Time: 72 h
Result: Showed antiproliferative activity with IC50s of 0.77, 1.02, 1.19, 0.28 µM for U87MG, U251, U87MG-vIII, GL261 cells, respectively.

Western Blot Analysis[1]

Cell Line: U87MG, U87vIII cells
Concentration: 0, 0.25, 1, 2 µM for U87MG cells, 0, 0.5, 1, 2, 4 µM
Incubation Time: 48 h
Result: Decreased the protein expression of p-EGFR in a dose-dependent manner.

Cell Cytotoxicity Assay[1]

Cell Line: U87MG cells
Concentration: 0.5, 1, 2 µM
Incubation Time: 48 h
Result: Induced cell cycle arrest at G0/G1 phase with the percentage of U87MG cells in G0/G1 phase increased from 60.51 to 63.57, 69.48, and 73.98%, respectively.
体内研究
(In Vivo)

EP26 (50, 100 mg/kg; p.o.; once a day for 21 days) 在小鼠中显示出抗肿瘤活性[1]。 药代动力学分析[1].

PK parameters i.v. administration (4 mg/kg, n = 5) p.o. administration (20 mg/kg, n = 5)
AUC(0-t) (µg/L*h) 2832.5 ± 954.8 3145.7 ± 778.7
AUC(0-∞) (µg/L*h) 2906.6 ± 1061.8 3238.3 ± 752.2
MRT(0-t) (h) 12.7 ± 0.8 17.5 ± 1.6
MRT(0-∞) (h) 2906.6 ± 1061.8 3238.3 ± 752.2
t1/2 (h) 6.8 ± 3.7 13.0 ± 5.3
Tmax (h) 0.04 ± 0.02 3.6 ± 0.9
Vz (L/kg) 13.7 ± 4.4 123.5 ± 64.6
CL (L/h/kg) 1.5 ± 0.6 6.4 ± 1.3
Cmax (µg/L) 325.6 ± 166.8 255.3 ± 123.0
F(%) - 22.2

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

Animal Model: C57BL/6 mice (GL261 cells)[1]
Dosage: 50, 100 mg/kg
Administration: P.o.; once a day for 21 days
Result: Decreased the tumor weight and tumor volume by 92.0 and 89.7% at 100 mg/kg, significantly inhibited glioblastoma tumor growth with tumor growth inhibitions (TGIs) of 61.4%, 89.4% at 50, 100 mg/kg, respectively.
分子量

737.26

Formula

C42H42ClFN4O5
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

EP26 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

EP26EP 26EP-26EGFRPD-1/PD-L1Epidermal growth factor receptorErbB-1HER1PD-1/Programmed death-ligand 1orally activep-EGFRG0/G1 phaseU87MGU87vIII cellsglioblastomaanticancerInhibitorinhibitorinhibit

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