1. JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
  2. EGFR
  3. JBJ-02-112-05

JBJ-02-112-05 

目录号: HY-135914
产品使用指南

JBJ-02-112-05 是一种有效的,突变选择性,变构和口服活性 EGFR 抑制剂,对 EGFRL858R/T790MIC50 为 15 nM。

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JBJ-02-112-05 Chemical Structure

JBJ-02-112-05 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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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

JBJ-02-112-05 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 15 nM for EGFRL858R/T790M[1].

IC50 & Target[1]

EGFRL858R/T790M

15 nM (IC50)

体外研究
(In Vitro)

In Ba/F3 cells, JBJ-02-112-05 inhibits the activities of wildtype EGFR, EGFRL858R, EGFRL858R/T790M and EGFRL858R/T790M/C797S with IC50 values of 9.29 µM; 8.35 µM; 8.53 µM and 2.13 µM, respectively[1].
JBJ-02-112-05 demonstrates mutant selectivity by inhibiting mutant EGFR and downstream AKT and ERK1/2 phosphorylation in Ba/F3 cells stably transfected with EGFRL858R, EGFRL858R/T790M, EGFRL858R/T790M/C797S mutations[1].

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

体内研究
(In Vivo)

JBJ-02-112-05 (100 mg/kg; oral gavage; once daily; for 3 days; EGFRL858R/T790M/C797S genetically engineered mice) treatment inhibits phosphorylation of EGFR and downstream signaling pathways[1].
JBJ-02-112-05 exhibits a moderate half-life of 3 hours and a Cmax of 13.7 µM following 3 mg/kg intravenous (i.v.) dose. A 5 mg/kg oral dose of JBJ-02-112-05 achieves a half-life of 16.4 hours and a CCmax of 1.31 µM[1].

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

Animal Model: EGFRL858R/T790M/C797S genetically engineered mice[1]
Dosage: 100 mg/kg
Administration: Oral gavage; once daily; for 3 days
Result: Inhibited phosphorylation of EGFR and downstream signaling pathways.
分子量

464.54

Formula

C₂₇H₂₀N₄O₂S

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.

参考文献
  • 摩尔计算器

  • 稀释计算器

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质量   浓度   体积   分子量 *
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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

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JBJ-02-112-05
目录号:
HY-135914
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