1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Apoptosis
  2. EGFR Apoptosis Bcl-2 Family Survivin
  3. JS04

JS04 是一种 EGFRL858R/T790M 激酶抑制剂。JS04 可激活内源性和外源性凋亡 (apoptosis) 通路,诱导细胞周期 G2/M 期阻滞。JS04 可用于耐药性非小细胞肺癌的研究。

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JS04

JS04 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

JS04 is a EGFRL858R/T790M kinase inhibitor. JS04 activates both endogenous and exogenous apoptosis (apoptosis) pathways and induces G2/M phase arrest of the cell cycle. JS04 is applicable to the research of drug-resistant non-small cell lung cancer[1].

IC50 & Target[1]

EGFRL858R/T790M

 

Bcl-2

 

Bcl-xL

 

体外研究
(In Vitro)

JS04 (72 h) 可强效抑制 H1975 和 A549 非小细胞肺癌 (NSCLC) 细胞的增殖,其 IC50 值分别为 8.11 μM 和 11.58 μM;同时该化合物针对人 Hs27 成纤维细胞具有良好的安全窗,选择性指数为 2.52[1]
JS04 (10-20 μM; 48 h) 可在 H1975 细胞中诱导剂量依赖性凋亡[1]
JS04 (10-20 μM; 48 h) 可在 H1975 细胞中诱导 G2/M 期细胞周期阻滞[1]
JS04 (72 h) 可同时激活内源性凋亡通路 (下调 BCL-2、BCL-xL、Survivin 表达) 与外源性凋亡通路 (上调 TRAIL R2/DR5 表达)[1]

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

Apoptosis Analysis[1]

Cell Line: H1975 NSCLC
Concentration: 10 and 20 μM
Incubation Time: 48 h
Result: At 20 μM, induced 74% total apoptotic cell death.
At 10 μM, produced a lower level of apoptosis compared to 20 μM, as confirmed by reduced viable cell populations.

Cell Cycle Analysis[1]

Cell Line: H1975 NSCLC
Concentration: 10 and 20 μM
Incubation Time: 48 h
Result: At 20 μM, caused an approximately 3 to 4-fold increase in the G2/M cell population (35% of cells in G2/M phase), with a concomitant decrease in G0/G1 phase cells.
体内研究
(In Vivo)

JS04 (6.25-100 μM;浸泡处理;持续给药;从 5.5 至 6 小时胚龄到 96 小时胚龄) 在斑马鱼 (Danio rerio) 胚胎中显示出良好的急性安全性[1]

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

Animal Model: AB-WT (fertilised embryos)[1]
Dosage: 6.25 μM; 12.5 μM; 25 μM; 50 μM; 100 μM
Administration: immersion; continuous; 5.5-6 hpf through 96 hpf
Result: Caused 100% embryo mortality at 100 μM and 96 hpf.
Resulted in < 20% mortality across all time points at 6.25, 12.5, and 25 μM.
分子量

382.89

Formula

C20H23ClN6

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
  • 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.

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HY-182031
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