1. Metabolic Enzyme/Protease Apoptosis
  2. MMP Apoptosis
  3. INCB3619

INCB3619 是一种选择性的,具有口服活性的 ADAM 抑制剂,作用于 ADAM10ADAM17IC50 值分别是 22 nM和 14 nM。INCB3619 具有抗肿瘤活性。

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INCB3619 Chemical Structure

INCB3619 Chemical Structure

CAS No. : 791826-72-7

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

INCB3619 is a selective and orally active ADAM inhibitor with IC50 of 22 nM and 14 nM for ADAM10 and ADAM17, respectively. INCB3619 has anti-tumor activity[1].

体外研究
(In Vitro)

INCB3619 (0-0.25 μM, 96 h) 可以抑制 heregulin 依赖性 HER3-Akt 通路,但不能抑制 A549 细胞中的 ERK 活性,可诱导 A549 细胞凋亡[1]
INCB3619 (0-10 μM, 72 h) 可以抑制 EGFR 自分泌细胞系 NCI-H1666 中的 EGFR 配体信号传导,并可与其他抗 EGFR 药物,如吉非替尼联合使用[1]
INCB3619 (2 µM) 抑制 NCI-H166 细胞中 ERK1/2 的表达,使其对吉非替尼 (Gefitinib,HY-50895) 敏感[1]

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

Apoptosis Analysis[1].

Cell Line: A549 cell
Concentration: 1, 10 μM
Incubation Time:
Result: Induced about 3% apoptosis at a concentration of 1 μM and about 5% at a concentration of 10 μM.

Cell Viability Assay[1].

Cell Line: NCI-H1666 cell
Concentration: 0-10 μM
Incubation Time: 72 h
Result: Inhibited proliferation of NCI-H1666 cells.
体内研究
(In Vivo)

INCB3619 (subcutaneous injection,60 mg/kg/d,14 d) 在 A549 异种移植的 BALB/c nu/nu 小鼠模型中,具有抗肿瘤活性,并使肿瘤对吉非替尼 (Gefitinib,HY-50895) 敏感[1]

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

Animal Model: BALB/c nu/nu mouse model of A549 xenograft
Dosage: 50, 60 mg/kg
Administration: subcutaneous injection, daily, 14 d
Result: Significant tumor growth inhibition and delay at 60 mg/kg dose, less active effect at 50 mg/kg.
分子量

413.47

Formula

C22H27N3O5

CAS 号
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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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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产品名称:
INCB3619
目录号:
HY-12636
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