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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Customer Review

  • 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].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
1 μM
Compound: INCB3619
Inhibition of ADAM17 in human A549 cells assessed as potentiation of gefitinib-mediated inhibition of cell viability by measuring gefitinib IC50 at 10 uM after 96 hrs by CellTiter-Glo assay (Rvb = 8 microM)
Inhibition of ADAM17 in human A549 cells assessed as potentiation of gefitinib-mediated inhibition of cell viability by measuring gefitinib IC50 at 10 uM after 96 hrs by CellTiter-Glo assay (Rvb = 8 microM)
[PMID: 26192023]
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
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (241.86 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4186 mL 12.0928 mL 24.1856 mL
5 mM 0.4837 mL 2.4186 mL 4.8371 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.46%

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4186 mL 12.0928 mL 24.1856 mL 60.4639 mL
5 mM 0.4837 mL 2.4186 mL 4.8371 mL 12.0928 mL
10 mM 0.2419 mL 1.2093 mL 2.4186 mL 6.0464 mL
15 mM 0.1612 mL 0.8062 mL 1.6124 mL 4.0309 mL
20 mM 0.1209 mL 0.6046 mL 1.2093 mL 3.0232 mL
25 mM 0.0967 mL 0.4837 mL 0.9674 mL 2.4186 mL
30 mM 0.0806 mL 0.4031 mL 0.8062 mL 2.0155 mL
40 mM 0.0605 mL 0.3023 mL 0.6046 mL 1.5116 mL
50 mM 0.0484 mL 0.2419 mL 0.4837 mL 1.2093 mL
60 mM 0.0403 mL 0.2015 mL 0.4031 mL 1.0077 mL
80 mM 0.0302 mL 0.1512 mL 0.3023 mL 0.7558 mL
100 mM 0.0242 mL 0.1209 mL 0.2419 mL 0.6046 mL
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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