1. Protein Tyrosine Kinase/RTK
  2. Anaplastic lymphoma kinase (ALK)
  3. JH-VIII-157-02

JH-VIII-157-02 是 alectinib 的结构类似物,为 ALK 抑制剂,对棘皮动物微管相关蛋白样 4 (EML4)-ALK G1202R 的 IC50 值为 2 nM。

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JH-VIII-157-02 Chemical Structure

JH-VIII-157-02 Chemical Structure

CAS No. : 1639422-97-1

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥5223
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1 mg ¥1942
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5 mg ¥5100
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10 mg ¥8150
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Top Publications Citing Use of Products
  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

JH-VIII-157-02 is a structural analogue of alectinib, acts as an ALK inhibitor, and shows an IC50 of 2 nM for echinoderm microtubule-associated protein-like 4-ALK (EML4-ALK) G1202R in cells.

IC50 & Target

IC50: 2 nM (EML4-ALK G1202R, cell assay), 2 nM (EML4-ALKwt, cell assay), 2 nM (EML4-ALK C1156Y, cell assay), 2 nM (EML4-ALK F1174L, cell assay), 2 nM (EML4-ALK F1174L, cell assay)[1]

体外研究
(In Vitro)

JH-VIII-157-02 is a structural analogue of alectinib, acts as an ALK inhibitor, and shows an IC50 of 2 nM for echinoderm microtubule-associated protein-like 4-ALK (EML4-ALK) G1202R in cells. JH-VIII-157-02 also potently inhibits EML4-ALKwt (Eawt), EAC1156Y, EAF1174L, EAS1206Y (IC50, 2 nM), EAG1269A (IC50, 3 nM), EAL1196M (IC50, 58 nM), EA1151Tins (IC50, 107 nM), and EAL1152R (IC50, 196 nM). Moreover, JH-VIII-157-02 has selectivity at other kinases, including IRAK1, CLK4, RET, RET V804L, RET V804M and IRAK 4, and the IC50s are 14 nM, 14 nM, 3 nM, 13 nM, 12 nM, and 465 nM respectively. JH-VIII-157-02 exhibits inhibitory growth of cancer cell lines, such as H3122, DFCI76 (L1152R] with EC50s of 5, 19 nM, respectively[1].

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

体内研究
(In Vivo)

JH-VIII-157-02 exhibits good oral bioavailability following an oral dose of 10 mg/kg in mice. JH-VIII-157-02 also penetrates the CNS of mice[1].

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

分子量

465.55

Formula

C28H27N5O2

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
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
In Vitro: 

DMSO 中的溶解度 : ≥ 25 mg/mL (53.70 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1480 mL 10.7400 mL 21.4800 mL
5 mM 0.4296 mL 2.1480 mL 4.2960 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 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
参考文献
Cell Assay
[1]

Cells are seeded at 4000 per well in 96 well plates and exposed to JH-VIII-157-02 in triplicate at 1 nM to 10 μM for 72 hours. Cell viability is evaluated using CellTiter-Glo Luminescent Cell Viability Assay. IC50 values are calculated by nonlinear regression (variable slope) using GraphPad Prism 5 software. Each experiment is repeated for at least twice[1].

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

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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1480 mL 10.7400 mL 21.4800 mL 53.6999 mL
5 mM 0.4296 mL 2.1480 mL 4.2960 mL 10.7400 mL
10 mM 0.2148 mL 1.0740 mL 2.1480 mL 5.3700 mL
15 mM 0.1432 mL 0.7160 mL 1.4320 mL 3.5800 mL
20 mM 0.1074 mL 0.5370 mL 1.0740 mL 2.6850 mL
25 mM 0.0859 mL 0.4296 mL 0.8592 mL 2.1480 mL
30 mM 0.0716 mL 0.3580 mL 0.7160 mL 1.7900 mL
40 mM 0.0537 mL 0.2685 mL 0.5370 mL 1.3425 mL
50 mM 0.0430 mL 0.2148 mL 0.4296 mL 1.0740 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:
JH-VIII-157-02
目录号:
HY-112140
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