2. Protein Tyrosine Kinase/RTK
  3. Anaplastic lymphoma kinase (ALK)
  4. CEP-28122 mesylate salt

CEP-28122 mesylate salt 

目录号: HY-18030A 纯度: 99.08%
COA 产品使用指南

摩尔计算器

CEP-28122 mesylate salt 是一种二氨基嘧啶衍生物，是一种高度有效的选择性且具有口服活性的 ALK 抑制剂，对重组 ALK 激酶活性的 IC50 为 1.9 nM。CEP-28122 在人类癌症的 ALK 阳性实验模型中具有抗肿瘤活性。 CEP-28122 具有良好的药效药代活性。

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CEP-28122 mesylate salt Chemical Structure

CEP-28122 mesylate salt Chemical Structure

CAS No. : 2070009-30-0

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥2096
In-stock
5 mg ￥1500
In-stock
10 mg ￥2400
In-stock
50 mg ￥5500
In-stock
100 mg 现货 询价
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500 mg   询价  

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Customer Review

Other Forms of CEP-28122 mesylate salt:

CEP-28122 mesylate salt 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CEP-28122 mesylate salt, a diaminopyrimidine derivative, is a potent, selective, and orally bioavailable ALK inhibitor, with an IC50 value of 1.9 nM for recombinant ALK kinase activity. CEP-28122 has antitumor activity in experimental models of ALK-positive human cancers. CEP-28122 mesylate salt has good pharmacodynamic and pharmacokinetic activity[1].

体外研究
(In Vitro)

CEP-28122 mesylate salt (3-3000 nM; 48 hours) treatment leads to concentration-dependent growth inhibition of Karpas-299 and Sup-M2 cells in culture, associates with concentration-related caspase 3/7 activation[1].
CEP-28122 mesylate salt (30-1000 nM; 2 hours) treatment leads to substantial suppression of phosphorylation of putative downstream effectors of ALK in Sup-M2 cells, indicating that the downstream signaling pathways are mediated by individual ALK fusion protein[1].

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

CEP-28122 mesylate salt 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: Karpas-299, Sup-M2, Toledo and HuT-102 cells
Concentration: 10 nM, 100 nM, 1000 nM, 10000 nM
Incubation Time: 48 hours
Result: Treatment led to concentration-dependent growth inhibition of Karpas-299 and Sup-M2 cells in culture.

Western Blot Analysis [1]

Cell Line: Sup-M2 cells
Concentration: 30 nM, 100 nM, 300 nM, 1000 nM
Incubation Time: 2 hours
Result: Resulted in substantial suppression of phosphorylation of putative downstream effectors of ALK, including Stat-3, Akt, and ERK1/2 in Sup-M2 cells.
体内研究
(In Vivo)

CEP-28122 mesylate salt (3-30 mg/kg; oral gavage; twice a day; 12 days) produces dose-dependent antitumor activity in Sup-M2 subcutaneous tumor xenografts in SCID mice.In contrast, CEP-28122 has no antitumor activity in nu/nu mice bearing HCT116, suggesting that the antitumor activity of CEP-28122 in NPM-ALK–positive Sup-M2 tumor models is due to sustained NPM-ALK inhibition in tumors [1].

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

Animal Model: Female SCID mice bearing Sup-M2 subcutaneous tumor xenografts and nu/nu mice bearing HCT116 aged 6-8 week old[1]
Dosage: 3 mg/kg, 10 mg/kg and 30 mg/kg
Administration: oral gavage; twice a day; 12 days
Result: CEP-28122 produced dose-dependent antitumor activity in Sup-M2 subcutaneous tumor xenografts in SCID mice. In contrast, CEP-28122 had no antitumor activity in nu/nu mice bearing HCT116.
分子量

635.17

Formula

C29H39ClN6O6S
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

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 6.4 mg/mL (10.08 mM; 超声加热助溶; 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 1.5744 mL 7.8719 mL 15.7438 mL
5 mM 0.3149 mL 1.5744 mL 3.1488 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 (sealed storage, away from moisture)。-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

只
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

CEP-28122 mesylate salt 相关分类

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 (sealed storage, away from moisture)。-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 1.5744 mL 7.8719 mL 15.7438 mL 39.3595 mL
5 mM 0.3149 mL 1.5744 mL 3.1488 mL 7.8719 mL
10 mM 0.1574 mL 0.7872 mL 1.5744 mL 3.9360 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.

Keywords:

CEP-281222070009-30-0CEP28122CEP 28122Anaplastic lymphoma kinase (ALK)Anaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246Inhibitorinhibitorinhibit

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