CEP-28122 mesylate salt|西域试剂

CEP-28122 mesylate salt,99.08%

产品编号：Bellancom-18030A| 分子式：C₂₉H₃₉ClN₆O₆S| 分子量：635.17

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-18030A	￥1500.00	杭州北京（现货）
Bellancom-18030A	￥2400.00	杭州北京（现货）
Bellancom-18030A	￥5500.00	杭州北京（现货）
Bellancom-18030A	￥10000.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

CEP-28122 mesylate salt

产品介绍

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。

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.

体外研究

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.
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.

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

Cell Cytotoxicity Assay

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

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 .

西域 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
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.

体内研究

西域 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
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.

体内研究

西域 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
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.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 6.4 mg/mL (10.08 mM)

* "≥" 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	1.5744 mL	7.8719 mL	15.7438 mL
5 mM	0.3149 mL	1.5744 mL	3.1488 mL
10 mM	0.1574 mL	0.7872 mL	1.5744 mL

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。

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)

参考文献