CEP-28122 mesylate salt

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目录号 : KM14516 纯度 : 98%

Data Sheet 产品使用指南

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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5mg		In-stock
10mg		In-stock
50mg		In-stock
100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

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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.

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

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 .

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.

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	6 months
	-20°C	1 month

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。-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。

纯度： 98%

Data Sheet

产品使用指南

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