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2070009-30-0

中文名称 CEP-28122 (Mesylate salt)
英文名称 CEP-28122 (Mesylate salt)
CAS
分子式 C28H35ClN6O3.CH4O3S
分子量 635.18
MOL 文件 2070009-30-0.mol
更新日期 2026/09/28 09:03:06
2070009-30-0 结构式 2070009-30-0 结构式

基本信息

中文别名
ALK抑制剂(CEP-28122 MESYLATE SALT)
英文别名
CEP-28122 (Mesylate salt)

物理化学性质

形态Solid
颜色White to off-white
CEP-28122 (Mesylate salt)价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2026/09/15HY-18030ACEP-28122 (Mesylate salt)
CEP-28122 mesylate salt
2070009-30-05 mg1500元
2026/09/15HY-18030ACEP-28122 (Mesylate salt)
CEP-28122 mesylate salt
2070009-30-010mg2400元
2026/09/15HY-18030ACEP-28122 (Mesylate salt)
CEP-28122 mesylate salt
2070009-30-025 mg3928元

常见问题列表

生物活性
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。
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.
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