CEP-28122 (Mesylate salt)
- CAS号:
- 英文名:CEP-28122 (Mesylate salt)
- 中文名:CEP-28122 (Mesylate salt)
- CBNumber:CB22666785
- 分子式:C??H??ClN?O?S
- 分子量:0
- MOL File:Mol file
- 形态 :Solid
- 颜色 :White to off-white
CEP-28122 (Mesylate salt)性质、用途与生产工艺
- 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。
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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.
- 更新日期：2024/11/08
- 产品编号：HY-18030A
- 产品名称：CEP-28122 (Mesylate salt) CEP-28122 mesylate salt
- CAS编号：
- 包装：5 mg
- 价格：1500元
- 更新日期：2024/11/08
- 产品编号：HY-18030A
- 产品名称：CEP-28122 (Mesylate salt) CEP-28122 mesylate salt
- CAS编号：
- 包装：10 mM * 1 mLin DMSO
- 价格：2096元
- 公司名称：MedChemexpress LLC
- 联系电话：021-58955995
- 电子邮件：sales@medchemexpress.cn
- 国家：美国
- 产品数：4861
- 优势度：58
- 公司名称：TargetMol Chemicals Inc.
- 联系电话：
- 电子邮件：support@targetmol.com
- 国家：美国
- 产品数：38631
- 优势度：58
- 公司名称：MedChemExpress
- 联系电话：--
- 电子邮件：sales@medchemexpress.com
- 国家：美国
- 产品数：6398
- 优势度：58
