CEP-28122 (Mesylate salt)
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- CAS号:
- 英文名:
- CEP-28122 (Mesylate salt)
- 英文别名:
- CEP-28122 (Mesylate salt)
- 中文名:
- CEP-28122 (Mesylate salt)
- 中文别名:
- ALK抑制剂(CEP-28122 MESYLATE SALT)
- CBNumber:
- CB22666785
- 分子式:
- C??H??ClN?O?S
- 分子量:
- 0
- MOL File:
- Mol file
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CEP-28122 (Mesylate salt)化学性质
CEP-28122 (Mesylate salt)性质、用途与生产工艺
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。
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
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Cell Line:
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Karpas-299, Sup-M2, Toledo and HuT-102 cells
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Concentration:
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10 nM, 100 nM, 1000 nM, 10000 nM
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Incubation Time:
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48 hours
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Result:
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Treatment led to concentration-dependent growth inhibition of Karpas-299 and Sup-M2 cells in culture.
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Western Blot Analysis
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Cell Line:
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Sup-M2 cells
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Concentration:
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30 nM, 100 nM, 300 nM, 1000 nM
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Incubation Time:
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2 hours
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Result:
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Resulted in substantial suppression of phosphorylation of putative downstream effectors of ALK, including Stat-3, Akt, and ERK1/2 in Sup-M2 cells.
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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
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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 .
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Animal Model:
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Female SCID mice bearing Sup-M2 subcutaneous tumor xenografts and
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mice bearing HCT116 aged 6-8 week old
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Dosage:
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3 mg/kg, 10 mg/kg and 30 mg/kg
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Administration:
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oral gavage; twice a day; 12 days
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Result:
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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
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nu
mice bearing HCT116.
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CEP-28122 (Mesylate salt)
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CEP-28122 (Mesylate salt) 试剂级价格
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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| 2024/04/30 | HY-18030A | CEP-28122 (Mesylate salt)
CEP-28122 mesylate salt | | 5 mg | 1500元 |
| 2024/04/30 | HY-18030A | CEP-28122 (Mesylate salt)
CEP-28122 mesylate salt | | 10 mM * 1 mLin DMSO | 2096元 |
CEP-28122 (Mesylate salt)
生产厂家
CEP-28122 (Mesylate salt) 相关搜索:
- 细胞生物学试剂
- ALK抑制剂(CEP-28122 MESYLATE SALT)
- CEP-28122 (Mesylate salt)