Bafetinib (INNO-406)
商品编号:
TS0224
备注:
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详细介绍
l 基本信息 |
产品名称 | 巴非替尼(Bafetinib (INNO-406)) |
一般描述 | Bafetinib (巴非替尼) is a potent and selective dual Bcr-Abl/Lyn inhibitor. |
别 称 | 4-[[(3S)-3-(dimethylamino)pyrrolidin-1-yl]methyl]-N-[4-methyl-3-[(4-pyrimidin-5-ylpyrimidin-2-yl)amino]phenyl]-3-(trifluoromethyl)benzamide; NS-187 |
纯 度 | ≥98.0%(HPLC) | CAS NO. | 859212-16-1 |
分子式 | C30H31F3N8O | 分子量 | 576.62 |
适用范围 | 生物试剂,适用于细胞培养等 |
l 理化信息 |
外 观 | 固体 |
溶解性(25℃) | DMSO | ≥50mg/mL |
乙醇 | Insoluble |
水 | Insoluble |
l 生物学信息 |
生物活性/药理作用 | Bafetinib is an orally active 2-phenylaminopyrimidine derivative with potential antineoplastic activity. INNO-406 specifically binds to and inhibits the Bcr/Abl fusion protein tyrosine kinase, an abnormal enzyme produced by Philadelphia chromosomal translocation associated with chronic myeloid leukemia (CML). Furthermore, this agent also inhibits the Src-family member Lyn tyrosine kinase, upregulated in imatinib-resistant CML cells and in a variety of solid cancer cell types. The inhibitory effect of INNO-406 on these specific tyrosine kinases decreases cellular proliferation and induces apoptosis. A high percentage of CML patients are refractory to imatinib, which sometimes
results from point mutations occurring in the kinase domain of the Bcr/Abl fusion product. Due to its dual inhibitory activity, INNO-406 has been shown to overcome this particular drug resistance and to be a potent and effective agent in the treatment of imatinib-resistant CML. Bafetinib (INNO-406) is a potent and selective dual Bcr-Abl/Lyn inhibitor with IC50 of 5.8 nM/19 nM in cell-free assays, does not inhibit the phosphorylation of the T315I mutant and is less potent to PDGFR and c-Kit. |
l 存储 |
存储温度 | -20℃ |
l 注意事项及免责声明 |
本产品仅用于实验研究,不得作为药物使用,不得用于家用或其它用途。 |
l 参考文献 |
1. http://www.drugbank.ca 2. https://ncit.nci.nih.gov 3. https://www.ncbi.nlm.nih.gov |