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详细介绍
l 基本信息 |
产品名称 | CEP-32496 |
一般描述 | CEP-32496 is a highly potent inhibitor of BRAF(V600E/WT) and c-Raf with Kd of 14 nM/36 nM and 39 nM, also potent to Abl-1, c-Kit, Ret, PDGFRβ and VEGFR2, respectively insignificant affinity for MEK-1, MEK-2, ERK-1 and ERK-2. |
别 称 | Agerafenib |
纯 度 | ≥98.5%(HPLC) | CAS NO. | 1188910-76-0 |
分子式 | C24H22F3N5O5 | 分子量 | 517.46 |
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°C) | DMSO | ~5mg/ml |
乙醇 | Insoluble |
水 | Very slightly soluble |
l 生物学信息 |
生物活性/药理作用 | Agerafenib is an orally available v-raf murine sarcoma viral oncogene homolog B1 (B-raf) serine/threonine protein kinase inhibitor with potential antineoplastic activity. Agerafenib specifically and selectively inhibits the activity of the mutated form (V600E) of B-raf kinase. This inhibits the activation of the RAF/mitogen-activated protein kinase kinase (MEK)/extracellular signal-related kinase (ERK) signaling pathway and may result in a decrease in the proliferation of tumor cells expressing the mutated B-raf gene. The Raf mutation BRAF V600E, in which valine is substituted for glutamic acid at residue 600, is frequently found in a variety of human tumors and results in the constitutive activation of the RAF/MEK/ERK signaling pathway that regulates cellular proliferation and survival. |
l 存储 |
存储温度 | -20°C |
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 |