上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。
Nirogacestat dihydrobromide (Synonyms: PF-3084014 dihydrobromide; PF-03084014 dihydrobromide)
Nirogacestat dihydrobromide (PF-3084014 dihydrobromide) 是一种有效的，具有口服活性的，可逆的非竞争性的选择性的 γ-secretase 抑制剂，IC50 为 6.2 nM。Nirogacestat dihydrobromide 抑制 Notch 信号通路，同时最小化胃肠道毒性。可用于研究 Notch 受体依赖性肿瘤。
Nirogacestat dihydrobromide Chemical Structure
CAS No. : 1962925-29-6
| 规格 | 是否有货 | ||
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| 100 mg | 询价 | ||
| 250 mg | 询价 | ||
| 500 mg | 询价 |
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Nirogacestat dihydrobromide 的其他形式现货产品:
| 生物活性 |
Nirogacestat dihydrobromide (PF-3084014 dihydrobromide) is a reversible, orally bioavailable, noncompetitive, and selective γ-secretase inhibitor with an IC50 of 6.2 nM. Inhibition of Notch signaling by Nirogacestat dihydrobromide while minimizing gastrointestinal toxicity presents a promising approach for research of Notch receptor-dependent cancers[1]. |
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| 体外研究 (In Vitro) |
The IC50 of Nirogacestat (PF-03084014) for γ-secretase enzyme inhibition in cell-free assay for Aβ production using detergent solubilized membranes derived from HeLa cells is determined to be 6.2 nM. When tested for inhibition of Notch receptor cleavage in cellular assays using HPB-ALL cells that harbor mutations in both the heterodimerization and PEST domains in Notch1, the cell IC50 is determined to be 13.3 nM. Nirogacestat causes a significant increase in caspase-3 activities in HPB-ALL and TALL-1 cells as well as an induction of cleaved PARP and cleaved caspase-3 after a 7-day treatment[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only. |
| 体内研究 (In Vivo) |
Nirogacestat (PF-03084014) shows robust antitumor activity in this model on 14-day twice daily dosing. Tumor growth inhibition is dose dependent, with maximal tumor growth inhibition of ~92% obtained at high dose levels (150 mg/kg). In tumor growth inhibition studies where mice receive repetitive twice daily dosing for more than a week, Nirogacestat is well tolerated at dose levels below 100 mg/kg as no significant weight loss, morbidity, or mortality is observed. When the dose is increased to 150 mg/kg, however, mice have diarrhea and show weight loss (10-15%) approximately 10 days after compound administration. The body weight of treated animals usually returns to normal if dosing holidays are given, suggesting that the toxicity of Nirogacestat is reversible[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only. |
| Clinical Trial |
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| 分子量 |
651.47 |
| Formula |
C27H43Br2F2N5O |
| CAS 号 |
1962925-29-6 |
| 运输条件 |
Room temperature in continental US; may vary elsewhere. |
| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis. |
| 参考文献 |
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