FT671
目录号: PL01637 纯度: ≥99%
CAS No. :1959551-26-8
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中文名称
FT671
英文名称
FT671
英文别名
(R)-5-((1-(4,4-Difluoro-3-(3-fluoro-1H-pyrazol-1-yl)butanoyl)-4-hydroxypiperidin-4-yl)methyl)-1-(4-fluorophenyl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one;5-[[1-[(3R)-4,4-Difluoro-3-(3-fluoropyrazol-1-yl)butanoyl]-4-hydroxypiperidin-4-yl]methyl]-1-(4-fluo;FT671
Cas No.
1959551-26-8
分子式
C24H23F4N7O3
分子量
533.48
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
FT671是有效、非共价的、选择性的 USP7 抑制剂,IC50 值为 52 nM,与USP7催化域结合的 Kd 值为65 nM。
生物活性
FT671 is a potent, non-covalent and selective USP7 inhibitor with an IC 50 of 52 nM and binds to the USP7 catalytic domain with a K d of 65 nM.
性状
Solid
IC50 & Target[1][2]
IC50: 52 nM (USP7)
Kd: 65 nM (USP7)
体外研究(In Vitro)
FT671 increases p53 protein levels in HCT116 or bone osteosarcoma (U2OS) cell lines, leading to induction of p53 target genes including BBC3 (which encodes PUMA), CDKN1A (p21), RPS27L (S27L) and MDM2. FT671 leads to the degradation of N-Myc and upregulation of p53 in the neuroblastoma cell line IMR-32. FT671 also stabilizes p53 in the MM.1S multiple myeloma cell line, which correlates with increased MDM2 ubiquitination and leads to expression of p53 target genes. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
FT671 (100 mg/kg and 200 mg/kg, Oral gavage, daily) treatment in mice leads to a significant dose-dependent inhibition of tumor growth. And FT671 is well-torelated even at high doses. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Turnbull AP, et al. Molecular basis of USP7 inhibition by selective small-molecule inhibitors. Nature. 2017 Oct 26;550(7677):481-486.
溶解度数据
In Vitro: DMSO : 50 mg/mL (93.72 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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