IPI-9119
目录号: PL14887 纯度: ≥98%
CAS No. :1346564-56-4
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中文名称
IPI-9119
英文名称
IPI-9119
英文别名
4-[[4-(2,6-Difluorophenyl)-5-oxotetrazole-1-carbonyl]-propan-2-ylamino]-3-phenoxybenzoic acid;IPI-9119
Cas No.
1346564-56-4
分子式
C24H19F2N5O5
分子量
495.44
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
IPI-9119 是一种具有口服活性,选择性和不可逆的 FASN 抑制剂,IC50 值为 0.3 nM。IPI-9119 抑制去势抵抗性前列腺癌 (CRPC) 异种移植小鼠模型中的肿瘤生长。
生物活性
IPI-9119 is an orally active, selective and irreversible FASN inhibitor with an IC 50 of 0.3 nM in vitro biochemical assay. IPI-9119 inhibits tumor growth of castration-resistant prostate cancer (CRPC) xenografts mouse models.
性状
Solid
IC50 & Target[1][2]
IC50: 0.3 nM (FASN)
体外研究(In Vitro)
IPI-9119 inhibits FASN in cellular occupancy assays (IC50~10nM), and shows more than 400-fold selectivity against several additional serine hydrolases.
IPI-9119 (0.1-0.5 μM; 6 days) inhibits cell growth and induces cell cycle arrest, apoptosis.
IPI-9119 (0.05-5 μM; 6 days) inhibits AR-FL and AR-V7 protein expression.
has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability Assay
体内研究(In Vivo)
IPI-9119 (SC pump infusion; 0.5 μL/h; 100 mg/mL; for 28 days) inhibits tumor growth of CRPC xenografts mouse models.
has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 8-10-week mal
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]. Giorgia Zadra, et al. Inhibition of de novo lipogenesis targets androgen receptor signaling in castration-resistant prostate cancer. Proc Natl Acad Sci U S A. 2019 Jan 8;116(2):631-640.
[2]. Erin Broph, et al. Abstract 1891: Pharmacological target validation studies of fatty acid synthase in carcinoma using the potent, selective and orally bioavailable inhibitor IPI-9119.
溶解度数据
In Vitro: DMSO : 100 mg/mL (201.84 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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