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IPI-9119
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
IPI-9119图片
CAS NO:1346564-56-4
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
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。
Cas No.1346564-56-4
分子式C24H19F2N5O5
分子量495.43
溶解度DMSO : 100 mg/mL (201.84 mM; Need ultrasonic)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

IPI-9119 is an orally active, selective and irreversible FASN inhibitor with an IC50 of 0.3 nM in vitro biochemical assay. IPI-9119 inhibits tumor growth of castration-resistant prostate cancer (CRPC) xenografts mouse models[1][2].

IPI-9119 inhibits FASN in cellular occupancy assays (IC50∼10nM), and shows more than 400-fold selectivity against several additional serine hydrolases[2]. IPI-9119 (0.1-0.5 μM; 6 days) inhibits cell growth and induces cell cycle arrest, apoptosis[1]. IPI-9119 (0.05-5 μM; 6 days) inhibits AR-FL and AR-V7 protein expression[1].

IPI-9119 (SC pump infusion; 0.5 μL/h; 100 mg/mL; for 28 days) inhibits tumor growth of CRPC xenografts mouse models[1].

[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.