IPI-9119

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IPI-9119  纯度: 98.13%

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。

IPI-9119

IPI-9119 Chemical Structure

CAS No. : 1346564-56-4

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥5450 In-stock
5 mg ￥5000 In-stock
10 mg ￥8500 In-stock
25 mg ￥18000 In-stock
50 mg ￥30000 In-stock
100 mg ￥46000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

IPI-9119 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Orally Active Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Anti-Obesity Compound Library
  • Lipid Metabolism Compound Library
  • Targeted Diversity Library

生物活性

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].

IC50 & Target

IC50: 0.3 nM (FASN)[1]
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[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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: Prostate cancer (PCa) cells (AD LNCaP, AI C4-2, LNCaP-95 and 22Rv1 AI cells)
Concentration: 0.1, 0.5 μM
Incubation Time: 6 days
Result: Inhibited PCa cell growth.
Had no growth inhibition in FASN KO PCa cells.

Cell Cycle Analysis[1]

Cell Line: PCa cells
Concentration: 0.1, 0.5 μM
Incubation Time: 6 days
Result: Reduced the proportion of S-phase cells and increased that of G0/G1-, sub-G1–phase cells and decreased expression of cyclin A2.

Western Blot Analysis[1]

Cell Line: PCa cells
Concentration: 0.05, 0.1, 0.25, 0.5, 5 μM
Incubation Time: 6 days
Result: Significantly decreased AR-FL protein levels in AD LNCaP, AI C4-2 cells (expressing only AR-FL) and reduced the expression of AR-V7 in LNCaP-95, 22Rv1 AI cells driven by this variant.

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[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 8-10-week male Ncr Nu Castrated mice or castrated NOD male SCID with 22Rv1 or LNCaP-95 cells[1]
Dosage: 100 mg/mL
Administration: SC pump infusion (0.5 μL/h; 100 mg/mL); for 28 days
Result: Inhibited tumor growth of castration-resistant prostate cancer (CRPC) xenografts mouse models.

分子量

495.43

Formula

C24H19F2N5O5
CAS 号

1346564-56-4
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
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (201.84 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0184 mL 10.0922 mL 20.1845 mL
5 mM 0.4037 mL 2.0184 mL 4.0369 mL
10 mM 0.2018 mL 1.0092 mL 2.0184 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.20 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.20 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.20 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.20 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.20 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.20 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
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.

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