IPI-9119|cas:1346564-56-4|西域试剂

IPI-9119,98.13%

产品编号：Bellancom-124628| CAS NO：1346564-56-4| 分子式：C₂₄H₁₉F₂N₅O₅| 分子量：495.43

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货号	价格	库存与货期
Bellancom-124628	￥5000.00	杭州北京（现货）
Bellancom-124628	￥8500.00	杭州北京（现货）
Bellancom-124628	￥18000.00	杭州北京（现货）
Bellancom-124628	￥30000.00	杭州北京（现货）
Bellancom-124628	￥46000.00	杭州北京（现货）

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IPI-9119

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。

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.

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

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

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

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.

西域 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
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.

体内研究

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

西域 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
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.

体内研究

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

西域 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
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.

性状

Solid

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。