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Eganelisib

Eganelisib

产品编号 T5432   CAS 1693758-51-8
别名: IPI-549

Eganelisib (IPI-549) 是 PI3Kγ的选择性抑制剂,其 IC50=16 nM,选择性是其他脂类和蛋白质激酶的 100 倍以上。

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Eganelisib Chemical Structure
Eganelisib, CAS 1693758-51-8
规格 价格/CNY 货期 数量
1 mg ¥ 270 现货
5 mg ¥ 587 现货
10 mg ¥ 1,090 现货
25 mg ¥ 2,160 现货
50 mg ¥ 2,670 现货
100 mg ¥ 3,980 现货
500 mg ¥ 8,730 现货
1 mL * 10 mM (in DMSO) ¥ 683 现货
产品目录号及名称: Eganelisib (T5432)
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选择批次  
纯度: 99.56%
纯度: 99.04%
更多批次查询请联系客服
生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Eganelisib (IPI-549) is an inhibitor of PI3Kγ (IC50 = 16, 3,200, 3,500, and >8,400 nM for PI3Kγ, PI3Kα, PI3Kβ, and PI3Kδ, respectively)
靶点活性 3.5 μM:PI3Kγ, 16 nM:, PI3Kα:3.2 μM
体外活性 IPI-549 sensitizes doxorubicin-resistant SW620/Ad300 cells to P-glycoprotein (P-gp) substrates, such as paclitaxel (IC50s = 710 and 6.7 nM for paclitaxel alone and in combination with IPI-549, respectively), and increases the level of intracellular paclitaxel in SW620/Ad300 cells[1].
体内活性 IPI-549 demonstrates favorable pharmacokinetic properties and robust inhibition of PI3K-γ mediated neutrophil migration in vivo[2].
动物实验 SW620 (4 X 10^6 ) and SW620/Ad300 (5 X 10^6 ) cells were injected subcutaneously at the flank near the armpits of athymic nude mice.?When the subcutaneous tumors were approximately 0.5 x 0.5 cm in size (day 0), the mice were randomized into four treatment groups.?The vehicle used to deliver the IPI-549 and paclitaxel by intraperitoneal (i.p.) injection was ethanol/Cremophor ELP/saline (10%/10%/80%).?Group one received the vehicle only;?group two received vehicle plus 3 mg/kg IPI-549;?group three received vehicle plus 15 mg/kg paclitaxel;?group four, the combination group, received vehicle plus 3 mg/kg IPI-549 one h prior to administration of vehicle plus 15 mg/kg paclitaxel.?The drug doses were administered every 3 days with a total of 4 doses.?Tumor volume was measured using calipers, and body weights were recorded prior to each dosing.
别名 IPI-549
分子量 528.56
分子式 C30H24N8O2
CAS No. 1693758-51-8

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 15 mg/mL (28.38 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8919 mL 9.4597 mL 18.9193 mL 47.2983 mL
5 mM 0.3784 mL 1.8919 mL 3.7839 mL 9.4597 mL
10 mM 0.1892 mL 0.946 mL 1.8919 mL 4.7298 mL
20 mM 0.0946 mL 0.473 mL 0.946 mL 2.3649 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. De Vera AA1, Gupta P.et al.Immuno-oncology agent IPI-549 is a modulator of P-glycoprotein (P-gp, MDR1, ABCB1)-mediated multidrug resistance (MDR) in cancer: In vitro and in vivo.Cancer Lett. 2019 Feb 1;442:91-103 2. Evans CA, et al. Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-γ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate. ACS Med Chem Lett. 2016 Jul 22;7(9):862-7.

文献引用

1. Jiang Y, Xiong W, Jia L, et al. Developing a Naïve Bayesian Classification Model with PI3Kγ structural features for virtual screening against PI3Kγ: Combining molecular docking and pharmacophore based on multiple PI3Kγ conformations. European Journal of Medicinal Chemistry. 2022: 114824. 2. Xiong W, Jia L, Liang J, et al. Investigation into the anti-airway inflammatory role of the PI3Kγ inhibitor JN-PK1: An in vitro and in vivo study. International Immunopharmacology. 2022, 111: 109102 3. Xiong W, Jia L, Liang J, et al.Investigation into the anti-airway inflammatory role of the PI3Kγ inhibitor JN-PK1: An in vitro and in vivo study.International Immunopharmacology.2022, 111: 109102. 4. Xiong W, Jia L, Cai Y, et al.Evaluation of the anti-inflammatory effects of PI3Kδ/γ inhibitors for treating acute lung injury.Immunobiology.2023: 152753.
Voxtalisib TG 100713 CAL-101 Copanlisib SKI V XL388 LAS191954 Pictilisib dimethanesulfonate

相关化合物库

该产品包含在如下化合物库中:
抗癌临床化合物库 抗癌药物库 高选择性抑制剂库 抗癌活性化合物库 临床期小分子药物库 氧化还原化合物库 抗胰腺癌化合物库 抗结直肠癌化合物库 抗抑郁症化合物库 ReFRAME 相关化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Eganelisib 1693758-51-8 PI3K/Akt/mTOR signaling PI3K inhibit Inhibitor IPI-549 IPI 549 IPI549 Phosphoinositide 3-kinase inhibitor

 

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