Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 15 mg/mL (28.38 mM)
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 |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
Eganelisib 1693758-51-8 PI3K/Akt/mTOR signaling PI3K inhibit Inhibitor IPI-549 IPI 549 IPI549 Phosphoinositide 3-kinase inhibitor