Powder: -20°C for 3 years | In solvent: -80°C for 1 year
IC-87114 是一种有效的、选择性的PI3Kδ抑制剂,其 IC50=0.5 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 283 | 现货 | ||
5 mg | ¥ 455 | 现货 | ||
10 mg | ¥ 728 | 现货 | ||
25 mg | ¥ 1,280 | 现货 | ||
50 mg | ¥ 2,160 | 现货 | ||
100 mg | ¥ 3,490 | 现货 | ||
200 mg | ¥ 4,980 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 490 | 现货 |
产品描述 | IC-87114 is a specific PI3Kδ inhibitor(IC50=0.5 μM). |
靶点活性 | PI3Kγ:29 μM, PI3Kδ:0.5 μM |
体外活性 | 在有炎症反应的鼠模型中,IC87114阻断TNF1α刺激产生蛋白酶的胞外分泌. |
体内活性 | 在人类中性粒细胞中,IC87114(5 μM)能够地抑制N-甲酰 - 甲硫氨酰 - 亮氨酰 - 苯丙氨酸(fMLP) - 刺激的磷脂酰肌醇三磷酸(PIP3)的生物合成和趋化性。在人类急性骨髓性白血病(AML)原始细胞如骨髓单个核细胞(BMMCs)中,IC87114(10 μM)抑制组成型和Flt-3刺激的Akt磷酸化和细胞增殖。在抗CD3刺激的小鼠CD62L +(幼稚)和CD62L-(效应/记忆)CD4 + T细胞中,IC87114抑制增殖和干扰素-γ(IFN-γ)产生。 |
激酶实验 | PI3K kinase assay: Phosphatidylinositol-(4,5)-bisphosphate (PIP2) containing phospholipid liposomes are prepared. Briefly, bovine PIP2 and phosphatidylserine (1:2 molar ratio) are vacuum-dried and resuspended at 1 mM PIP2 in 20 mM HEPES-KOH, pH 7.4, 50 mM NaCl, and 5 mM EDTA. The lipid suspension is subjected to a brief sonication, followed by 5 freeze-thaw cycles and then 20 extrusion cycles to produce the liposomes. The assay is conducted in 60 μL reaction volumes in 20 mM HEPES, pH 7.4, buffer containing 1 nM PI3K, 1 μM PIP2, 200 μM ATP, 1 μCi [γ-32P]ATP, 5 mM MgCl2, plus 50 μg/mL horse IgG as carrier protein. The reaction is incubated for 10 min at room temperature, quenched in 140 of 1 M K2PO4, 30 mM EDTA, pH 8.0, captured onto a 96-well polyvinylidene difluoride filter plate, and washed five times with 1 M K2PO4. The filter is allowed to dry completely, and the bound radioactivity is quantitated. IC87114 dilutions are assayed in a final concentration of 1% (w/w) DMSO. |
细胞实验 | For AML cell proliferation assay, BMMCs are isolated and cultured in α-medium with 5% fetal calf serum (FCS) with or without FLT-3 ligand (10 ng/mL) for 48 hours and with or without IC87114. [3H]-thymidine (1 μCi [37 kBq]) is added for a final 6 hours and the amount of radioactivity incorporated is determined by trichloracetic acid precipitation. CD34+ cells from cord blood are cultured in stem cell factor (SCF; 20 ng/mL), FLT-3 ligand (10 ng/mL), and Tpo (20 nM) for 48 hours with or without 10 μM IC87114 and pulsed for 12 hours with [3H]-thymidine. (Only for Reference) |
别名 | IC 87114 |
分子量 | 397.43 |
分子式 | C22H19N7O |
CAS No. | 371242-69-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 8 mg/mL (20.13 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.5162 mL | 12.5808 mL | 25.1617 mL | 62.9042 mL |
5 mM | 0.5032 mL | 2.5162 mL | 5.0323 mL | 12.5808 mL | |
10 mM | 0.2516 mL | 1.2581 mL | 2.5162 mL | 6.2904 mL | |
20 mM | 0.1258 mL | 0.629 mL | 1.2581 mL | 3.1452 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。
IC-87114 371242-69-2 PI3K/Akt/mTOR signaling PI3K IC 87114 Inhibitor inhibit IC87114 Phosphoinositide 3-kinase inhibitor