Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AS-605240 是一种有效且特异性的 PI3Kγ 抑制剂,IC50值为 8 nM,Ki 值为 7.8 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 159 | 现货 | ||
5 mg | ¥ 347 | 现货 | ||
10 mg | ¥ 549 | 现货 | ||
25 mg | ¥ 1,070 | 现货 | ||
50 mg | ¥ 1,930 | 现货 | ||
100 mg | ¥ 3,270 | 现货 | ||
200 mg | ¥ 4,680 | 现货 | ||
500 mg | ¥ 7,180 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 297 | 现货 |
产品描述 | AS-605240 is an effective and specific inhibitor of PI3Kγ (IC50/Ki: 87.8 nM). |
靶点活性 | PI3Kγ:87.8 nM |
体外活性 | 在肥胖症诱导的糖尿病ob/ob鼠模型中,AS-605240(10 mg/kg)会降低血糖水平, 使胰岛素敏感性和葡萄糖耐量显著提高,且对体重无影响,30 mg/kg剂量的效果更好,对体重只有轻微影响.AS-605240使ATMs量和MCP-1循环水平降低. 在αCII诱导的关节炎中,AS-605240(50 mg/kg)保护其免受 αCII-IA症状.在胶原诱导的关节炎鼠模型中,AS-605240(50 mg/kg)也抑制关节炎症和损伤.AS-605240可使RANTES诱导的患腹膜炎鼠体内的中性粒细胞趋化性降低(ED50:9.1 mg/kg). |
体内活性 | 在骨髓单核细胞中,AS-605240(1 μM)对MCP-1或CSF-1诱导的PKB磷酸化有抑制作用。在鼠的SC-CA1突触中,AS-605240(100 nM)消除NMDAR LTD,但对mGluR LTD和LTP无影响。AS-605240对PI3Kα/β/δ(IC50:60/270/300 nM)也有抑制作用。AS-605240还抑制C5a调节的PKB磷酸化(IC50:90 nM)。 |
激酶实验 | In vitro PI3K lipid kinase assay: (1) For PI3Kγ: human PI3Kγ (100 ng) is incubated at RT with kinase buffer (10 mM MgCl2, 1 mM β-glycerophosphate, 1 mM DTT, 0.1 mM Na3VO4, 0.1% Na Cholate and 15 μM ATP/100 nCi γ[33P]ATP, final concentrations) and lipid vesicles containing 18 μM PtdIns and 250 μM of PtdSer (final concentrations), in the presence of AS-605240 or DMSO. Kinase reaction is stopped by adding 250 μg of Neomycin-coated Scintillation Proximity Assay (SPA) beads. (2) For PI3Kα, β, and δ: varying amounts of ATP are incubated with the different purified PI3K isoforms and saturating concentrations of PtdIns. Consequently, IC50 determinations with PI3Kα, β, and δ, to evaluate inhibitor selectivity are performed as follows: 60 ng of PI3Kα are incubated at RT with kinase buffer, as described for PI3Kγ (but containing 89 μM ATP/300 nCi γ[33P]ATP and no Na Cholate, instead) and lipid vesicles containing 212 μM PtdIns and 58 μM of PtdSer. 100 ng of PI3Kβ are incubated at RT with kinase buffer (containing 70 μM ATP/300 nCi γ[33P]ATP, 4 mM MgCl2 and no Na Cholate) and lipid vesicles containing 225 μM PtdIns and 45 μM of PtdSer. 90 ng of PI3Kδ are incubated with kinase buffer (containing 65 μM ATP/300 nCi γ[33P]ATP, 1 mM MgCl2, and no Na Cholate) and lipid vesicles containing 100 μM PtdIns and 170 μM of PtdSer. The reactions are stopped after 2 hours. |
细胞实验 | After a 3-hour starvation in serum-free medium, Cells are pretreated with AS-605240 or DMSO for 30 min and stimulated for 5 min with 50 nM of C5a. PKB phosphorylation is monitored using phosphorylated Ser473 Akt-specific antibody and standard ELISA protocols. (Only for Reference) |
别名 | 5-(6-喹噁啉yl亚甲基)-2,4-噻唑烷二酮, AS 605240 |
分子量 | 257.27 |
分子式 | C12H7N3O2S |
CAS No. | 648450-29-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 5.8 mg/mL (22.54 mM), Sonification is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.887 mL | 19.4348 mL | 38.8697 mL | 97.1742 mL |
5 mM | 0.7774 mL | 3.887 mL | 7.7739 mL | 19.4348 mL | |
10 mM | 0.3887 mL | 1.9435 mL | 3.887 mL | 9.7174 mL | |
20 mM | 0.1943 mL | 0.9717 mL | 1.9435 mL | 4.8587 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。
AS-605240 648450-29-7 Autophagy PI3K/Akt/mTOR signaling PI3K inhibit Inhibitor Phosphoinositide 3-kinase 5-(6-喹噁啉yl亚甲基)-2,4-噻唑烷二酮 AS 605240 AS605240 inhibitor