Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AS252424 是一种有效的、选择性的 PI3Kγ 抑制剂,其 IC50=30±10 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 289 | 现货 | ||
2 mg | ¥ 397 | 现货 | ||
5 mg | ¥ 618 | 现货 | ||
10 mg | ¥ 1,150 | 现货 | ||
25 mg | ¥ 1,780 | 现货 | ||
50 mg | ¥ 2,660 | 现货 | ||
100 mg | ¥ 3,990 | 现货 | ||
500 mg | ¥ 8,730 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 685 | 现货 |
产品描述 | AS-252424 is a potent and selective inhibitor of PI3Kγ with IC50 of 33 nM; >10 fold selectivity for PI3Kγ versus PI3Kα. |
靶点活性 | PI3Kγ:33 nM |
体外活性 | AS-252424 is a furan-2-ylmethylene thiazolidinedione as a selective ATP-competitive PI3Kγ inhibitor with IC50 with 33 nM. AS-252424 shows reduced potency on PI3Kα with an IC50 with 935 nM. When screening against 80 different Ser/Thr and Tyr kinases, AS-252424 doesn't show significant inhibit towards any of them at 10 μM except for CK2. AS-252424 inhibits C5a-mediated PKB/Akt phosphorylation in a concentration- dependent manner with submicromolar or low-micromolar IC50 value. AS-252424 inhibits MCP-1-mediated chemotaxis in wild-type primary monocytes in a concentration-dependent manner with an IC50 value of 52 μM, as well as in the monocytic cell line THP-1 with an IC50 value of 53 μM. [1] AS252424 specifically blocks proliferation in the pancreatic cancer cell lines HPAF and Capan1, as assessed by cell counting. [2] A recent research indicates 100 nM of AS-252424 significantly reduces [Ca2+]i, ICa and Ca2+ transients in HL-1 cardiomyocytes. [3] |
体内活性 | Oral administration of AS-252424 at 10 mg/kg results in moderate reduction of neutrophil recruitment (35%), almost matching the result observed in PI3Kγ-deficient mice. [1] |
激酶实验 | In vitro PI3Kγ Kinase Assay: 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 M ATP/100 nCi γ[33]ATP, final concentrations) and lipid vesicles containing 18 M PtdIns and 250 M of PtdSer (final concentrations), in the presence of AS-252424 or DMSO. Kinase reaction is stopped by adding 250 g of Neomycin-coated Scintillation Proximity Assay (SPA) beads and preceded. |
细胞实验 | After 3 hours of starvation in serum-free medium, Raw-264 macrophages are pretreated with AS-252424 or DMSO for 30 minutes and stimulated for 5 minutes with 50 nM C5a. PKB/Akt phosphorylation is monitored using phospho-Ser-473 Akt specific antibody and standard ELISA protocols.(Only for Reference) |
分子量 | 305.28 |
分子式 | C14H8FNO4S |
CAS No. | 900515-16-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 30.5 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.2757 mL | 16.3784 mL | 32.7568 mL | 81.892 mL |
5 mM | 0.6551 mL | 3.2757 mL | 6.5514 mL | 16.3784 mL | |
10 mM | 0.3276 mL | 1.6378 mL | 3.2757 mL | 8.1892 mL | |
20 mM | 0.1638 mL | 0.8189 mL | 1.6378 mL | 4.0946 mL | |
50 mM | 0.0655 mL | 0.3276 mL | 0.6551 mL | 1.6378 mL | |
100 mM | 0.0328 mL | 0.1638 mL | 0.3276 mL | 0.8189 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-252424 900515-16-4 Metabolism PI3K/Akt/mTOR signaling Stem Cells Casein Kinase PI3K inhibit Phosphoinositide 3-kinase Inhibitor AS 252424 AS252424 inhibitor