AS-604850 是一种有效的，具有选择性的和 ATP 竞争性的PI3Kγ抑制剂，IC50值为 0.25 μM，Ki值为 0.18 μM。AS-604850 是PI3Kγ的同工型选择性抑制剂，对PI3Kγ的选择性是 PI3Kδ/β 的 30 倍以上，是 PI3Kα 的 18 倍以上。
| 生物活性 | AS-604850 is a potent, selective and ATP-competitivePI3Kγinhibitor with anIC50value of 0.25 μM and aKivalue of 0.18 μM. AS-604850 shows isoform selective inhibitor ofPI3Kγwith over 30-fold selectivity forPI3Kδand β, and 18-fold selectivity overPI3Kα, respectively[1]. |
| IC50& Target[1] | PI3Kγ 0.25 μM (IC50) | PI3Kγ 0.18 μM (Ki) | PI3Kα 4.5 μM (IC50) |
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体外研究
(In Vitro) | AS-604850 inhibits C5a-mediated PKB phosphorylation with anIC50of 10 μM in RAW264 mouse macrophages[1].
AS-604850 blocks PKB phosphorylation induced by MCP-1 and has little or no effect after stimulation with CSF-1 in in primary monocytes from Pik3cg+/+or Pik3cg–/–mice[1].
AS-604850 (0-30 μM; 15 minutes; primary monocytes from Pik3cg+/+mice) treatment inhibits MCP-1-mediated phosphorylation of PKB and its downstream substrates GSK3α andβ in a concentration-dependent manner. MCP-1-induced phosphorylation of p44/42 ERK (ERK1/2) MAPKs is also reduced, in a concentration dependent manner in primary monocytes from Pik3cg+/+mice[1].
Western Blot Analysis[1] | Cell Line: | Primary monocytes from Pik3cg+/+mice | | Concentration: | 0 μM, 1 μM, 3 μM, 10 μM, 30 μM | | Incubation Time: | 15 minutes | | Result: | Inhibited MCP-1-mediated phosphorylation of PKB and its downstream substrates GSK3α andβ in a concentration-dependent manner. MCP-1-induced phosphorylation of p44/42 ERK (ERK1/2) MAPKs was also reduced, in a concentrationdependent manner in primary monocytes from Pik3cg+/+mice. |
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体内研究
(In Vivo) | AS-604850 (10-100 mg/kg; oral administration; for 4.5 or 4.25 hours; Balb/C or C3H mice) treatment reduces RANTES-induced peritoneal neutrophil recruitment with anED50value of 42.4 mg/kg. In the thioglycollate-induced peritonitis model, oral administration of 10 mg/kg AS-604850 results in a 31% reduction of neutrophil recruitment[1].
| Animal Model: | Balb/C or C3H mice with human recombinant RANTES or thioglycollate[1] | | Dosage: | 10 mg/kg, 30 mg/kg or 100 mg/kg | | Administration: | Oral administration; for 4.5 or 4.25 hours | | Result: | Reduced RANTES-induced peritoneal neutrophil recruitment with anED50value of 42.4 mg/kg. In the thioglycollate-induced peritonitis model, resulted in a 31% reduction of neutrophil recruitment. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 250 mg/mL(876.52 mM;Need ultrasonic) H2O :< 0.1 mg/mL (ultrasonic;warming;heat to 60℃)(insoluble) 配制储备液 | 1 mM | 3.5061 mL | 17.5303 mL | 35.0607 mL | | 5 mM | 0.7012 mL | 3.5061 mL | 7.0121 mL | | 10 mM | 0.3506 mL | 1.7530 mL | 3.5061 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (7.29 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (7.29 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (7.29 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (7.29 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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