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AS-604850
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AS-604850图片
CAS NO:648449-76-7
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
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)

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.
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.
分子量

285.22

性状

Solid

Formula

C11H5F2NO4S

CAS 号

648449-76-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
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
浓度溶剂体积质量1 mg5 mg10 mg
1 mM3.5061 mL17.5303 mL35.0607 mL
5 mM0.7012 mL3.5061 mL7.0121 mL
10 mM0.3506 mL1.7530 mL3.5061 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。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 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。