AS-604850-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAS-604850Cat. No.: HY-13531CAS No.: 648449-76-7分式: CHFNOS分量: 285.22作靶點: PI3K作通路: PI3K/Akt/mTOR儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 250 mg/mL (876.52 mM; Need ultrasonic)Mass Solv

2、ent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 3.5061 mL 17.5303 mL 35.0607 mL5 mM 0.7012 mL 3.5061 mL 7.0121 mL10 mM 0.3506 mL 1.7530 mL 3.5061 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗 請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍福渲魄罢埾扰渲瞥蔚膬湟?，再依次添加助溶?為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分指該溶劑在您配

3、制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (7.29 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (7.29 mM); Clear solutionBIOLOGICAL ACTIVITY1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE物活性 AS-604850種有效的，具有選擇性的和 ATP 競爭性的

4、 PI3K 抑制劑，IC50 值為 0.25 M，Ki 值為 0.18M。AS-604850PI3K 的同型選擇性抑制劑，對 PI3K 的選擇性PI3K/ 的 30 倍以上，PI3K 的 18 倍以上。IC50 & Target PI3K PI3K PI3K0.25 M (IC50) 0.18 M (Ki) 4.5 M (IC50)體外研究 AS-604850 inhibits C5a-mediated PKB phosphorylation with an IC50 of 10 M in RAW264 mousemacrophages 1.AS-604850 blocks PKB phosp

5、horylation induced by MCP-1 and has little or no effect after stimulation withCSF-1 in in primary monocytes from Pik3cg+/+ or Pik3cg/ mice 1.AS-604850 (0-30 M; 15 minutes; primary monocytes from Pik3cg+/+ mice) treatment inhibits MCP-1-mediated phosphorylation of PKB and its downstream substrates GS

6、K3 and in a concentration-dependentmanner. MCP-1-induced phosphorylation of p44/42 ERK (ERK1/2) MAPKs is also reduced, in aconcentration dependent manner in primary monocytes from Pik3cg+/+ mice 1.Western Blot Analysis 1Cell Line: Primary monocytes from Pik3cg+/+ miceConcentration: 0 M, 1 M, 3 M, 10

7、 M, 30 MIncubation Time: 15 minutesResult: Inhibited MCP-1-mediated phosphorylation of PKB and its downstream substrates GSK3 and in a concentration-dependent manner. MCP-1-induced phosphorylation of p44/42ERK (ERK1/2) MAPKs was also reduced, in a concentrationdependent manner inprimary monocytes fr

8、om Pik3cg+/+ mice.體內(nèi)研究 AS-604850 (10-100 mg/kg; oral administration; for 4.5 or 4.25 hours; Balb/C or C3H mice) treatment reducesRANTES-induced peritoneal neutrophil recruitment with an ED50 value of 42.4 mg/kg. In the thioglycollate-induced peritonitis model, oral administration of 10 mg/kg AS-6048

9、50 results in a 31% reduction of neutrophilrecruitment 1.Animal Model: Balb/C or C3H mice with human recombinant RANTES or thioglycollate 1Dosage: 10 mg/kg, 30 mg/kg or 100 mg/kgAdministration: Oral administration; for 4.5 or 4.25 hoursResult: Reduced RANTES-induced peritoneal neutrophil recruitment

10、 with an ED50 value of 42.4mg/kg. In the thioglycollate-induced peritonitis model, resulted in a 31% reduction ofneutrophil recruitment.REFERENCES2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE1. Camps M, et al. Blockade of PI3Kgamma suppresses joint inflammation and damage in mouse models of rheumatoid arthritis. Nat Med.2005 Sep;11(9):936-43.McePdfHeightCaution: Product has not been fully v