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| 品牌 | absin | CAS | 900515-16-4 |
|---|---|---|---|
| 分子式 | C14H8FNO4S | 纯度 | 98% |
| 分子量 | 305.28 | 货号 | abs47028278 |
| 规格 | 10mg | 供货周期 | 现货 |
| 主要用途 | is a potent and selective inhibitor of P | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
AS-252424 900515-16-4
| 产品描述 | |
| 描述 | AS-252424 is a potent and selective inhibitor of PI3Kγ with IC50 of 33 nM; >10 fold selectivity for PI3Kγ versus PI3Kα. |
| 纯度 | 98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | AS252424；AS 252424 |
| 外观 | Yellow to brown crystalline solid. |
| 可溶性/溶解性 | DMSO : 30.5 mg/mL (100 mM) |
| 生物活性 | |
| 靶点 | Casein Kinase 2 ,PI3Kγ ,PI3Kα |
| In vitro(体外研究) | 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-micromolarIC50 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. AS252424 specifically blocks proliferation in the pancreatic cancer cell lines HPAF and Capan1, as assessed by cell counting. A recent research indicates 100 nM of AS-252424 significantly reduces i, ICa and Ca2+ transients in HL-1 cardiomyocytes. |
| In vivo(体内研究) | 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. |
| 研究领域 | |
| 研究领域 | CancerTumor biomarkers Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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