CHMFL-PI3KD-317 - PI3K 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECHMFL-PI3KD-317Cat. No.: HY-112608CAS No.: 2244992-76-3分式: CHClNOS分量: 494.03作靶点: PI3K作通路: PI3K/Akt/mTOR储存式: Please store the product under the recommended conditions inthe COA.BIOLOGICAL ACTIVITY物活性 CHMFL-PI3KD-317种效、选择性、可服的 PI3

2、K 抑制剂，IC50 值为 6 nM，对其选择性是对其他PIKK 家族的 10-1500 倍，例如 PI3K (IC50，62.6 nM)，PI3K (IC50，284 nM)，PI3K (IC50，202.7nM)，PIK3C2A (IC50，10000 nM)，PIK3C2B (IC50，882.3 nM)，VPS34 (IC50，1801.7 nM)，PI4KIIIA(IC50，574.1 nM) 和 PI4KIIIB (IC50，300.2 nM)。在 Raji 细胞中，CHMFL-PI3KD-317 抑制 PI3K 介导的 AktT308 磷酸化，EC50 值为 4.3 nM。CHM

3、FL-PI3KD-317 对癌细胞具有抗增殖作 1。IC50 & Target PI3K PI3K PI3K PI3K6 nM (IC50) 62.6 nM (IC50) 202.7 nM (IC50) 284 nM (IC50)PIK3C2B Vps34 PI4KIIIB PI4KIIIA882.3 nM (IC50) 1801.7 nM (IC50) 300.2 nM (IC50) 574.1 nM (IC50)体外研究 CHMFL-PI3KD-317 has antiproliferative effects, with GI50s of 3.50.8, 4.00.9, 4.80.2,

4、3.30.2,3.00.4 M against PF382, NALM-6, MV4-11, MOLM-14 and MOLM-13 cells, respectively 1.体内研究CHMFL-PI3KD-317 (Compound 15i; 25, 50 and 100mg/kg/day, p.o., for 14 days) inhibits the growth of theMOLM14 tumor in mice 1.CHMFL-PI3KD-317 shows favorable oral bioavailability and acceptable half-life (T1/2

5、=3.28h) in Sprague-Dawley rats 1.Animal Model: Female nu/nu mice bearing MOLM-14 tumor xenografts 1Dosage: 25, 50 and 100mg/kg/day1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEAdministration: P.O. for 14 daysResult: Inhibited the growth of the MOLM14 tumor without mortality or obvious weight loss

6、 inmice.REFERENCES1. Liang X, et al. Discovery of (S)-2-amino-N-(5-(6-chloro-5-(3-methylphenylsulfonamido)pyridin-3-yl)-4-methylthiazol-2-yl)-3-methylbutanamide (CHMFL-PI3KD-317) as a potent and selective phosphoinositide 3-kinase delta (PI3K) inhibitor. Eur J Med Chem. 2018Aug 5;156:831-846.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 40