| 产品描述： | CHMFL-PI3KD-317 is a highly potent, selective and orally active PI3Kδ inhibitor, with an IC50 of 6 nM, and exhibits over 10-1500 fold selectivity over other class I, II and III PIKK family isoforms, such as PI3Kα (IC50, 62.6 nM), PI3Kβ (IC50, 284 nM), PI3Kγ (IC50, 202.7 nM), PIK3C2A (IC50, >10000 nM), PIK3C2B (IC50, 882.3 nM), VPS34 (IC50, 1801.7 nM), PI4KIIIA (IC50, 574.1 nM) and PI4KIIIB (IC50, 300.2 nM). CHMFL-PI3KD-317 inhibits PI3Kδ-mediated Akt T308 phosphorylation in Raji cells, with an EC50 of 4.3 nM. CHMFL-PI3KD-317 has antiproliferative effects on cancer cells |
| 靶点： |
PI3Kδ:6 nM (IC50);PI3Kα:62.6 nM (IC50);PI3Kβ:284 nM (IC50);PI3Kγ:202.7 nM (IC50);PIK3C2B:882.3 nM (IC50);Vps34:1801.7 nM (IC50);PI4KIIIA:574.1 nM (IC50);PI4KIIIB:300.2 nM (IC50);PI3K; PI4K |
| 体外研究： |
CHMFL-PI3KD-317 has antiproliferative effects, with GI50s of 3.5 ± 0.8, 4.0 ± 0.9, 4.8 ± 0.2, 3.3 ± 0.2, 3.0 ± 0.4 μM against PF382, NALM-6, MV4-11, MOLM-14 and MOLM-13 cells, respectively. |
| 体内研究： |
CHMFL-PI3KD-317 (Compound 15i; 25, 50 and 100 mg/kg/day, p.o., for 14 days) inhibits the growth of the MOLM14 tumor in mice. CHMFL-PI3KD-317 shows favorable oral bioavailability and acceptable half-life (T1/2 = 3.28 h) in Sprague-Dawley rats. Animal Model: Female nu/nu mice bearing MOLM-14 tumor xenografts Dosage: 25, 50 and 100 mg/kg/day Administration: P.O. for 14 days Result: Inhibited the growth of the MOLM14 tumor without mortality or obvious weight loss in mice. |
| 参考文献： |
1. 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 (PI3Kδ) inhibitor. Eur J Med Chem. 2018 |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.024 ml |
10.121 ml |
20.242 ml |
| 5 mM |
0.405 ml |
2.024 ml |
4.048 ml |
| 10 mM |
0.202 ml |
1.012 ml |
2.024 ml |
| 50 mM |
0.04 ml |
0.202 ml |
0.405 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京