• 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。

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *