• 產(chǎn)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

• 靶點(diǎn)： 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

• 體外研究：
  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.

• 體內(nèi)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.

• 參考文獻(xiàn)：
  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

• 保存條件： -20℃

• 配置溶液濃度參考：
  

  	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：部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

輸入產(chǎn)品批號(hào)：

本計(jì)算器可幫助您計(jì)算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系，公式為：

質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

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