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CHMFL-PI3KD-317

    
98%

源葉(MedMol)
S89363 一鍵復(fù)制產(chǎn)品信息
2244992-76-3
C21H24ClN5O3S2
494.03
貨號(hào) 規(guī)格 價(jià)格 上海 北京 武漢 南京 購(gòu)買數(shù)量
S89363-5mg 98% ¥800.00 6 - - -
S89363-10mg 98% ¥1500.00 7 - - -
S89363-25mg 98% ¥3500.00 6 - - -
S89363-100mg 98% ¥9000.00 貨期:2-3天 - - -
產(chǎn)品介紹 參考文獻(xiàn) 質(zhì)檢證書(shū)(COA) 摩爾濃度計(jì)算器 相關(guān)產(chǎn)品

產(chǎn)品介紹

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

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
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參考文獻(xiàn)

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摩爾濃度計(jì)算器

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