| Hazard Information | Back Directory | [Uses]
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[1]. | [in vivo]
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[1].
CHMFL-PI3KD-317 shows favorable oral bioavailability and acceptable half-life (T1/2 = 3.28 h) in Sprague-Dawley rats[1]. | Animal Model: | Female nu/nu mice bearing MOLM-14 tumor xenografts[1] | | 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. |
| [IC 50]
PI3Kδ: 6 nM (IC50); PI3Kα: 62.6 nM (IC50); PI3Kγ: 202.7 nM (IC50); PI3Kβ: 284 nM (IC50); PIK3C2B: 882.3 nM (IC50); Vps34: 1801.7 nM (IC50); PI4KIIIB: 300.2 nM (IC50); PI4KIIIA: 574.1 nM (IC50) | [References]
[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 Aug 5;156:831-846. DOI:10.1016/j.ejmech.2018.07.036 |
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BOC Sciences
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1-631-485-4226; 16314854226 |
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