CHMFL-PI3KD-317 |
| カタログ番号GC65969 |
CHMFL-PI3KD-317 は、非常に強力で選択的な経口活性 PI3Kδ です。 IC50 が 6 nM の阻害剤であり、PI3Kα などの他のクラス I、II、および III PIKK ファミリー アイソフォームよりも 10 ～ 1500 倍以上の選択性を示します。 (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)、および PI4KIIIB (IC50、300.2 nM)。 CHMFL-PI3KD-317 は、4.3 nM の EC50 で、Raji 細胞における PI3Kδ を介した Akt T308 リン酸化を阻害します。 CHMFL-PI3KD-317 は、がん細胞に対して増殖抑制効果があります。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2244992-76-3
Sample solution is provided at 25 µL, 10mM.
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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].
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[1].
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. |
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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