| Name | CHMFL-PI3KD-317 |
| Description | CHMFL-PI3KD-317 is a highly potent, selective, and orally active PI3Kδ inhibitor with an IC50 of 6 nM, exhibiting 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). It inhibits PI3Kδ-mediated Akt T308 phosphorylation in Raji cells with an EC50 of 4.3 nM and has antiproliferative effects on cancer cells. |
| In vitro | CHMFL-PI3KD-317 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), PI4KIIIA (IC50, 574.1 nM) and PI4KIIIB (IC50, 300.2 nM). CHMFL-PI3KD-317 has antiproliferative effects, with GI50s of 4.0, 3.5, 4.8, 3.0, 3.3 μM against NALM-6, PF382, MV4-11, MOLM-13 cells, and MOLM-14, respectively. |
| 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 and, in Sprague-Dawley rats, shows favorable oral bioavailability and an acceptable half-life (T1/2 = 3.28 h). |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 45 mg/mL (91.09 mM), Sonication is recommended.
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| Keywords | Vps34 | PIK3C2B | PI4KIIIβ | PI4KIIIα | PI4KIIIB | PI4KIIIA | PI3Kδ | PI3Kγ | PI3Kβ | PI3Kα | CHMFL-PI3KD-317 | CHMFL-PI-3KD-317 | CHMFL-PI3KD317 | CHMFLPI3KD317 | CHMFL-PI3KD 317 | CHMFL PI3KD 317 |
| Inhibitors Related | Myricetin | Erucic acid | Sapanisertib | (2S,3R,4S)-4-Hydroxyisoleucine | 3-Methyladenine | Duvelisib (R enantiomer) hydrochloride | Isoprenaline hydrochloride | Quercetin | Inavolisib | Quercetin Dihydrate | Apilimod | Idelalisib |
| Related Compound Libraries | Anti-Colorectal Cancer Compound Library | Reprogramming Compound Library | Glycometabolism Compound Library | Bioactive Compound Library | Kinase Inhibitor Library | Anti-Breast Cancer Compound Library | Inhibitor Library | Immunology/Inflammation Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Covalent Inhibitor Library | Anti-Cancer Active Compound Library |
United States
