CHMFL-PI3KD-317

SKU: orb1710056

Description

CHMFL-PI3KD-317 is a potent, selective, and orally bioavailable PI3Kδ inhibitor (IC50 = 6 nM). It effectively blocks PI3Kδ-mediated Akt phosphorylation in Raji cells (EC50 = 4.3 nM) and demonstrates antiproliferative activity, making it a valuable tool for oncology and immunology research in both cellular and animal models.

Research Area

Signal Transduction

Key Properties

• CAS Number: 2244992-76-3
• MW: 494.03
• Purity: 99.16% (May vary between batches)
• Formula: C₂₁H₂₄ClN₅O₃S₂
• SMILES: CC(C)[C@H](N)C(=O)Nc1nc(C)c(s1)-c1cnc(Cl)c(NS(=O)(=O)c2cccc(C)c2)c1
• Target: PI3K,PI4K
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.05 mM);DMSO:45 mg/mL (91.09 mM)

Bioactivity

• Target IC50:
  VPS34:1801.7 nM|PI3Kδ:6 nM|PIK3C2B:882.3 nM|PI4KIIIA:574.1 nM|PI3Kβ:284 nM|PI3Kα:62.6 nM|PI3Kγ:202.7 nM|PI4KIIIB:300.2 nM
• 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).
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CHMFL PI3KD 317, CHMFL-PI3KD-317, CHMFL-PI3KD 317, CHMFLPI3KD317, CHMFL-PI3KD317, CHMFL-PI-3KD-317, PI4KIIIβ, PI4KIIIα, PI4KIIIA, PI4KIIIB, PI3Kβ, PI3Kγ, PI3Kδ, PI3Kα, PIK3C2B, Vps34

Compound Identifiers

PubChem CID

137333450