FPFT-2216

SKU: orb1689419

Description

FPFT-2216 is a molecular glue degrader targeting IKZF1, IKZF3, and CK1α, demonstrating potential antitumor and immunomodulatory activity. It is a research tool for studying hematological cancers and immune system diseases in both cellular and animal models.

Research Area

Immunology & Inflammation, Metabolism Research, Pharmacology & Drug Discovery, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 2367619-87-0
• MW: 292.31
• Purity: 99.35% (May vary between batches)
• Formula: C₁₂H₁₂N₄O₃S
• SMILES: COc1cscc1-c1cn(nn1)C1CCC(=O)NC1=O
• Target: Molecular Glues,IKZF,Casein Kinase,PDE
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.84 mM);DMSO:20 mg/mL (68.42 mM)

Bioactivity

• In Vivo:
  FPFT-2216 (30 mg/kg; oral or intraperitoneal) induces significant degradation of CK-1α and IKZF1 in CRBNI391V mice.
• In Vitro:
  FPFT-2216 (1 μM; 5 hours) not only degrades its known targets IKZF1, IKZF3, and CK1α in MOLT4 cells but also demonstrates the degradation of PDE6D. FPFT-2216 (1 μM; 0 h, 2 h, 4 h, 6 h, 16 h, 24 h) shows complete degradation of PDE6D within 2 hours, and the degradation of PDE6D persists for at least 24 hours in MOLT4 cells.FPFT-2216 (0 nM, 1.6 nM, 8 nM, 40 nM, 200 nM, 1 μM; 4 hours) exhibits over 50% degradation of PDE6D at the dose of 8 nM, with maximal degradation of PDE6D, IKZF1, IKZF3, and CK1α observed at the dose of 200 nM in MOLT4 cells. FPFT-2216 does not impede the growth of KRASG12C-dependent MIA PaCa-2 cells.FPFT-2216 (10, 20, 40 μM; 14 or 24 hours) significantly upregulates IL-2, although its effect in naive CD4+ T cells is less potent than Pomalidomide.FPFT-2216 (10 μM; 14 or 24 hours) degrades the immune modulatory drug (IMiD) ubiquitin-proteasome degradation substrates IKZF1 and CK-1α in naive CD4+ T cells.
  Read more...

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

MolecularGlues, Molecular Glues, CaseinKinase, Casein Kinase, Phosphodiesterase (PDE)

Compound Identifiers

PubChem CID

151861511