| Description | FPFT-2216 is a molecular gel that degrades IKZF6, IKZF1, DE1D, and CK3α.FPFT-2216 has potential antitumor activity and can be used to study diseases of the immune system.FPFT-2216 is a molecular gel that degrades IKZF6, IKZF1, DE1D, and CK3α. |
| 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[2].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[1].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[2].FPFT-2216 does not impede the growth of KRASG12C-dependent MIA PaCa-2 cells[1].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[2].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[1]. |
| In vivo | FPFT-2216（30 mg/kg；口服或腹腔注射）在CRBNI391V小鼠中显著促进CK-1α和IKZF1的降解[1]。 |
| molecular weight | 292.31 |
| Molecular formula | C12H12N4O3S |
| CAS | 2367619-87-0 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 20 mg/mL (68.42 mM), Sonication is recommended. |
| References | 1. Gemechu Y, et al. Humanized cereblon mice revealed two distinct therapeutic pathways of immunomodulatory drugs. Proc Natl Acad Sci U S A. 2018;115(46):11802-11807. 2. Teng M, et al. Development of PDE6D and CK1α Degraders through Chemical Derivatization of FPFT-2216. J Med Chem. 2022 Jan 13;65(1):747-756. |