| Name | FPFT-2216 |
| 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; oral or intraperitoneal) induces significant degradation of CK-1α and IKZF1 in CRBNI391V mice[1]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (6.84 mM), Sonication is recommended.
DMSO : 20 mg/mL (68.42 mM), Sonication is recommended.
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| Keywords | Phosphodiesterase (PDE) | MolecularGlues | Molecular Glues | CaseinKinase | Casein Kinase |
| Inhibitors Related | Balipodect | Theophylline monohydrate | Casein | D(+)-Raffinose pentahydrate | Theobromine | Apremilast | Isoprenaline hydrochloride | Indomethacin | Lenalidomide | Icariin | Sildenafil citrate | Doxofylline |
| Related Compound Libraries | Bioactive Compound Library | Kinase Inhibitor Library | Multi-Target Compound Library | Post-Translational Modification Compound Library | Stem Cell Differentiation Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library |
United States
