2367619-87-0
Chemical Structure
FPFT-2216
- CAS No.: 2367619-87-0
- Formula:C12H12N4O3S
- Molecular Weight:292.32
IUPAC Name: 3-(4-(4-methoxythiophen-3-yl)-1H-1,2,3-triazol-1-yl)piperidine-2,6-dione
InChIKey: SKUSCUALKIOIST-UHFFFAOYSA-N
SMILES: O=C(C(N1N=NC(C2=CSC=C2OC)=C1)CC3)NC3=O
Biological Activity: FPFT-2216 is an orally active Molecular glue degrader targeting IKZF1, IKZF3, CK-1α, and PDE6D, with a DC50 of 8 nM against PDE6D. FPFT-2216 mediates ubiquitin-proteasome degradation via the CRL4CRBN E3 ubiquitin ligase complex and interacts with the non-isoprenoid-binding region of PDE6D. FPFT-2216 activates the p53 signaling pathway, inhibits the CBM complex/NF-κB pathway, upregulates IL-2, suppresses IL-1β and IL-6, and induces tumor cell Apoptosis. FPFT-2216 exhibits anticancer activity against multiple myeloma and lymphoma. FPFT-2216 can be used in research related to multiple myeloma, lymphoma, acute lymphoblastic leukemia, acute myeloid leukemia, pancreatic ductal adenocarcinoma, non-small cell lung cancer, and gastric adenocarcinoma[1][2][3][4].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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FPFT-2216 | 99.55% | FPFT-2216 is an orally active Molecular glue degrader targeting IKZF1, IKZF3, CK-1α, and PDE6D, with a DC50 of 8 nM against PDE6D. FPFT-2216 mediates ubiquitin-proteasome degradation via the CRL4CRBN E3 ubiquitin ligase complex and interacts with the non-isoprenoid-binding region of PDE6D. FPFT-2216 activates the p53 signaling pathway, inhibits the CBM complex/NF-κB pathway, upregulates IL-2, suppresses IL-1β and IL-6, and induces tumor cell Apoptosis. FPFT-2216 exhibits anticancer activity against multiple myeloma and lymphoma. FPFT-2216 can be used in research related to multiple myeloma, lymphoma, acute lymphoblastic leukemia, acute myeloid leukemia, pancreatic ductal adenocarcinoma, non-small cell lung cancer, and gastric adenocarcinoma. | ||||||||||||||||||||
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References
- [1]. Gemechu Y, et al. Humanized cereblon mice revealed two distinct therapeutic pathways of immunomodulatory drugs. Proceedings of the National Academy of Sciences of the United States of America. 2018 Nov 13;115(46):11802-11807. [Content Brief]
- [2]. Teng M, et al. Development of PDE6D and CK1α Degraders through Chemical Derivatization of FPFT-2216. Journal of medicinal chemistry. 2022 Jan 13;65(1):747-756. [Content Brief]
- [3]. Ueda Y, et al. Design, synthesis, and evaluation of a novel protein degrader FPFT-2216. Bioorganic & medicinal chemistry letters. 2025 Aug 01;123:130193. [Content Brief]
- [4]. Kanaoka D, et al. FPFT-2216, a Novel Anti-lymphoma Compound, Induces Simultaneous Degradation of IKZF1/3 and CK1α to Activate p53 and Inhibit NFκB Signaling. Cancer research communications. 2024 Feb 06;4(2):312-327.
