| Identification | Back Directory | [Name]
FHD-609 | [CAS]
2676211-64-4 | [Synonyms]
FHD-609
(S)-3-(6-(7-((1-(4-(6-(Azetidin-1-yl)-2-methyl-1-oxo-1,2-dihydro-2,7-naphthyridin-4-yl)-2,6-dimethoxybenzyl)piperidin-4-yl)methyl)-2,7-diazaspiro[3.5]nonan-2-yl)-1-oxoisoindolin-2-yl)piperidine-2,6-dione | [Molecular Formula]
C47H56N8O6 | [MOL File]
2676211-64-4.mol | [Molecular Weight]
829.02 |
| Hazard Information | Back Directory | [Uses]
FHD-609 is a PROTAC degrader and inhibitor of BRD9 (Bromodomain-containing protein 9). FHD-609 targets to ncBAF, can be used for research of wide range of cancers that contain a mutation in a BAF complex subunit. FHD-609 in combination with Telomelysin or INO5401, may play a role in adrenocortical carcinoma (ACC) treatment. (Blue: BRD9 ligand-6 (HY-49393), Black: linker (HY-168309); Pink: (S)-Deoxy-thalidomide-Br (HY-168308) )[1][2][3][4][5]. | [in vivo]
FHD-609 (1mg/kg, i.v., twice a week for 28 days) maintains BRD9 degradation levels up to 28 days and achieves anti-tumor activities in SYO-1 xenograft mouse model[3]. | Animal Model: | SYO-1 xenograft mouse model | | Dosage: | 1mg/kg | | Administration: | i.v., twice a week for 28 days | | Result: | Maintained plasma PK and BRD9 degradation levels up to 28 days, achieved dose-dependent in vivo anti-tumor activities. |
| [IC 50]
BRD9 | [References]
[1] Rechberger JS, et al. Atypical teratoid rhabdoid tumor (ATRT): disease mechanisms and potential drug targets. Expert Opin Ther Targets. 2022 Mar;26(3):187-192. DOI:10.1080/14728222.2022.2040017
[2] Hescheler DA, et al. Targeted Therapy for Adrenocortical Carcinoma: A Genomic-Based Search for Available and Emerging Options. Cancers (Basel). 2022 May 31;14(11):2721. DOI:10.3390/cancers14112721
[3] Lin M, et al. Long acting injectable FHD-609 micro-suspension: A potent BRD9 degrader with comparable efficacy, reduced frequency of dosing in preclinical models[J]. Cancer Research, 2024, 84(6_Supplement): 7185-7185.
[4] Collins M, et al. Preclinical validation of target engagement assays and investigation of mechanistic impacts of FHD-609, a clinical-stage BRD9 degrader being developed for the treatment of synovial sarcoma[J]. strategies, 2022, 36: 936-950.
[5] Liu X, et al. PROTACs in Epigenetic Cancer Therapy: Current Status and Future Opportunities. Molecules. 2023 Jan 26;28(3):1217. DOI:10.3390/molecules28031217 |
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| Company Name: |
ChemOrigin Pharm
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021-15026428026 15026428026 |
| Website: |
chemorigin.com/ |
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