| Chemical Properties | Back Directory | [Boiling point ]
856.9±65.0 °C(Predicted) | [density ]
1.36±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [form ]
Solid | [pka]
11.01±0.40(Predicted) | [color ]
Light green to green | [InChIKey]
GNRGNRCQXHMQQV-ZQAZVOLISA-N | [SMILES]
N1C(=O)CC[C@H](NC2=CC=C(N3CCN([C@H]4CCN(CC5=C(OC)C=C(C6C(C)=C(C)C(=O)N(C)C=6)C=C5OC)CC4(F)F)CC3)C(F)=C2)C1=O |
| Hazard Information | Back Directory | [Uses]
CFT8634 is an orally bioavailable PROTAC BRD9 targeted degrader based on the E3 ubiquitin ligase CRBN mechanism. CFT8634 can be used for the study of synovial sarcoma and SMARCB1-deficient solid tumors (Pink: BRD9 ligand (HY-169988); Blue: E3 ligase ligand (HY-169989); Black: linker (HY-169991). CFT8634 is a heterobifunctional molecule that binds to BRD9 at one end and recruits CRBN at the other end, which can inhibit the growth of tumor cells that depend on BRD9. CFT8634 can be used for the study of SMARCB1-related cancers (such as synovial sarcoma and malignant rhabdoid tumor)[1][2][3][4]. | [in vivo]
CFT8634 (compound 18) has excellent oral bioavailability in rats with F=83%, Clobs=22 mL/min/kg, and low hERG inhibitory activity (>30 μM)[1]. | [IC 50]
Cereblon | [storage]
Store at -20°C | [References]
[1] Zeng S, et al. Current advances and development strategies of orally bioavailable PROTACs. Eur J Med Chem. 2023 Dec 5;261:115793. DOI:10.1016/j.ejmech.2023.115793
[2] Jackson, et al. "Abstract ND09: The discovery and characterization of CFT8634: A potent and selective degrader of BRD9 for the treatment of SMARCB1-perturbed cancers." Cancer Research 82.12_Supplement (2022): ND09-ND09.
[3] Poling, et al. "CFT8634, a clinical stage BRD9 Bi DAC? degrader, is active in a subset of multiple myeloma cell line models and synergistic when combined with pomalidomide." Blood 142 (2023): 6594.
[4] Poling, et al. "CFT8634, a BRD9 BiDAC? degrader, is active in a subset of multiple myeloma cell line models and synergistic when combined with pomalidomide or dexamethasone." Cancer Research 84.6_Supplement (2024): 6046-6046. |
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| Company Name: |
BOC Sciences
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| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
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