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Submit ReviewFHT 2344
Description: Potent SMARCA2/4 inhibitor
Chemical Name: N-[(1S)-1-(Methoxymethyl)-2-[[4-[3-(1-methyl-1H-pyrazol-3-yl)phenyl]-2-thiazolyl]amino]-2-oxoethyl]-1-(methylsulfonyl)-1H-pyrrole-3-carboxamide
Purity: ≥95% (HPLC)
Biological Activity for FHT 2344
FHT 2344 is a potent allosteric and ATP-competitive inhibitor of SMARCA2/SMARCA4 ATPases (also known as BRM/BRG1) of the BAF complex (IC50 values are 13.8 and 26.1 nM at SMARCA2 and SMARCA4, respectively). FHT 2344 inhibits SMARCA2 transcriptional activity in a BRG1-mutant cell line and SMARCA4 transcription in a BRM-mutant cell line (IC50 values are 29.8 and 30.2 nM, respectively). Dose-dependently reduces tumor growth in a uveal melanoma xenograft model and suppresses SOX10 transcription.
Licensing Information
Sold under license from Foghorn Therapeutics
Technical Data for FHT 2344
| M. Wt | 528.6 |
| Formula | C23H24N6O5S2 |
| Storage | Store at -20°C |
| Purity | ≥95% (HPLC) |
| CAS Number | 2468058-90-2 |
| InChI Key | APLVGTKXOIMODQ-IBGZPJMESA-N |
| Smiles | COC[C@@H](C(NC1=NC(C2=CC(C3=NN(C=C3)C)=CC=C2)=CS1)=O)NC(C4=CN(S(C)(=O)=O)C=C4)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for FHT 2344
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 26.43 | 50 |
Preparing Stock Solutions for FHT 2344
The following data is based on the product molecular weight 528.6. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 3.78 mL | 18.92 mL | 37.84 mL |
| 2.5 mM | 0.76 mL | 3.78 mL | 7.57 mL |
| 5 mM | 0.38 mL | 1.89 mL | 3.78 mL |
| 25 mM | 0.08 mL | 0.38 mL | 0.76 mL |
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Product Datasheets for FHT 2344
References for FHT 2344
References are publications that support the biological activity of the product.
Centore et al (2021) Discovery of novel BAF inhibitors for the treatment of transcription factor-driven cancers. Cancer Res. 81 1224
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Keywords: FHT 2344, FHT 2344 supplier, FHT2344, SMARCA, SMARCA2, SMARCA4, potent, inhibitor, inhibitors, BRM, BRG1, BAF, complex, transcription, tumour, tumor, uveal, melanoma, xenograft, SOX10, Bromodomains, Other, ATPases, 7645, Tocris Bioscience
Citations for FHT 2344
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