| Chemical Properties | Back Directory | [Boiling point ]
354.975±42.00 °C(Press: 760.00 Torr)(predicted) | [density ]
1.678±0.06 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted) | [pka]
11.877±0.70(predicted) |
| Hazard Information | Back Directory | [Uses]
SMARCA2-IN-7 (compound 12), a dual inhibitor of BRM and BRG1 (IC50 < 0.005 for both), has an anti-tumor proliferation effect that inhibits BRG1-deleted SKMEL5 tumor proliferation with a cell proliferation activity AAC50 of 13 nM in SKMEL5. The cell proliferation activity AAC50 of KRT880 in H1299 cells was 42 nM[1]. | [References]
[1] Papillon JPN,et al. Discovery of Orally Active Inhibitors of Brahma Homolog (BRM)/SMARCA2 ATPase Activity for the Treatment of Brahma Related Gene 1 (BRG1)/SMARCA4-Mutant Cancers. Medicinal Chemistry. 2018 Nov 21;61(22):10155-10172. DOI:10.1021/acs.jmedchem.8b01318 |
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