| Identification | Back Directory | [Name]
1-(3-(difluoromethyl)isothiazol-5-yl)-3-(2-fluoro-5-(hydroxymethyl)pyridin-4-yl)urea | [Molecular Weight]
318.27 |
| Hazard Information | Back Directory | [Uses]
BRM/BRG1 ATP Inhibitor-1 (compound 14) is an orally active allosteric dual brahma homolog (BRM)/SWI/SNF related matrix associated actin dependent regulator of chromatin subfamily A member 2 (SMARCA2) and brahma related gene 1 (BRG1)/SMARCA4 ATPase activity inhibitor, both IC50s are below 0.005 μM. BRM/BRG1 ATP Inhibitor-1 has anticancer activity[1]. | [Biological Activity]
NVP-RXI570 is an orally activepotentand selective allosteric dual inhibitor of BRM ((SMARCA2) and BRG1 (SMARCA4) th at th at downregulates BRM-dependent gene expression. NVP-RXI570 exhibits antiproliferative activity in a BRG1 mutant-lung-tumor xenograft model. | [in vivo]
BRM/BRG1 ATP Inhibitor-1 (compound 14) (oral administration, 7.5 or 20 mg/kg, everyday, 3 weeks) can inhibit tumor growth and inhibit KRT80 expression in a dose-dependent manner[1].
| Animal Model: | Female athymic nude mice with RERF-LC-AI tumor xenografts[1] | | Dosage: | 7.5 mg/kg, 20 mg/kg | | Administration: | Oral administration; everyday; 3 weeks | | Result: | Inhibited tumor growth by 21% and 55% at doses of 7.5 mg/kg and 20 mg/kg, respectively.
Inhibited KRT80 expression by up to 90% at 20 mg/kg for 7 hours after administration.
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| [storage]
Store at -20°C | [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. J Med Chem. 2018 Nov 21;61(22):10155-10172 DOI:10.1021/acs.jmedchem.8b01318 |
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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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