1-(3-(difluoromethyl)isothiazol-5-yl)-3-(2-fluoro-5-(hydroxymethyl)pyridin-4-yl)urea

Product Name: 1-(3-(difluoromethyl)isothiazol-5-yl)-3-(2-fluoro-5-(hydroxymethyl)pyridin-4-yl)urea
CAS No.: 2270879-17-7
Chemical Name: 1-(3-(difluoromethyl)isothiazol-5-yl)-3-(2-fluoro-5-(hydroxymethyl)pyridin-4-yl)urea
Synonyms: NVP-RXI570;BRM/BRG1 ATP Inhibitor-1, 10 mM in DMSO;1-(3-(difluoromethyl)isothiazol-5-yl)-3-(2-fluoro-5-(hydroxymethyl)pyridin-4-yl)urea;3-[3-(difluoromethyl)-1,2-thiazol-5-yl]-1-[2-fluoro-5-(hydroxymethyl)pyridin-4-yl]urea;Urea, N-[3-(difluoromethyl)-5-isothiazolyl]-N'-[2-fluoro-5-(hydroxymethyl)-4-pyridinyl]-;BRM/BRG1 ATP Inhibitor 1,Epigenetic Reader Domain,ATPase inhibitor,BRM/BRG-1 ATP Inhibitor-1,anticancer,BRM/BRG1 ATP Inhibitor-1,(BRG1)/SMARCA4,dual inhibitor,Inhibitor,inhibit,(BRM)/SMARCA2,BRM/BRG1 ATP Inhibitor1
CBNumber: CB35832995
Molecular Formula: C11H9F3N4O2S
Formula Weight: 318.27
MOL File: 2270879-17-7.mol

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1-(3-(difluoromethyl)isothiazol-5-yl)-3-(2-fluoro-5-(hydroxymethyl)pyridin-4-yl)urea Property

Boiling point:: 333.4±42.0 °C(Predicted)
Density: 1.659±0.06 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: DMSO: soluble
form: A solid
pka: 11.76±0.70(Predicted)
color: White to off-white

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML3545
Product name: NVP-RXI570
Purity: ≥98% (HPLC)
Packaging: 5MG
Price: $102
Updated: 2025/07/31

Sigma-Aldrich

Product number: SML3545
Product name: NVP-RXI570
Purity: ≥98% (HPLC)
Packaging: 25MG
Price: $410
Updated: 2025/07/31

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1-(3-(difluoromethyl)isothiazol-5-yl)-3-(2-fluoro-5-(hydroxymethyl)pyridin-4-yl)urea Chemical Properties,Usage,Production

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 active, potent, and 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.

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

1-(3-(difluoromethyl)isothiazol-5-yl)-3-(2-fluoro-5-(hydroxymethyl)pyridin-4-yl)urea Preparation Products And Raw materials

Raw materials

Preparation Products

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1-(3-(difluoromethyl)isothiazol-5-yl)-3-(2-fluoro-5-(hydroxymethyl)pyridin-4-yl)urea Suppliers

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2270879-17-7, 1-(3-(difluoromethyl)isothiazol-5-yl)-3-(2-fluoro-5-(hydroxymethyl)pyridin-4-yl)ureaRelated Search:

1-(3-(difluoromethyl)isothiazol-5-yl)-3-(2-fluoro-5-(hydroxymethyl)pyridin-4-yl)urea

Urea, N-[3-(difluoromethyl)-5-isothiazolyl]-N'-[2-fluoro-5-(hydroxymethyl)-4-pyridinyl]-

BRM/BRG1 ATP Inhibitor 1,Epigenetic Reader Domain,ATPase inhibitor,BRM/BRG-1 ATP Inhibitor-1,anticancer,BRM/BRG1 ATP Inhibitor-1,(BRG1)/SMARCA4,dual inhibitor,Inhibitor,inhibit,(BRM)/SMARCA2,BRM/BRG1 ATP Inhibitor1

NVP-RXI570

3-[3-(difluoromethyl)-1,2-thiazol-5-yl]-1-[2-fluoro-5-(hydroxymethyl)pyridin-4-yl]urea

BRM/BRG1 ATP Inhibitor-1, 10 mM in DMSO

2270879-17-7