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NVS-BPTF-1

Chemical Structure : NVS-BPTF-1

CAS No.: 2662454-54-6

NVS-BPTF-1

Catalog No.: PC-72789Not For Human Use, Lab Use Only.

NVS-BPTF-1 is the first highly potent and selective BPTF-bromodomain inhibitor with IC50 of 56 nM in an AlphaScreen assay and Kd of 71 nM in a BLI assay.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

NVS-BPTF-1 is the first highly potent and selective BPTF-bromodomain inhibitor with IC50 of 56 nM in an AlphaScreen assay and Kd of 71 nM in a BLI assay.
NVS-BPTF-1 displays no significant interaction in DSF screen and a BROMOscan against a panel of other human bromodomains.
In HEK293 cells, NVS-BPTF-1 showed on-target activity with an IC50 of 16 nM, as measured by a nanoBRET assay.
NVS-BPTF-1 did not affect the proliferation of multiple human cancer cell lines, and NVS-BPTF-1 did not affect the level of PSMB8 and PSMB9 or TAP1 and TAP2, unlike BPTF siRNA knockdown caused effect.

Physicochemical Properties

M.Wt 537.614
Formula C26H28FN7O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

7-(1-cyclopropyl-1H-pyrazol-4-yl)-2-((2-fluoro-4-((4-methylpiperazin-1-yl)sulfonyl)phenyl)amino)-3-methyl-4H-pyrido[1,2-a]pyrimidin-4-one

References

1. Léa Mélin, et al. Bioorg Med Chem Lett. 2021 Sep 1;47:128208.

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