NVS-BPTF-1

Chemical Structure : NVS-BPTF-1

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货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	537.614
分子式	C26H28FN7O3S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
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

参考文献

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

NVS-BPTF-1

生物&药学活性

物理化学性质&存储条件

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NVS-BPTF-1

生物&药学活性

物理化学性质&存储条件

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