RP-1664 (RP1664)

Chemical Structure : RP-1664

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货号: PC-24639Not For Human Use, Lab Use Only.

RP-1664 (RP1664) is potent, selective and orally available inhibitor of PLK4 with IC50 of 3 nM, >1900-fold selective over Aurora A/B.

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生物&药学活性

RP-1664 (RP1664) is potent, selective and orally available inhibitor of PLK4 with IC50 of 3 nM, >1900-fold selective over Aurora A/B.
RP-1664 has EC50 of 0.13 uM in PLK4 centriole depletion assay definition (CDA), and EC50 of 0.051 uM for viability assay in MCF7 cells
RP-1664 binds PLK4 with 59-fold selectivity over FAK and 3-fold selectivity over TNK1 in NanoBRET assays.
RP-1664 potently inhibits TRIM37-high cell lines with IC50 of 80 and 26 nM in cell growth assays, respectively, for CAL-148 and TRIM37 gain-carrying neuroblastoma CHP-134 cells.
RP-1664 (6, 11, and 21 mg/kg PO BID) demonstrates responsive tumor growth inhibition, stasis and regressionsin CAL-148 breast and CHP-134 neuroblastoma model.

物理化学性质&存储条件

分子量	514.56
分子式	C23H24F2N8O2S
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	5-cyclopropyl-N2-(2,6-difluoro-4-(methylsulfonyl)phenyl)-N2-methyl-6-(1-methyl-1H-imidazol-4-yl)-N4-(5-methyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine

参考文献

1. Vallée F, et al. J Med Chem. 2025 May 16. doi: 10.1021/acs.jmedchem.5c00529.

RP-1664 (RP1664)

生物&药学活性

物理化学性质&存储条件

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RP-1664 (RP1664)

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物理化学性质&存储条件

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